DGIdb - AKT1 Gene Record

AKT1 207 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

207
AKT SERINE/THREONINE KINASE 1
AKT1
AKT
CWS6
PKB
PKB-ALPHA
PRKBA
RAC
RAC-ALPHA
164730
391
ENSG00000142208
OTTHUMG00000170795
Proto-oncogene c-Akt
PKB alpha
RAC-PK-alpha
Protein kinase B alpha
Protein kinase B
RAC-alpha serine/threonine-protein kinase
2
P31749
AKT1_HUMAN
PA24684
1479
NP_001014431
NM_001014431
RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (RAC-PK-ALPHA) (PROTEIN KINASE B) (PKB) (C-AKT). [SOURCE:UNIPROT/SWISSPROT;ACC:P31749]
T67619

Gene Info:

GuideToPharmacology Gene Category ID	285
Human Readable Name	DRUGGABLE GENOME
CancerCommons Reported Gene Name	AKT
Target Class	Enzymes
Target Subclass	EC:2.7.11.1
Uniprot Status	Swiss-Prot
Human Readable Name	KINASE
Interpro Name	Serine/threonine- / dual-specificity protein kinase, catalytic domain
Interpro Short Name	Ser/Thr_dual-sp_kinase_dom
Interpro Type	Domain
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR002290
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	Akt (Protein kinase B, PKB) family

(26 More Sources)

Gene Categories: Category Details

TRANSPORTER
KINASE
SERINE THREONINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME
TRANSCRIPTION FACTOR

Publications:

Saura et al., 2017, A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors., Cancer Discov
Blake JF et al., 2012, Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors., J Med Chem
Jang SW et al., 2007, Gambogic amide, a selective agonist for TrkA receptor that possesses robust neurotrophic activity, prevents neuronal cell death., Proc Natl Acad Sci U S A
Lassen et al., 2014, Effects of AKT inhibitor therapy in response and resistance to BRAF inhibition in melanoma., Mol. Cancer
Dumble et al., 2014, Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor., PLoS ONE
Pachl et al., 2013, Characterization of a chemical affinity probe targeting Akt kinases., J. Proteome Res.
Gungor et al., 2015, Dose-Finding Quantitative 18F-FDG PET Imaging Study with the Oral Pan-AKT Inhibitor GSK2141795 in Patients with Gynecologic Malignancies., J. Nucl. Med.
Vivanco et al., 2014, A kinase-independent function of AKT promotes cancer cell survival., Elife
Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
Kammasud et al., 2009, 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases., Bioorg. Med. Chem. Lett.
Xu JL et al., 2012, Genetic variants in the PI3K/PTEN/AKT/mTOR pathway predict platinum-based chemotherapy response of advanced non-small cell lung cancers in a Chinese population., Asian Pac J Cancer Prev
Sasano et al., 2015, Preclinical Efficacy for AKT Targeting in Clear Cell Carcinoma of the Ovary., Mol. Cancer Res.
Ikeda M et al., 2008, Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia., Pharmacogenomics
Ai Y et al., 2015, Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer., J Med Chem
Mavrakis et al., 2008, Tumorigenic activity and therapeutic inhibition of Rheb GTPase., Genes Dev.
Venkatesan et al., 2010, Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor., J. Med. Chem.
Karelia N et al., 2010, Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells., Bioorg Med Chem Lett
Myers et al., 2016, Tumor mutational analysis of GOG248, a phase II study of temsirolimus or temsirolimus and alternating megestrol acetate and tamoxifen for advanced endometrial cancer (EC): An NRG Oncology/Gynecologic Oncology Group study., Gynecol. Oncol.
Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov
Weller et al., 2017, Durable Control of Metastatic AKT1-Mutant WHO Grade 1 Meningothelial Meningioma by the AKT Inhibitor, AZD5363., J. Natl. Cancer Inst.
Hyman et al., 2017, AKT Inhibition in Solid Tumors With AKT1 Mutations., J. Clin. Oncol.
Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.
Tamura et al., 2016, Safety and tolerability of AZD5363 in Japanese patients with advanced solid tumors., Cancer Chemother. Pharmacol.
Garrett et al., 2011, Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT., Invest New Drugs
Kastrinsky DB et al., 2015, Reengineered tricyclic anti-cancer agents., Bioorg Med Chem
Fiorino F et al., 2011, Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents., Eur J Med Chem
Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
Itoh T et al., 2008, Eupalinin A isolated from Eupatorium chinense L. induces autophagocytosis in human leukemia HL60 cells., Bioorg Med Chem
Chen HW et al., 2011, Inhibition of TNF-α-Induced Inflammation by andrographolide via down-regulation of the PI3K/Akt signaling pathway., J Nat Prod
Kim EJ et al., 2010, OGA inhibition by GlcNAc-selenazoline., Bioorg Med Chem
Kaneko R et al., 2007, Survivin down-regulation plays a crucial role in 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor-induced apoptosis in cancer., J Biol Chem
Allen et al., 2013, Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects., Sci Transl Med
Tirosh et al., 1999, Oxidative stress disrupts insulin-induced cellular redistribution of insulin receptor substrate-1 and phosphatidylinositol 3-kinase in 3T3-L1 adipocytes. A putative cellular mechanism for impaired protein kinase B activation and GLUT4 translocation., J. Biol. Chem.
Shome D et al., 2008, Ulcerative keratitis in gastrointestinal stromal tumor patients treated with perifosine., Ophthalmology
Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
Okuzumi T et al., 2009, Inhibitor hijacking of Akt activation., Nat Chem Biol
Won et al., 2006, Small molecule-based reversible reprogramming of cellular lifespan., Nat. Chem. Biol.
Hudkins RL et al., 2012, Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent., J Med Chem
Hechtman et al., 2015, AKT1 E17K in Colorectal Carcinoma Is Associated with BRAF V600E but Not MSI-H Status: A Clinicopathologic Comparison to PIK3CA Helical and Kinase Domain Mutants., Mol. Cancer Res.
Rodina A et al., 2007, Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer., Nat Chem Biol
Su JL et al., 2007, Forkhead proteins are critical for bone morphogenetic protein-2 regulation and anti-tumor activity of resveratrol., J Biol Chem
Hsieh TC et al., 2014, Biochemical and cellular evidence demonstrating AKT-1 as a binding partner for resveratrol targeting protein NQO2., PLoS One
Charoenrungruang S et al., 2014, Gigantol, a bibenzyl from Dendrobium draconis, inhibits the migratory behavior of non-small cell lung cancer cells., J Nat Prod
Samadi AK et al., 2010, Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma., J Nat Prod

