DGIdb - FGFR3 Gene Record

FGFR3 2261 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

2261
FIBROBLAST GROWTH FACTOR RECEPTOR 3
FGFR3
ACH
CD333
CEK2
HSFGFR3EX
JTK4
134934
3690
ENSG00000068078
OTTHUMG00000121148
CD_antigen=CD333
FGFR-3
P22607
FGFR3_HUMAN
FIBROBLAST GROWTH FACTOR RECEPTOR 3 PRECURSOR (EC 2.7.1.112) (FGFR-3). [SOURCE:UNIPROT/SWISSPROT;ACC:P22607]
FGFR1-3
1810
23
NP_000133
NM_000142
PA28129
T91331

Gene Info:

Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR001245
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Uniprot Status	Swiss-Prot
Interpro Type	Domain
Human Readable Name	KINASE
Human Readable Name	DRUGGABLE GENOME
CancerCommons Reported Gene Name	FGFRs
CancerCommons Reported Gene Name	FGFR3 and others (VEGFR)
Target Class	Receptors
Target Subclass	EC:2.7.10.1
Target Main Class	Receptors
Target Subclass	Kinase
Target Subclass	FGFR
Transmembrane Helix Count	1
GuideToPharmacology Gene Category Name	Type V RTKs: FGF (fibroblast growth factor) receptor family
GuideToPharmacology Gene Category ID	323
Gene Biotype	PROTEIN_CODING

(26 More Sources)

Gene Categories: Category Details

CELL SURFACE
KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. Cancer
Hahn et al., 2017, A Phase II Trial of Dovitinib in BCG-Unresponsive Urothelial Carcinoma with FGFR3 Mutations or Overexpression: Hoosier Cancer Research Network Trial HCRN 12-157., Clin. Cancer Res.
Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.
Hänze et al., 2013, Epithelial mesenchymal transition status is associated with anti-cancer responses towards receptor tyrosine-kinase inhibition by dovitinib in human bladder cancer cells., BMC Cancer
Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.
Goyal et al., 2017, Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma., Cancer Discov
Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
Beer et al., 2000, Fibroblast growth factor (FGF) receptor 1-IIIb is a naturally occurring functional receptor for FGFs that is preferentially expressed in the skin and the brain., J. Biol. Chem.
Cancilla et al., 2001, Fibroblast growth factor receptors and their ligands in the adult rat kidney., Kidney Int.
Launay et al., 1994, Comparative analysis of the tissue distribution of three fibroblast growth factor receptor mRNAs during amphibian morphogenesis., Differentiation
Mummery et al., 1993, Fibroblast growth factor-mediated growth regulation and receptor expression in embryonal carcinoma and embryonic stem cells and human germ cell tumours., Biochem. Biophys. Res. Commun.
Yamanaka et al., 2000, Isolation and serum-free culture of epithelial cells derived from epithelial rests of Malassez in human periodontal ligament., In Vitro Cell. Dev. Biol. Anim.
Liu PCC et al., 2020, INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models., PLoS One
Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.
Perera et al., 2017, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor., Mol. Cancer Ther.
Di Stefano et al., 2015, Detection, Characterization, and Inhibition of FGFR-TACC Fusions in IDH Wild-type Glioma., Clin. Cancer Res.
Patani et al., 2016, Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use., Oncotarget
Tabernero et al., 2015, Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors., J. Clin. Oncol.
Loriot Y et al., 2019, Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma., N Engl J Med
Nishina T et al., 2018, Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors., Invest New Drugs
Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.
Capelletti et al., 2014, Identification of recurrent FGFR3-TACC3 fusion oncogenes from lung adenocarcinoma., Clin. Cancer Res.
Gozgit et al., 2013, Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models., Cancer Chemother. Pharmacol.
Yang Z et al., 2018, Somatic FGFR3 Mutations Distinguish a Subgroup of Muscle-Invasive Bladder Cancers with Response to Neoadjuvant Chemotherapy., EBioMedicine
Pal SK et al., 2018, Efficacy of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Inhibitor, in Patients with Previously Treated Advanced Urothelial Carcinoma with <i>FGFR3</i> Alterations., Cancer Discov
Nogova et al., 2017, Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study., J. Clin. Oncol.
Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., Clin. Cancer Res.
Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., Cancer Discov
Singh et al., 2012, Transforming fusions of FGFR and TACC genes in human glioblastoma., Science
von Mässenhausen et al., 2016, Evaluation of FGFR3 as a Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Target Oncol
Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.
Zhao et al., 2011, A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models., Mol. Cancer Ther.
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
St-Germain et al., 2009, Multiple myeloma phosphotyrosine proteomic profile associated with FGFR3 expression, ligand activation, and drug inhibition., Proc. Natl. Acad. Sci. U.S.A.
Watanabe Miyano et al., 2016, E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models., Mol. Cancer Ther.
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
Xie X et al., 2019, FGFR<sup>3S249C</sup> mutation promotes chemoresistance by activating Akt signaling in bladder cancer cells., Exp Ther Med
Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov
Deeks, 2012, Pazopanib: in advanced soft tissue sarcoma., Drugs
Sethakorn N et al., 2016, Spectrum of genomic alterations in FGFR3: current appraisal of the potential role of FGFR3 in advanced urothelial carcinoma., BJU Int
Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.
Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.
Chell et al., 2013, Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance., Oncogene
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.

