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Ref Type | Journal Article | ||||||||||||
PMID | (32439931) | ||||||||||||
Authors | Kostaras E, Kaserer T, Lazaro G, Heuss SF, Hussain A, Casado P, Hayes A, Yandim C, Palaskas N, Yu Y, Schwartz B, Raynaud F, Chung YL, Cutillas PR, Vivanco I | ||||||||||||
Title | A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. | ||||||||||||
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Abstract Text | AKT, a critical effector of the phosphoinositide 3-kinase (PI3K) signalling cascade, is an intensely pursued therapeutic target in oncology. Two distinct classes of AKT inhibitors have been in clinical development, ATP-competitive and allosteric. Class-specific differences in drug activity are likely the result of differential structural and conformational requirements governing efficient target binding, which ultimately determine isoform-specific potency, selectivity profiles and activity against clinically relevant AKT mutant variants.We have carried out a systematic evaluation of clinical AKT inhibitors using in vitro pharmacology, molecular profiling and biochemical assays together with structural modelling to better understand the context of drug-specific and drug-class-specific cell-killing activity.Our data demonstrate clear differences between ATP-competitive and allosteric AKT inhibitors, including differential effects on non-catalytic activity as measured by a novel functional readout. Surprisingly, we found that some mutations can cause drug resistance in an isoform-selective manner despite high structural conservation across AKT isoforms. Finally, we have derived drug-class-specific phosphoproteomic signatures and used them to identify effective drug combinations.These findings illustrate the utility of individual AKT inhibitors, both as drugs and as chemical probes, and the benefit of AKT inhibitor pharmacological diversity in providing a repertoire of context-specific therapeutic options. |
Molecular Profile | Treatment Approach |
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No data available in table |
Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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No data available in table |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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KU-57788 | KU57788|KU 57788 | DNA_PK Inhibitor 9 | KU-57788 is an inhibitor of DNA-PK, potentially inducing tumor cell death (PMID: 32439931). | |
OSU-T315 | OSUT315|OSU T315 | OSU-T315 is an ILK inhibitor potentially inhibiting Akt signaling and inducing tumor cell cytotoxicity (PMID: 32439931, PMID: 25293770). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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No data available in table |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
PIK3CA C420R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA C420R | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E542K | stomach cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and ARQ 751combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + GSK2334470 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | KU-57788 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Ipatasertib (GDC-0068) combination treatment increased cell death compared to Ipatasertib (GDC-0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | MK2206 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | decreased response | ARQ 751 + LAM-002A | Preclinical - Cell culture | Actionable | In a preclinical study, LAM-002A (Apilimod dimesylate) and ARQ 751 combination treatment resulted in less cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK2334470 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | AZD0156 + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and MK2206 combination treatment increased cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + AZD0156 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | GSK690693 + Sirolimus | Preclinical - Cell culture | Actionable | In a preclinical study, Rapamune (sirolimus) and GSK690693 combination treatment increased cell death compared to GSK690693 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | decreased response | LAM-002A + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, LAM-002A (Apilimod dimesylate) and MK2206 combination treatment resulted in less cell death compared to MK2206 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Miransertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | KU-57788 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | ARQ 751 + Torin 1 | Preclinical - Cell culture | Actionable | In a preclinical study, Torin 1 and ARQ 751 combination treatment increased cell death compared to ARQ 751 alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA E545K | breast cancer | sensitive | Ipatasertib + KU-57788 | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Ipatasertib (GDC-0068) combination treatment increased cell death compared to Ipatasertib (GDC-0068) alone in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA H1047R | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | GSK2334470 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, GSK2334470 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | Miransertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | AZD0156 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, AZD0156 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | KU-57788 + Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, KU-57788 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA K111N | breast cancer | sensitive | Ipatasertib + OSU-T315 | Preclinical - Cell culture | Actionable | In a preclinical study, OSU-T315 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | predicted - sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PIK3CA P449T | colorectal cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). | 32439931 |
PTEN L108R | breast cancer | sensitive | Miransertib | Preclinical - Cell culture | Actionable | In a preclinical study, Miransertib (ARQ092) treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). | 32439931 |
PTEN L108R | breast cancer | sensitive | Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Ipatasertib (GDC-0068) treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). | 32439931 |
PTEN L108R | breast cancer | predicted - sensitive | GSK690693 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). | 32439931 |
PTEN L108R | breast cancer | sensitive | MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). | 32439931 |
PTEN L108R | breast cancer | sensitive | ARQ 751 | Preclinical - Cell culture | Actionable | In a preclinical study, ARQ 751 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). | 32439931 |
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