GIGANTOL AKT1

Interaction Score: 1.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24844664

Sources:
DTC
EUPALININ A AKT1

Interaction Score: 1.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17980607

Sources:
DTC
CHEMBL1086397 AKT1

Interaction Score: 1.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20855208

Sources:
DTC
CHEMBL480356 AKT1

Interaction Score: 1.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19110422

Sources:
DTC
IPATASERTIB AKT1

Interaction Score: 1.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase II

Response Type predicted – sensitive

Indication/Tumor Type triple-receptor negative breast cancer

PMIDs:
27872130 22934575

Sources:
DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial TTD
CAPIVASERTIB AKT1

Interaction Score: 1.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type ovarian cancer

Evidence Type Actionable

Approval Status Phase I

PMIDs:
28376212 28489509 26351323 26931343

Sources:
MyCancerGenome ClearityFoundationClinicalTrial JAX-CKB CIViC GuideToPharmacology TTD OncoKB
PERIFOSINE AKT1

Interaction Score: 1.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name perifosine, KRX-0401

Novel drug target Novel Target

Indication/Tumor Type ovarian clear cell carcinoma

PMIDs:
25519148 18201764

Sources:
TALC TdgClinicalTrial JAX-CKB MyCancerGenomeClinicalTrial
UPROSERTIB AKT1

Interaction Score: 1.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
24735930 24978597 23795919 26429956

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology
CANTHIN-6-ONE AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL258844 AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17603540