VOFATAMAB FGFR3

Interaction Score: 2.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type multiple myeloma

Response Type sensitive

Approval Status Phase I

PMIDs:
None found

Sources:
JAX-CKB TTD
ERDAFITINIB FGFR3

Interaction Score: 1.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28341788 25609060 26992226 26324363 31340094 28965185

Sources:
JAX-CKB CIViC GuideToPharmacology PharmGKB OncoKB
E-7090 FGFR3

Interaction Score: 1.37

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
19901323 23175443 27535969

Sources:
JAX-CKB
LY-2874455 FGFR3

Interaction Score: 1.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
23175443 28034880 21900693

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology
PALIFERMIN FGFR3

Interaction Score: 1.2

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance

Novel drug target Established target

PMIDs:
10821861 11422746 7890137 7680555 11149756

Sources:
TdgClinicalTrial TEND
PEMIGATINIB FGFR3

Interaction Score: 1.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
32315352

Sources:
JAX-CKB GuideToPharmacology
INFIGRATINIB FGFR3

Interaction Score: 0.89

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
29848605 27870574 27401245 23002168 25589496 25294908 22837387 27053219 28034880 26270481 27998968

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB
ROGARATINIB FGFR3

Interaction Score: 0.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology
FUTIBATINIB FGFR3

Interaction Score: 0.51

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
JAX-CKB GuideToPharmacology
DERAZANTINIB FGFR3

Interaction Score: 0.51

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
TRAPIDIL FGFR3

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BRIVANIB FGFR3

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
22238366 20124951

Sources:
JAX-CKB ChemblInteractions PharmGKB
NINTEDANIB FGFR3

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Indication/Tumor Type urinary bladder cancer

Evidence Type Actionable

PMIDs:
22238366 18559524 31016670

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB GuideToPharmacology
DEBIO-1347 FGFR3

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology OncoKB
PONATINIB FGFR3

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
25294908 28034880 22238366 23468082

Sources:
TALC MyCancerGenome JAX-CKB CIViC
RO-4987655 FGFR3

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type bladder transitional cell papilloma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26438159

Sources:
JAX-CKB
BRIVANIB ALANINATE FGFR3

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD
TRAFERMIN FGFR3

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name trafermin, fibro/

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
AZD-4547 FGFR3

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CAPIVASERTIB FGFR3

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26351323

Sources:
JAX-CKB
MASITINIB FGFR3

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
FP-1039 FGFR3

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name FP-1039

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
DOVITINIB FGFR3

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Indication/Tumor Type bladder urothelial carcinoma

Approval Status Preclinical - Cell culture

PMIDs:
21119661 27932416 25589496 24325461 23175443 28034880 22238366

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons TTD
ENMD-2076 FGFR3

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions
AEE-788 FGFR3

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MK-2461 FGFR3

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD
CP-459632 FGFR3

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
XL-228 FGFR3

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome
PAZOPANIB FGFR3

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
23558953 23072642 27271022

Sources:
JAX-CKB CIViC
RABEPRAZOLE SODIUM FGFR3

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome TTD
NINTEDANIB ESYLATE FGFR3

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
BORTEZOMIB FGFR3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
20542753 26619011 19331127 21273588 22869148 25157968 19381019

Sources:
CGI DoCM
ORANTINIB FGFR3

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PAZOPANIB HYDROCHLORIDE FGFR3

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XL-999 FGFR3

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CEDIRANIB FGFR3

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
25589496 22238366

Sources:
DTC JAX-CKB
BUPARLISIB FGFR3

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
28108151

Sources:
JAX-CKB
SELUMETINIB FGFR3

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type no benefit

Approval Status Preclinical

PMIDs:
26438159

Sources:
JAX-CKB
TRAMETINIB FGFR3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung cancer

Response Type no benefit

Approval Status Preclinical

PMIDs:
27338794

Sources:
JAX-CKB
DACTOLISIB FGFR3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

PMIDs:
26270481

Sources:
JAX-CKB
CHEMBL578061 FGFR3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MLN-8054 FGFR3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENMD-981693 FGFR3

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SORAFENIB FGFR3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

PMIDs:
26270481

Sources:
DTC JAX-CKB
ALPELISIB FGFR3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type transitional cell carcinoma

