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mTOR

Preclinical evaluation of drug combinations identifies co-inhibition of Bcl-2/XL/W and MDM2 as a potential therapy in uveal melanoma

0 views | Jan 16 2020

Clapes V et al. showed that inhibition of Bcl-2/XL/W sensitised the UM cell lines to other treatments encouraging investigation of the underlying mechanisms. [Read the Full Post]

Adverse Drug Reactions Involving Protein Kinase Inhibitors: A French Pharmacovigilance Database Study Comparing Safety in Younger and Older Patients (≥ 75 years) with Cancer

0 views | Jan 11 2020

Clapes V et al. showed that PKI-related ADRs in older patients were similar to those in younger adults, except for vascular ADRs, which were significantly more frequent in the older population. [Read the Full Post]

AZD8055 Exerts Antitumor Effects on Colon Cancer Cells by Inhibiting mTOR and Cell-cycle Progression

7 views | Dec 26 2019

Chen Y et al. indicated that AZD8055 induces cytotoxicity, apoptosis, and cell-cycle arrest of colon cancer cells, and exerts an antitumor effect in mice. It also inhibits the mTOR signaling pathway and mTOR-dependent cell-cycle progression. [Read the Full Post]

The PI3K/mTOR dual inhibitor BEZ235 suppresses proliferation and migration and reverses multidrug resistance in acute myeloid leukemia

7 views | Dec 24 2019

Deng L et al. indicated that the PI3K/mTOR dual inhibitor BEZ235 effectively chemosensitizes AML cells via increasing miR-1-3p and subsequently down-regulating BAG4, EDN1 and ABCB1. [Read the Full Post]

NVP-BEZ235 synergizes cisplatin sensitivity in osteosarcoma

10 views | Dec 24 2019

Huang JC et al. suggested NVP-BEZ235 could synergize cisplatin sensitivity in OS, combination of NVP-BEZ235 with cisplatin could represent a novel therapeutic strategy for treatment of OS. [Read the Full Post]

Dactolisib (NVP-BEZ235) toxicity in murine brain tumour models

10 views | Dec 23 2019

Netland IA et al. suggested that despite the anti-neoplastic efficacy of dactolisib in glioma treatment in vitro, its utility in vivo is questionable due to toxicity. [Read the Full Post]

First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies

8 views | Dec 15 2019

Munster P et al. indicated although the MTD of GSK458 was 2.5 mg once daily, twice-daily dosing may increase duration of target inhibition. Fasting insulin and glucose levels served as pharmacodynamic markers of drug exposure. Select patients achieved durable responses; however,PIK3CAmutations were neither necessary nor predictive of response. Combination treatment strategies and novel biomarkers may be needed to optimally target PI3K. [Read the Full Post]

Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF

18 views | Dec 12 2019

Mercer PF et al. indicated the data define PI3K as a promising therapeutic target in IPF and provide a scientific and dosing framework for progressing GSK2126458 to clinical testing in this disease setting. A proof-of-mechanism trial of this agent is currently underway. [Read the Full Post]

PI3K inhibition reduces murine and human liver fibrogenesis in precision-cut liver slices

11 views | Dec 12 2019

Gore E et al. showed that omipalisib has antifibrotic properties in ex vivo mouse and human liver PCTS, but higher concentrations showed toxicity in jejunum PCTS. While the PI3K/mTOR pathway appears to be a promising target for the treatment of liver fibrosis, PCTS revealed likely side effects in the intestine at higher doses. [Read the Full Post]

The successful use of pembrolizumab in a renal transplant recipient with metastatic melanoma

24 views | Nov 16 2019

Hanna DL et al. reported a case in which a renal transplant recipient with metastatic melanoma had an excellent response to treatment with second line programmed cell death protein 1 (PD-1) inhibitor therapy, pembrolizumab. [Read the Full Post]