Sources:
DTC
5-METHOXYCANTHINONE AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ARCHEXIN AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name RX-0201 ,Archexin

combination therapy Everolimus + RX-0201

PMIDs:
None found

Sources:
TdgClinicalTrial JAX-CKB TTD
TRICIRIBINE AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type no benefit

PMIDs:
20644979

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB
CHEMBL379218 AKT1

Interaction Score: 0.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
AFURESERTIB AKT1

Interaction Score: 0.66

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD
MK-2206 AKT1

Interaction Score: 0.62

Interaction Types & Directionality:

allosteric modulator

inhibitory allosteric modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

combination therapy MK2206 + Vemurafenib

Indication/Tumor Type melanoma

PMIDs:
25551293 24265152

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial
MIRANSERTIB AKT1

Interaction Score: 0.58

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
ANDROGRAPHOLIDE AKT1

Interaction Score: 0.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22026410

Sources:
DTC
BAY-1125976 AKT1

Interaction Score: 0.44

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL257158 AKT1

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20822912

Sources:
DTC
CMX-2043 AKT1

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ONC-201 AKT1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
23390247

Sources:
JAX-CKB
XL-418 AKT1

Interaction Score: 0.35

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
TRICIRIBINE PHOSPHATE AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SR-13668 AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MK-2201 AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MSC-2363318A AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD
AZD-5363 AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
GAMBOGIC AMIDE AKT1

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17911251

Sources:
DTC
BARDOXOLONE METHYL AKT1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25675144

Sources:
DTC
A-443654 AKT1

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
19465931

Sources:
DTC GuideToPharmacology
LY-294002 AKT1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16767085

Sources:
DTC
LY-2780301 AKT1

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
WITHAFERIN A AKT1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20726569

Sources:
DTC
NELFINAVIR AKT1

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
CANERTINIB AKT1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TOPOTECAN AKT1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21440338

Sources:
DTC
TEMSIROLIMUS AKT1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted – sensitive

PMIDs:
27016228

Sources:
JAX-CKB
CEP-11981 AKT1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22148921

Sources:
DTC
DABRAFENIB AKT1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24265155

Sources:
CIViC
VEMURAFENIB AKT1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type sensitive

combination therapy MK2206 + Vemurafenib

Evidence Type Actionable

PMIDs:
24265152

Sources:
JAX-CKB CIViC
ENZASTAURIN AKT1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NINTEDANIB AKT1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18559524

Sources:
DTC
GSK-690693 AKT1

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
BMS-754807 AKT1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
EVEROLIMUS AKT1

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Phase Ib/II

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB CGI MyCancerGenomeClinicalTrial
TRIFLUOPERAZINE AKT1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26372073

Sources:
DTC
GEDATOLISIB AKT1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20166697

Sources:
DTC
PICTILISIB AKT1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type resistant

PMIDs:
27604488

Sources:
JAX-CKB
RESVERATROL AKT1

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17513867 24968355

Sources:
DTC
ALPELISIB AKT1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
27604488

Sources:
JAX-CKB
WORTMANNIN AKT1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10187855

Sources:
NCI
OMIPALISIB AKT1

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
LOVASTATIN AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17472962

Sources:
DTC
CETUXIMAB AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Irinotecan

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
25714871

Sources:
JAX-CKB
CI-1040 AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
APITOLISIB AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type endometrial cancer

Response Type sensitive

Approval Status Phase II

PMIDs:
None found

Sources:
JAX-CKB
IRINOTECAN AKT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Irinotecan

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
25714871

Sources:
JAX-CKB
LAUROGUADINE AKT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SIROLIMUS AKT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type predicted – sensitive

combination therapy Doxorubicin + Sirolimus

Evidence Type Actionable

PMIDs:
18708578

Sources:
JAX-CKB
FASUDIL AKT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RISPERIDONE AKT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18855532

Sources:
PharmGKB
CISPLATIN AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cisplatin + Perifosine

Indication/Tumor Type ovarian clear cell carcinoma

Response Type predicted – sensitive

PMIDs:
22901187 25519148

Sources:
JAX-CKB PharmGKB
CARBOPLATIN AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22901187

Sources:
PharmGKB
GSK-269962A AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOXORUBICIN AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lymphoma

