ipatasertib






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1 18755143 Ryanodine receptor phosphorylation at Serine 2030, 2808 and 2814 in rat cardiomyocytes. Biochem Biophys Res Commun 2008 Nov 7 2
2 22487381 PKA phosphorylation of cardiac ryanodine receptor modulates SR luminal Ca2+ sensitivity. J Mol Cell Cardiol 2012 Jul 4
3 22934575 Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem 2012 Sep 27 2
4 23287563 Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res 2013 Apr 1 13
5 24141624 Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068. Clin Cancer Res 2013 Dec 15 4
6 24705351 Inhibition of Akt reverses the acquired resistance to sorafenib by switching protective autophagy to autophagic cell death in hepatocellular carcinoma. Mol Cancer Ther 2014 Jun 2
7 26617788 Long noncoding RNA AK056155 involved in the development of Loeys-Dietz syndrome through AKT/PI3K signaling pathway. Int J Clin Exp Pathol 2015 2
8 27081168 Differential Receptor Tyrosine Kinase PET Imaging for Therapeutic Guidance. J Nucl Med 2016 Sep 2
9 27797456 Microsecond molecular dynamics simulations provide insight into the ATP-competitive inhibitor-induced allosteric protection of Akt kinase phosphorylation. Chem Biol Drug Des 2017 May 9
10 27872130 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 2017 Jan 9
11 28065668 Ablation of the cardiac ryanodine receptor phospho-site Ser2808 does not alter the adrenergic response or the progression to heart failure in mice. Elimination of the genetic background as critical variable. J Mol Cell Cardiol 2017 Feb 1
12 28473255 Inhibition of Akt and other AGC kinases: A target for clinical cancer therapy? Semin Cancer Biol 2018 Feb 1
13 29100327 Phosphatidylinositol 3-kinase (PI3Kα)/AKT axis blockade with taselisib or ipatasertib enhances the efficacy of anti-microtubule drugs in human breast cancer cells. Oncotarget 2017 Sep 29 3
14 29408595 STX3 represses the stability of the tumor suppressor PTEN to activate the PI3K-Akt-mTOR signaling and promotes the growth of breast cancer cells. Biochim Biophys Acta Mol Basis Dis 2018 May 2
15 29417298 Targeting the PI3K/AKT/mTOR pathway in triple-negative breast cancer: a review. Breast Cancer Res Treat 2018 Jun 1
16 30037818 Randomized Phase II Study Evaluating Akt Blockade with Ipatasertib, in Combination with Abiraterone, in Patients with Metastatic Prostate Cancer with and without PTEN Loss. Clin Cancer Res 2019 Feb 1 1
17 30185800 Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis 2018 Sep 5 7
18 30385525 Correction: 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 2018 Nov 2
19 30877085 Patient-Driven Discovery, Therapeutic Targeting, and Post-Clinical Validation of a Novel <i>AKT1</i> Fusion-Driven Cancer. Cancer Discov 2019 May 3
20 31147675 FAIRLANE, a double-blind placebo-controlled randomized phase II trial of neoadjuvant ipatasertib plus paclitaxel for early triple-negative breast cancer. Ann Oncol 2019 Aug 1 5
21 31173106 Targeting the PI3K/Akt/mTOR pathway with the pan-Akt inhibitor GDC-0068 in PIK3CA-mutant breast cancer brain metastases. Neuro Oncol 2019 Nov 4 14
22 31316618 FGFR<sup>3S249C</sup> mutation promotes chemoresistance by activating Akt signaling in bladder cancer cells. Exp Ther Med 2019 Aug 1
23 31558316 Ipatasertib sensitizes colon cancer cells to TRAIL-induced apoptosis through ROS-mediated caspase activation. Biochem Biophys Res Commun 2019 Nov 19 9
24 31619255 Inhaled gold nanoparticles cause cerebral edema and upregulate endothelial aquaporin 1 expression, involving caveolin 1 dependent repression of extracellular regulated protein kinase activity. Part Fibre Toxicol 2019 Oct 16 3
25 31663655 PTEN promotes intervertebral disc degeneration by regulating nucleus pulposus cell behaviors. Cell Biol Int 2020 Feb 3
