AKT1
ENSG00000142208
Target class
Kinase
Chromosome
14
Approved drugs
1
Clinical candidates (approved and in development)
16
- Approved drugs
- 1
- ClinGen gene-disease validity
- Limited
- Clinical candidates (approved and in development)
- 16
- Chemical probe available
- Yes
- Target name
- AKT1
- Gene name
- AKT serine/threonine kinase 1
- Gene symbol
- AKT1
- Protein name
- RAC-alpha serine/threonine-protein kinase (EC 2.7.11.1) (Protein kinase B) (PKB) (Protein kinase B alpha) (PKB alpha) (Proto-oncogene c-Akt) (RAC-PK-alpha)
- RAC
- PKB
- PRKBA
- AKT
- RAC-alpha
- Gene biotype
- Protein coding
- Gene family
- Pleckstrin homology domain containing|AKT kinase family
- Target class
- Kinase
- Target type
- Human gene
- Tissues expressed in
- 54
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 88.76
- Tissue specificity (Gini)
- 0.24
- Tissue specificity (tau)
- 0.458
- KEGG gene identifiers
- hsa:207
- Protein interaction confidence
- 0.845678
- Protein interaction partners
- 428
- R-HSA-111447
- R-HSA-1257604
- R-HSA-1358803
- R-HSA-1445148
- R-HSA-1474151
- R-HSA-165159
- R-HSA-165181
- R-HSA-198323
- R-HSA-198693
- R-HSA-199418
- R-HSA-203615
- R-HSA-211163
- R-HSA-354192
- R-HSA-3769402
- R-HSA-389357
- R-HSA-389513
- R-HSA-392451
- R-HSA-450385
- R-HSA-450604
- R-HSA-5218920
- R-HSA-5628897
- R-HSA-5674400
- R-HSA-6785807
- R-HSA-6804757
- R-HSA-6804758
And 18 more, listed on the interactive page.
- End position
- 104799934
- Start position
- 104769348
- Chromosome
- 14
- Strand
- Reverse
- Cytoplasm . Nucleus . Cell membrane . Mitochondrion intermembrane space . Note=Nucleus after activation by integrin-linked protein kinase 1 (ILK1). Nuclear translocation is enhanced by interaction with TCL1A. Phosphorylation on Tyr-176 by TNK2 results in its localization to the cell membrane where it is targeted for further phosphorylations on Thr-308 and Ser-473 leading to its activation and the activated form translocates to the nucleus. Colocalizes with WDFY2 in intracellular vesicles (PubMed:16792529). Also localizes to mitochondrial intermembrane space in response to rapamycin treatment (By similarity). .
- Calyx
- End piece
- Nucleoplasm
- Perinuclear theca
- Principal piece
- PubMed 20333297
- PubMed 40285646
- PubMed 16792529
- Tissue specificity (tau)
- 0.457981
- Expression inequality (Gini)
- 0.240246
Expression in transcripts per million
- Artery - Aorta
- 88.76
- Esophagus - Muscularis
- 83.67
- Artery - Tibial
- 82.26
- Cells - Cultured fibroblasts
- 80.84
- Lung
- 80.3
Expression in transcripts per million
- Artery - Aorta88.76
- Esophagus - Muscularis83.67
- Artery - Tibial82.26
- Cells - Cultured fibroblasts80.84
- Lung80.3
- Colon - Sigmoid75.06
- Adrenal Gland73.61
- Esophagus - Gastroesophageal Junction73.34
- Prostate71.55
- Cervix - Endocervix71.12
- Cervix - Ectocervix70.89
- Uterus70.77
- Artery - Coronary69.56
- Thyroid68.03
- Fallopian Tube66.79
- Nerve - Tibial66.19
- Adipose - Subcutaneous61.14
- Spleen60.9
- Bladder59.26
- Breast - Mammary Tissue58.73
- Cells - EBV-transformed lymphocytes56.2
- Vagina55.25
- Adipose - Visceral (Omentum)54.4
- Ovary53.73
- Minor Salivary Gland51.64
And 29 more, listed on the interactive page.
- GO:0001649
- GO:0001938
- GO:0002042
- GO:0002430
- GO:0003376
- GO:0005979
- GO:0006468
- GO:0006809
- GO:0006924
- GO:0007165
- GO:0007173
- GO:0007186
- GO:0008283
- GO:0008286
- GO:0009408
- GO:0010507
- GO:0010595
- GO:0010628
- GO:0010748
- GO:0010907
- GO:0018105
- GO:0018107
- GO:0019221
- GO:0030154
- GO:0030307
And 55 more, listed on the interactive page.