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB
HESPERADIN FGFR3

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
GEMCITABINE FGFR3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29941343

Sources:
CIViC
ALISERTIB FGFR3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OSI-632 FGFR3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CISPLATIN FGFR3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29941343 31316618

Sources:
CIViC
ENTRECTINIB FGFR3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LINIFANIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
R-406 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SP-600125 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

Ensembl: ENSG00000068078
- Version: 101_38
Alternate Names:

FGFR3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P22607
- Version: 01-August-2011
Alternate Names:

ENSG00000068078 Ensembl Gene Id

FGFR3_HUMAN Uniprot Id

2261 Entrez Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass Kinase

Target Subclass FGFR

Publications:
TdgClinicalTrial: P22607
- Version: January-2014
Alternate Names:

FGFR3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:
RussLampel: ENSG00000068078
- Version: 26-July-2011
Alternate Names:

FGFR3 Display Id

ENSG00000068078 Ensembl Gene Id

FIBROBLAST GROWTH FACTOR RECEPTOR 3 PRECURSOR (EC 2.7.1.112) (FGFR-3). [SOURCE:UNIPROT/SWISSPROT;ACC:P22607] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: P22607
- Version: 11-September-2012
Alternate Names:

FGFR3 Uniprot Gene Name

FGFR3_HUMAN Uniprot Id

P22607 Uniprot Accession

Gene Info:

Uniprot Evidence 1: Evidence at protein level

Interpro Acc IPR001245

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
CancerCommons: FGFR3
- Version: 25-July-2013
Alternate Names:

2261 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name FGFRs

CancerCommons Reported Gene Name FGFR3 and others (VEGFR)

Publications:
GuideToPharmacology: 2261
- Version: 29-September-2020
Alternate Names:

3690 HUGO Gene ID

3690 HUGO Gene Symbol

fibroblast growth factor receptor 3 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type V RTKs: FGF (fibroblast growth factor) receptor family

GuideToPharmacology Gene Category ID 323

Publications:

JAX-CKB: FGFR3

Version: 27-September-2017

Alternate Names:

2261 CKB Entrez Id

FGFR3 CKB Gene Synonym

ACH CKB Gene Synonym

Gene Info:

Publications:

Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.

Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.

Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE

PharmGKB: FGFR3
- Version: 18-August-2020
Alternate Names:

PA28129 PharmGKB ID

Gene Info:

Publications:

Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics

CIViC: FGFR3

Version: 14-September-2020

Alternate Names:

2261 Entrez Gene ID

23 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE, CLINICALLY ACTIONABLE

Publications:

Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.

Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov

Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. Cancer

CGI: FGFR3

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.

Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.

DoCM: FGFR3

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.

Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol

DTC: FGFR3
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
HingoraniCasas: ENSG00000068078
- Version: 31-May-2017
Alternate Names:

ENSG00000068078 Gene Symbol

FGFR3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: FGFR-3
- Version: 12-May-2016
Alternate Names:

FGFR-3 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: JTK4
- Version: chembl_23
Alternate Names:

JTK4 GENE_SYMBOL

FGFR3 GENE_SYMBOL

Fibroblast growth factor receptor 3 UNIPROT

Gene Info:

Publications:
MyCancerGenome: FGFR3
- Version: 20-Jun-2017
Alternate Names:

2261 Entrez Gene Id

FGFR3 MyCancerGenome Gene Symbol

FGFR1-3 MyCancerGenome Reported Gene Name

Gene Info:

Publications:
TALC: FGFR3
- Version: 12-May-2016
Alternate Names:

FGFR3 Gene Symbol

Gene Info:

Publications:
OncoKB: FGFR3
- Version: 23-July-2020
Alternate Names:

2261 OncoKB Entrez Id

JTK4 OncoKB Gene Synonym

HSFGFR3EX OncoKB Gene Synonym

Gene Info:

Publications:
Tempus: FGFR3
- Version: 11-November-2018
Alternate Names:

FGFR3 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: FGFR3
- Version: 27-Jun-2013
Alternate Names:

2261 Gene ID

ACH dGene Synonym

CD333 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Fibroblast growth factor receptor 3
- Version: 2020.06.01
Alternate Names:

FGFR3 TTD Gene Abbreviation

T91331 TTD Target ID

Gene Info:

Publications:
GO: FGFR3
- Version: 01-May-2021
Alternate Names:

JTK4 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, TYROSINE KINASE

Publications:
Pharos: FGFR3
- Version: 01-May-2021
Alternate Names:

Fibroblast growth factor receptor 3 Gene Name

P22607 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
ClearityFoundationClinicalTrial: FGFR3
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: FGFR3
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
MskImpact: FGFR3
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: FGFR3
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: FGFR3
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: FGFR3
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Indication/Tumor Type	multiple myeloma
Response Type	sensitive
Approval Status	Phase I