26 31859249 Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol 2020 Jan 16 5
27 32205017 Antitumor activity of ipatasertib combined with chemotherapy: results from a phase Ib study in solid tumors. Ann Oncol 2020 May 1
28 32294525 Akt-targeted therapy as a promising strategy to overcome drug resistance in breast cancer - A comprehensive review from chemotherapy to immunotherapy. Pharmacol Res 2020 Jun 2
29 32451180 Activating AKT1 and PIK3CA Mutations in Metastatic Castration-Resistant Prostate Cancer. Eur Urol 2020 Dec 3
30 32530390 Combined inhibition of ACK1 and AKT shows potential toward targeted therapy against KRAS-mutant non-small-cell lung cancer. Bosn J Basic Med Sci 2021 Apr 1 1
31 32737717 A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Invest New Drugs 2021 Feb 1
32 33040459 EBP2, a novel NPM-ALK-interacting protein in the nucleolus, contributes to the proliferation of ALCL cells by regulating tumor suppressor p53. Mol Oncol 2021 Jan 3
33 33177006 Durable Clinical Activity to the AKT Inhibitor Ipatasertib in a Heavily Pretreated Patient With an AKT1 E17K Mutant Metastatic Breast Cancer. Clin Breast Cancer 2021 Jun 1
34 33230431 miR-301a-PTEN-AKT Signaling Induces Cardiomyocyte Proliferation and Promotes Cardiac Repair Post-MI. Mol Ther Nucleic Acids 2020 Dec 4 2
35 33373654 A Rho kinase inhibitor (Fasudil) suppresses TGF-β mediated autophagy in urethra fibroblasts to attenuate traumatic urethral stricture (TUS) through re-activating Akt/mTOR pathway: An in vitro study. Life Sci 2021 Feb 15 3
36 33648537 Recombinant CCL17-dependent CCR4 activation alleviates neuroinflammation and neuronal apoptosis through the PI3K/AKT/Foxo1 signaling pathway after ICH in mice. J Neuroinflammation 2021 Mar 1 1
37 33989112 Protein kinase inhibitors for the treatment of prostate cancer. Expert Opin Pharmacother 2021 Oct 2
38 34049965 Evaluation of Ipatasertib Interactions with Itraconazole and Coproporphyrin I and III in a Single Drug Interaction Study in Healthy Subjects. J Pharmacol Exp Ther 2021 Aug 8
39 34066055 Akt Kinase Intervenes in Flavivirus Replication by Interacting with Viral Protein NS5. Viruses 2021 May 12 1
40 34066144 Enhanced Antitumor Effect of Trastuzumab and Duligotuzumab or Ipatasertib Combination in HER-2 Positive Gastric Cancer Cells. Cancers (Basel) 2021 May 12 3
41 34264439 Final results of the double-blind placebo-controlled randomized phase 2 LOTUS trial of first-line ipatasertib plus paclitaxel for inoperable locally advanced/metastatic triple-negative breast cancer. Breast Cancer Res Treat 2021 Sep 2
42 34359829 ER+ Breast Cancer Strongly Depends on MCL-1 and BCL-xL Anti-Apoptotic Proteins. Cells 2021 Jul 2 1
43 34471960 Single- and multiple-dose pharmacokinetics, potential for CYP3A inhibition, and food effect in patients with cancer and healthy subjects receiving ipatasertib. Cancer Chemother Pharmacol 2021 Dec 2
44 34907082 Functional Mapping of AKT Signaling and Biomarkers of Response from the FAIRLANE Trial of Neoadjuvant Ipatasertib plus Paclitaxel for Triple-Negative Breast Cancer. Clin Cancer Res 2022 Mar 1 5
45 35306249 Ipatasertib (GDC-0068) and erdafitinib co-treatment for inducing mitochondrial apoptosis through Bim upregulation in bladder cancer cells. Biochem Biophys Res Commun 2022 May 14 1
46 35428895 Assessment of cytochrome P450 3A4-mediated drug-drug interactions for ipatasertib using a fit-for-purpose physiologically based pharmacokinetic model. Cancer Chemother Pharmacol 2022 May 5
47 35440108 Distinct resistance mechanisms arise to allosteric vs. ATP-competitive AKT inhibitors. Nat Commun 2022 Apr 19 1
48 35603567 Identification of novel natural inhibitors targeting AKT Serine/Threonine Kinase 1 (AKT1) by computational study. Bioengineered 2022 May 1