- GO:0005634
- GO:0005654
- GO:0005737
- GO:0005829
- GO:0005886
- GO:0016020
- GO:0031982
- GO:0032991
- GO:0004672
- GO:0004674
- GO:0004712
- GO:0005515
- GO:0005516
- GO:0005524
- GO:0005547
- GO:0016301
- GO:0019900
- GO:0030235
- GO:0030291
- GO:0042802
- GO:0042803
- GO:0043325
- GO:0071889
- GO:0099104
- GO:0106310
- GO:1904841
heart disease
Studies
- preclinical: Highly important for the heart and vasculature based on findings in genetically modified or kinase-inhibitor-treated mice. Role of kinase in heart/vasculature: Regulator of cardiomyocyte survival, growth and metabolism
Biological samples
- cardiovascular system
PubMed 21283106apoptototic cell death in cancer cells
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: apoptototic cell death in cancer cells
Biological samples
- cardiovascular system
Evidence sourcehyperglycemia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: hyperglycemia
Biological samples
- cardiovascular system
Evidence source
regulation of catalytic activity
- biochemical: NVS_ENZ_hAKT1, is one of one assay component(s) measured or calculated from the NVS_ENZ_hAKT1 assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
- biochemical: NVS_ENZ_hAKT1, is one of one assay component(s) measured or calculated from the NVS_ENZ_hAKT1 assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
Biological samples
- cell-free
Evidence source
Related records
Trials (211)
- A Combination Therapy Study of MK-2206 and AZD6244 in Participants With Advanced Solid Tumors (MK-2206-010)
- A Multi-centre Study to Assess the Safety, Tolerability, and Pharmacokinetics of Capivasertib (AZD5363) in Combination With Novel Agents in Patients With Metastatic Prostate Cancer
- A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer
- A Phase I Study of MK-2206 in Combination With Standard Chemotherapy in Participants With Locally Advanced or Metastatic Solid Tumors (MK-2206-003)
- A Phase I Study to Investigate the Pharmacokinetics and Safety of Capivasertib in Participants With Moderate Hepatic Impairment
- A Phase I, Open-Label, First-Time-In-Human Study of the Oral AKT Inhibitor GSK2141795
- A Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site
- A Phase II Study of Akt Inhibitor MK2206 in the Treatment of Recurrent Platinum-Resistant Ovarian, Fallopian Tube, or Peritoneal Cancer
- A Phase IIIB Study to Evaluate the Use of Capivasertib in Combination With Fulvestrant in Patients With Advanced Breast Cancer Who Have Relapsed/Progressed on ET and CDK4/6 Inhibitor Reflecting Real World Clinical Practice in Spain
- A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study
- A Single-Arm Phase II Study of Neoadjuvant Intensified Androgen Deprivation (Leuprolide and Abiraterone Acetate) in Combination With AKT Inhibition (Capivasertib) for High-Risk Localized Prostate Cancer With PTEN Loss
- A Study Assessing the Safety and Efficacy of Adding Ipatasertib to Paclitaxel Treatment in Participants With Breast Cancer That Has Spread Beyond the Initial Site, and the Cancer Does Not Have Certain Hormonal Receptors
- A Study Conducted in Subjects With Relapsed/Refractory Multiple Myeloma (MM); to Determine Dose of Afuresertib in Combination With Carfilzomib (Part 1) and to Investigate the Safety, Pharmacokinetic and Clinical Activity of the Combination Compared With Carfilzomib Alone (Part 2)
- A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response
- A Study Evaluating the Effect of Formulation on the Bioavailability of Ipatasertib in Healthy Volunteers
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer
- A Study Evaluating the Safety and Tolerability of GDC-0068 in Patients With Refractory Solid Tumors
- A Study Evaluating The Safety, Efficacy and Pharmacokinetics Of Ipatasertib In Combination With Atezolizumab And Docetaxel In Metastatic Castration-Resistant Prostate Cancer (mCRPC).
Drugs (16)
- Afuresertib Serine/threonine-protein kinase AKT inhibitor
- BAY-1125976 Serine/threonine-protein kinase AKT inhibitor
- Capivasertib Serine/threonine-protein kinase AKT inhibitor
- GSK-690693 Serine/threonine-protein kinase AKT inhibitor
- Ipatasertib Serine/threonine-protein kinase AKT inhibitor
- LY-2780301 Serine/threonine-protein kinase AKT inhibitor
- Miransertib Serine/threonine-protein kinase AKT inhibitor
- MK-2201 Serine/threonine-protein kinase AKT inhibitor
- MK-2206 Serine/threonine-protein kinase AKT inhibitor
- Pifusertib Serine/threonine-protein kinase AKT negative allosteric modulator
- Rupitasertib Serine/threonine-protein kinase AKT inhibitor
- SR-13668 Serine/threonine-protein kinase AKT inhibitor
- TAS0612 Serine/threonine-protein kinase AKT inhibitor
- Triciribine phosphate Serine/threonine-protein kinase AKT inhibitor
- Uprosertib Serine/threonine-protein kinase AKT inhibitor
- XL-418 Serine/threonine-protein kinase AKT inhibitor