Response Type decreased response

Approval Status Preclinical - Cell line xenograft

PMIDs:
18708578

Sources:
JAX-CKB
SOTRASTAURIN AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB AKT1

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome
CHEMBL225519 AKT1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEMCITABINE AKT1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cisplatin + Gemcitabine + Sorafenib

Indication/Tumor Type invasive bladder transitional cell carcinoma

Response Type predicted – resistant

PMIDs:
None found

Sources:
JAX-CKB
SORAFENIB AKT1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cisplatin + Gemcitabine + Sorafenib

Indication/Tumor Type invasive bladder transitional cell carcinoma

Response Type predicted – resistant

PMIDs:
None found

Sources:
JAX-CKB
CYC-116 AKT1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PACLITAXEL AKT1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ipatasertib + Paclitaxel

Indication/Tumor Type triple-receptor negative breast cancer

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB

Ensembl: ENSG00000142208
- Version: 101_38
Alternate Names:

AKT1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P31749
- Version: January-2014
Alternate Names:

AKT1 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.11.1

Publications:

RussLampel: ENSG00000142208

Version: 26-July-2011

Alternate Names:

RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (RAC-PK-ALPHA) (PROTEIN KINASE B) (PKB) (C-AKT). [SOURCE:UNIPROT/SWISSPROT;ACC:P31749] Description

ENSG00000142208 Ensembl Gene Id

AKT1 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P31749
- Version: 11-September-2012
Alternate Names:

P31749 Uniprot Accession

RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE Uniprot Protein Name

207 Entrez Gene Id

Gene Info:

Uniprot Status Swiss-Prot

Human Readable Name KINASE

Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
CancerCommons: AKT1
- Version: 25-July-2013
Alternate Names:

207 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name AKT

Publications:
GuideToPharmacology: 207
- Version: 29-September-2020
Alternate Names:

391 HUGO Gene ID

391 HUGO Gene Symbol

AKT serine/threonine kinase 1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Akt (Protein kinase B, PKB) family

GuideToPharmacology Gene Category ID 285

Gene Categories:

ENZYME

Publications:

JAX-CKB: AKT1

Version: 27-September-2017

Alternate Names:

207 CKB Entrez Id

AKT1 CKB Gene Synonym

AKT CKB Gene Synonym

Gene Info:

Publications:

Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov

Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov

Sasano et al., 2015, Preclinical Efficacy for AKT Targeting in Clear Cell Carcinoma of the Ovary., Mol. Cancer Res.

PharmGKB: AKT1

Version: 18-August-2020

Alternate Names:

PA24684 PharmGKB ID

Gene Info:

Publications:

Ikeda M et al., 2008, Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia., Pharmacogenomics

Xu JL et al., 2012, Genetic variants in the PI3K/PTEN/AKT/mTOR pathway predict platinum-based chemotherapy response of advanced non-small cell lung cancers in a Chinese population., Asian Pac J Cancer Prev

CIViC: AKT1

Version: 14-September-2020

Alternate Names:

207 Entrez Gene ID

2 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.

Hyman et al., 2017, AKT Inhibition in Solid Tumors With AKT1 Mutations., J. Clin. Oncol.

Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov

NCI: AKT1

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Tirosh et al., 1999, Oxidative stress disrupts insulin-induced cellular redistribution of insulin receptor substrate-1 and phosphatidylinositol 3-kinase in 3T3-L1 adipocytes. A putative cellular mechanism for impaired protein kinase B activation and GLUT4 translocation., J. Biol. Chem.

DTC: AKT1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Jang SW et al., 2007, Gambogic amide, a selective agonist for TrkA receptor that possesses robust neurotrophic activity, prevents neuronal cell death., Proc Natl Acad Sci U S A

Venkatesan et al., 2010, Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor., J. Med. Chem.