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Indication/Tumor Type	breast carcinoma
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

Trial Name	rHu-KGF, keratinocyte growth factor (KGF),Kepivance
Novel drug target	Established target

Evidence Type	Actionable
Approval Status	Preclinical - Cell line xenograft
Response Type	sensitive

Notes
Mechanism of Interaction	Fibroblast growth factor receptor inhibitor
Direct Interaction	yes

Response Type	resistant
Indication/Tumor Type	urinary bladder cancer
Evidence Type	Actionable

Indication/Tumor Type	bladder transitional cell papilloma
Response Type	no benefit
Approval Status	Preclinical - Cell culture

Trial Name	trafermin, fibro/
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	Fibroblast growth factor receptor 3 inhibitor

Notes
Indication/Tumor Type	bladder urothelial carcinoma
Approval Status	Preclinical - Cell culture

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

Indication/Tumor Type	lung cancer
Response Type	no benefit
Approval Status	Preclinical

combination therapy	Sorafenib + BEZ235
Indication/Tumor Type	urinary bladder cancer
Response Type	sensitive

combination therapy	BGJ398 + BYL719
Indication/Tumor Type	transitional cell carcinoma
Response Type	predicted – sensitive

ENSG00000068078	Ensembl Gene Id
FGFR3_HUMAN	Uniprot Id
2261	Entrez Gene Id

FGFR3	Display Id
ENSG00000068078	Ensembl Gene Id
FIBROBLAST GROWTH FACTOR RECEPTOR 3 PRECURSOR (EC 2.7.1.112) (FGFR-3). [SOURCE:UNIPROT/SWISSPROT;ACC:P22607]	Description

FGFR3	Uniprot Gene Name
FGFR3_HUMAN	Uniprot Id
P22607	Uniprot Accession

3690	HUGO Gene ID
3690	HUGO Gene Symbol
fibroblast growth factor receptor 3	HUGO Gene Name

FGFR3 Gene Record

FGFR3 2261 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type multiple myeloma Response Type sensitive Approval Status Phase I

PMIDs: None found

Sources: JAX-CKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 28341788 25609060 26992226 26324363 31340094 28965185

Sources: JAX-CKB CIViC GuideToPharmacology PharmGKB OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast carcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 19901323 23175443 27535969

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical

PMIDs: 23175443 28034880 21900693

Sources: JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance Novel drug target Established target

PMIDs: 10821861 11422746 7890137 7680555 11149756

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell line xenograft Response Type sensitive

PMIDs: 32315352

Sources: JAX-CKB GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Mechanism of Interaction Fibroblast growth factor receptor inhibitor Direct Interaction yes

PMIDs: 29848605 27870574 27401245 23002168 25589496 25294908 22837387 27053219 28034880 26270481 27998968

Sources: TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: JAX-CKB GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Fibroblast growth factor receptor inhibitor Direct Interaction yes Indication/Tumor Type Advanced Solid Tumor

PMIDs: 22238366 20124951

Sources: JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type resistant Indication/Tumor Type urinary bladder cancer Evidence Type Actionable

PMIDs: 22238366 18559524 31016670

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type resistant Approval Status Preclinical - Cell line xenograft Response Type predicted – sensitive

PMIDs: 25294908 28034880 22238366 23468082

Sources: TALC MyCancerGenome JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type bladder transitional cell papilloma Response Type no benefit Approval Status Preclinical - Cell culture

PMIDs: 26438159

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name trafermin, fibro/ Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type multiple myeloma

Response Type sensitive

Approval Status Phase I

PMIDs:
None found

Sources:
JAX-CKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28341788 25609060 26992226 26324363 31340094 28965185

Sources:
JAX-CKB CIViC GuideToPharmacology PharmGKB OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
19901323 23175443 27535969

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
23175443 28034880 21900693

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance

Novel drug target Established target

PMIDs:
10821861 11422746 7890137 7680555 11149756

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
32315352

Sources:
JAX-CKB GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
29848605 27870574 27401245 23002168 25589496 25294908 22837387 27053219 28034880 26270481 27998968

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
JAX-CKB GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
22238366 20124951

Sources:
JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Indication/Tumor Type urinary bladder cancer

Evidence Type Actionable

PMIDs:
22238366 18559524 31016670

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
25294908 28034880 22238366 23468082

Sources:
TALC MyCancerGenome JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type bladder transitional cell papilloma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26438159

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name trafermin, fibro/

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26351323

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

JTK4	GENE_SYMBOL
FGFR3	GENE_SYMBOL
Fibroblast growth factor receptor 3	UNIPROT

2261	OncoKB Entrez Id
JTK4	OncoKB Gene Synonym
HSFGFR3EX	OncoKB Gene Synonym

Fibroblast growth factor receptor 3	Gene Name
P22607	UniProt ID