Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). - Wikidata - wikimedia - TriplyDB

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).

http://www.wikidata.org/entity/Q35543223

about

Mitochondria, cholesterol and cancer cell metabolism Modulation of Protein-Protein Interactions for the Development of Novel Therapeutics Regulation of Bim in Health and Disease The BCL2 Family: Key Mediators of the Apoptotic Response to Targeted Anticancer Therapeutics Mito-priming as a method to engineer Bcl-2 addiction.Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods Mitochondrial apoptosis and BH3 mimetics Inhibition of MARCH5 ubiquitin ligase abrogates MCL1-dependent resistance to BH3 mimetics via NOXA Chemical parsing: Dissecting cell dependencies with a toolkit of selective BCL-2 family inhibitors The emergence of acid ceramidase as a therapeutic target for acute myeloid leukemia.Acid ceramidase is upregulated in AML and represents a novel therapeutic target.Epstein-Barr virus ensures B cell survival by uniquely modulating apoptosis at early and late times after infection Targeting MCL-1 sensitizes human esophageal squamous cell carcinoma cells to cisplatin-induced apoptosis Small-Molecule and Peptide Inhibitors of the Pro-Survival Protein Mcl-1 Allosteric inhibition of antiapoptotic MCL-1.Constitutive BAK activation as a determinant of drug sensitivity in malignant lymphohematopoietic cells.Diffuse Large B Cell Lymphoma Cell Line U-2946: Model for MCL1 Inhibitor Testing.BCL-2 Antagonism to Target the Intrinsic Mitochondrial Pathway of Apoptosis.Synergistic drug combinations for cancer identified in a CRISPR screen for pairwise genetic interactions Loss in MCL-1 function sensitizes non-Hodgkin's lymphoma cell lines to the BCL-2-selective inhibitor venetoclax (ABT-199)Potential mechanisms of resistance to venetoclax and strategies to circumvent it.Attacking cancer's Achilles heel: antagonism of anti-apoptotic BCL-2 family members Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.Deubiquitylating enzyme USP9x regulates radiosensitivity in glioblastoma cells by Mcl-1-dependent and -independent mechanisms.Critical B-lymphoid cell intrinsic role of endogenous MCL-1 in c-MYC-induced lymphomagenesis.Structural Re-engineering of the α-Helix Mimetic JY-1-106 into Small Molecules: Disruption of the Mcl-1-Bak-BH3 Protein-Protein Interaction with 2,6-Di-Substituted Nicotinates Targeting MCL-1/BCL-XL Forestalls the Acquisition of Resistance to ABT-199 in Acute Myeloid Leukemia.Defining specificity and on-target activity of BH3-mimetics using engineered B-ALL cell lines.Effect of cobalt(II) chloride hexahydrate on some human cancer cell lines FGFR1 inhibition in lung squamous cell carcinoma: questions and controversies.High-Resolution Mapping of RNA Polymerases Identifies Mechanisms of Sensitivity and Resistance to BET Inhibitors in t(8;21) AML.MCL-1 is required throughout B-cell development and its loss sensitizes specific B-cell subsets to inhibition of BCL-2 or BCL-XL.Computationally designed high specificity inhibitors delineate the roles of BCL2 family proteins in cancer.MCL-1 inhibition provides a new way to suppress breast cancer metastasis and increase sensitivity to dasatinib.Killing Two Cells with One Stone: Pharmacologic BCL-2 Family Targeting for Cancer Cell Death and Immune Modulation.Bcl-2 protein family expression pattern determines synergistic pro-apoptotic effects of BH3 mimetics with hemisynthetic cardiac glycoside UNBS1450 in acute myeloid leukemia.Emerging understanding of Bcl-2 biology: Implications for neoplastic progression and treatment.New dimension in therapeutic targeting of BCL-2 family proteins.Targeting BCL-2 to enhance vulnerability to therapy in estrogen receptor-positive breast cancer.

P2860

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P2860

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).

http://www.wikidata.org/entity/Q35543223

description

2015 nî lūn-bûn

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2015 թուականի Յունուարին հրատարակուած գիտական յօդուած

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2015 թվականի հունվարին հրատարակված գիտական հոդված

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2015年の論文

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Cell Death and Disease

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A J Souers

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A Tanaka

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C Tse

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C Wong

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D C Phillips

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D J Anderson

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D Sampath

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G S Sheppard

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H Zhang

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I Wertz

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P2860

Mcl-1 is critical for survival in a subgroup of non-small-cell lung cancer cell lines

Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia

Chemical genomics identifies small-molecule MCL1 repressors and BCL-xL as a predictor of MCL1 dependency

Mitochondria primed by death signals determine cellular addiction to antiapoptotic BCL-2 family members

BH3 profiling--measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions

Structural insights into the degradation of Mcl-1 induced by BH3 domains

A novel BH3 ligand that selectively targets Mcl-1 reveals that apoptosis can proceed without Mcl-1 degradation

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

Rational Design of Proteolytically Stable, Cell-Permeable Peptide-Based Selective Mcl-1 Inhibitors

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

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e1590

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10.1038/CDDIS.2014.561

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6

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2015-01-15T00:00:00Z

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