Karelia N et al., 2010, Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells., Bioorg Med Chem Lett

HingoraniCasas: ENSG00000142208
- Version: 31-May-2017
Alternate Names:

ENSG00000142208 Gene Symbol

AKT1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
MyCancerGenome: AKT1
- Version: 20-Jun-2017
Alternate Names:

207 Entrez Gene Id

AKT1 MyCancerGenome Gene Symbol

AKT MyCancerGenome Reported Gene Name

Gene Info:

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

AKT Gene Symbol

Gene Info:

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

RAC GENE_SYMBOL

AKT1 GENE_SYMBOL

RAC-alpha serine/threonine-protein kinase UNIPROT

Gene Info:

Publications:
OncoKB: AKT1
- Version: 23-July-2020
Alternate Names:

207 OncoKB Entrez Id

PRKBA OncoKB Gene Synonym

RAC OncoKB Gene Synonym

Gene Info:

Publications:
HumanProteinAtlas: AKT1
- Version: 19.3
Alternate Names:

ENSG00000142208 Ensembl Gene ID

AKT Human Protein Atlas Gene Synonym

PKB Human Protein Atlas Gene Synonym

Gene Info:

Gene Categories:

ENZYME

Publications:
Tempus: AKT1
- Version: 11-November-2018
Alternate Names:

AKT1 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: AKT1
- Version: 27-Jun-2013
Alternate Names:

207 Gene ID

AKT dGene Synonym

PKB dGene Synonym

Gene Info:

Gene Categories:

KINASE, SERINE THREONINE KINASE

Publications:
TTD: RAC-alpha serine/threonine-protein kinase
- Version: 2020.06.01
Alternate Names:

AKT1 TTD Gene Abbreviation

T67619 TTD Target ID

Gene Info:

Publications:
GO: AKT1
- Version: 01-May-2021
Alternate Names:

PKB GO Gene Synonym

RAC GO Gene Synonym

Gene Info:

Gene Categories:

KINASE, SERINE THREONINE KINASE

Publications:
Pharos: AKT1
- Version: 01-May-2021
Alternate Names:

RAC-alpha serine/threonine-protein kinase Gene Name

P31749 UniProt ID

Gene Info:

Gene Categories:

TRANSPORTER, KINASE, TRANSCRIPTION FACTOR

Publications:
CGI: AKT1
- Version: 27-September-2017
Alternate Names:

Gene Info:

Publications:
MskImpact: AKT1
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
MyCancerGenomeClinicalTrial: AKT1
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
ClearityFoundationClinicalTrial: AKT1
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
ClearityFoundationBiomarkers: AKT1
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
FoundationOneGenes: AKT1
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: AKT1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: AKT1
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Approval Status	Phase II
Response Type	predicted – sensitive
Indication/Tumor Type	triple-receptor negative breast cancer

Indication/Tumor Type	ovarian cancer
Evidence Type	Actionable
Approval Status	Phase I

Trial Name	perifosine, KRX-0401
Novel drug target	Novel Target
Indication/Tumor Type	ovarian clear cell carcinoma

Direct Interaction	yes
Mechanism of Interaction	Serine/threonine-protein kinase AKT inhibitor
Specific Action of the Ligand	Inhibition

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

Notes
combination therapy	MK2206 + Vemurafenib
Indication/Tumor Type	melanoma

Indication/Tumor Type	Advanced Solid Tumor
Response Type	predicted – sensitive
Approval Status	Preclinical - Cell line xenograft

Response Type	sensitive
combination therapy	MK2206 + Vemurafenib
Evidence Type	Actionable

Indication/Tumor Type	breast cancer
Response Type	resistant
Approval Status	Preclinical - Cell culture

combination therapy	Cetuximab + Irinotecan
Indication/Tumor Type	colorectal cancer
Response Type	resistant

allosteric modulator
inhibitory allosteric modulator (inhibitory)
inhibitor (inhibitory)

allosteric modulator
inhibitor (inhibitory)

Indication/Tumor Type	endometrial cancer
Response Type	sensitive
Approval Status	Phase II

combination therapy	Cisplatin + Perifosine
Indication/Tumor Type	ovarian clear cell carcinoma
Response Type	predicted – sensitive

Indication/Tumor Type	lymphoma
Response Type	decreased response
Approval Status	Preclinical - Cell line xenograft

combination therapy	Cisplatin + Gemcitabine + Sorafenib
Indication/Tumor Type	invasive bladder transitional cell carcinoma
Response Type	predicted – resistant

combination therapy	Ipatasertib + Paclitaxel
Indication/Tumor Type	triple-receptor negative breast cancer
Response Type	predicted – sensitive

RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (RAC-PK-ALPHA) (PROTEIN KINASE B) (PKB) (C-AKT). [SOURCE:UNIPROT/SWISSPROT;ACC:P31749]	Description
ENSG00000142208	Ensembl Gene Id
AKT1	Display Id

P31749	Uniprot Accession
RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE	Uniprot Protein Name
207	Entrez Gene Id

391	HUGO Gene ID
391	HUGO Gene Symbol
AKT serine/threonine kinase 1	HUGO Gene Name

207	Entrez Gene Id
AKT1	MyCancerGenome Gene Symbol
AKT	MyCancerGenome Reported Gene Name

RAC	GENE_SYMBOL
AKT1	GENE_SYMBOL
RAC-alpha serine/threonine-protein kinase	UNIPROT

AKT1 Gene Record

AKT1 207 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24844664

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17980607

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20855208

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19110422

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Approval Status Phase II Response Type predicted – sensitive Indication/Tumor Type triple-receptor negative breast cancer

PMIDs: 27872130 22934575

Sources: DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type ovarian cancer Evidence Type Actionable Approval Status Phase I

PMIDs: 28376212 28489509 26351323 26931343

Sources: MyCancerGenome ClearityFoundationClinicalTrial JAX-CKB CIViC GuideToPharmacology TTD OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name perifosine, KRX-0401 Novel drug target Novel Target Indication/Tumor Type ovarian clear cell carcinoma

PMIDs: 25519148 18201764

Sources: TALC TdgClinicalTrial JAX-CKB MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor Specific Action of the Ligand Inhibition

PMIDs: 24735930 24978597 23795919 26429956

Sources: JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17603540

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Novel Target Trial Name RX-0201 ,Archexin combination therapy Everolimus + RX-0201

PMIDs: None found

Sources: TdgClinicalTrial JAX-CKB TTD

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Phase I Response Type no benefit

PMIDs: 20644979

Sources: ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: allosteric modulator inhibitory allosteric modulator (inhibitory) inhibitor (inhibitory)

Interaction Info: Notes combination therapy MK2206 + Vemurafenib Indication/Tumor Type melanoma

PMIDs: 25551293 24265152

Sources: TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22026410

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor Direct Interaction yes

Interaction Types & Directionality:

n/a

PMIDs:
24844664

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17980607

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20855208

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19110422

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase II

Response Type predicted – sensitive

Indication/Tumor Type triple-receptor negative breast cancer

PMIDs:
27872130 22934575

Sources:
DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type ovarian cancer

Evidence Type Actionable

Approval Status Phase I

PMIDs:
28376212 28489509 26351323 26931343

Sources:
MyCancerGenome ClearityFoundationClinicalTrial JAX-CKB CIViC GuideToPharmacology TTD OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name perifosine, KRX-0401

Novel drug target Novel Target

Indication/Tumor Type ovarian clear cell carcinoma

PMIDs:
25519148 18201764

Sources:
TALC TdgClinicalTrial JAX-CKB MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
24735930 24978597 23795919 26429956

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17603540

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name RX-0201 ,Archexin

combination therapy Everolimus + RX-0201

PMIDs:
None found

Sources:
TdgClinicalTrial JAX-CKB TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type no benefit

PMIDs:
20644979

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

allosteric modulator

inhibitory allosteric modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

combination therapy MK2206 + Vemurafenib

Indication/Tumor Type melanoma

PMIDs:
25551293 24265152

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22026410

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
20822912

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
23390247

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Novel drug target Novel Target

207	OncoKB Entrez Id
PRKBA	OncoKB Gene Synonym
RAC	OncoKB Gene Synonym

ENSG00000142208	Ensembl Gene ID
AKT	Human Protein Atlas Gene Synonym
PKB	Human Protein Atlas Gene Synonym

RAC-alpha serine/threonine-protein kinase	Gene Name
P31749	UniProt ID