100 articles for thisTarget
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Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Shandong University
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.
Wuhan University School Of Pharmaceutical Sciences
Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
China Pharmaceutical University
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.
University Of Kansas
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Vanderbilt University School Of Medicine
Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.
University Of Maryland
Inhibitors of the Antiapoptotic Myeloid Cell Leukemia-1 (Mcl-1) May Provide Effective Treatment for Cancer.
Therachem Research Medilab (India)
Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors.
Shandong University
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
Shandong University
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Novartis Institutes For Biomedical Research
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.
Vanderbilt University School Of Medicine
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Abbvie
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Shandong University
Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors.
University Of Nebraska
Biased and unbiased strategies to identify biologically active small molecules.
Institut De Chimie Des Substances Naturelles
Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1).
Institute
A simple and widely applicable hit validation strategy for protein-protein interaction inhibitors based on a quantitative ligand displacement assay.
Takeda Pharmaceutical
Endiandric acid analogues from Beilschmiedia ferruginea as dual inhibitors of Bcl-xL/Bak and Mcl-1/Bid interactions.
Institut De Chimie Des Substances Naturelles (Icsn)
3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
University Of Michigan Medical School
Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein.
Research & Development, Abbvie
Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins.
Takeda Pharmaceutical
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.
Eutropics Pharmaceuticals
Design and application of a rigid quinazolone scaffold based on two-face Bima-helix mimicking.
Dalian University Of Technology
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
The Walter And Eliza Hall Institute Of Medical Research
Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach.
Dalian University Of Technology
Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors.
Dalian University Of Technology
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
Vanderbilt University School Of Medicine
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.
Dalian University Of Technology
An anthraquinone scaffold for putative, two-face Bim BH3a-helix mimic.
Dalian University Of Technology
Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.
Clermont Universit£
Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.
University Of Michigan
Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.
University Of Michigan
Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction.
Universit£
BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues.
University Of Minnesota
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Mcgill University
Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity.
Second Military Medical University
SAR by interligand nuclear overhauser effects (ILOEs) based discovery of acylsulfonamide compounds active against Bcl-x(L) and Mcl-1.
Sanford-Burnham Medical Research Institute
Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design.
Dalian University Of Technology
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
The Walter And Eliza Hall Institute Of Medical Research
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.
Dalian University Of Technology
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University Of Thessaloniki
Cryptosphaerolide, a cytotoxic Mcl-1 inhibitor from a marine-derived ascomycete related to the genus Cryptosphaeria.
University Of California San Diego
Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii.
Florida Atlantic University
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
Institute Of Chemical And Engineering Sciences
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
University Of Michigan
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
University Of Michigan
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University Of Michigan
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
Universit£
From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).
University Of Calgary
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Vanderbilt University School Of Medicine
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Servier Research Institute Of Medicinal Chemistry
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an ?-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
TBA
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.
Eberhard Karls University T£Bingen
Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
National Institute Of Chemistry
Indole: A privileged scaffold for the design of anti-cancer agents.
Hunan University Of Science And Technology
Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.
Astrazeneca
Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.
TBA
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like ?-Helical Mimetics.
Dalian University Of Technology
Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.
Shandong University
Lipophilic Isosteres of a ?-? Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction.
Novartis Institutes For Biomedical Research
NMR strategy for unraveling structures of bioactive sponge-derived oxy-polyhalogenated diphenyl ethers.
University Of California
Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors.
Shandong University
Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
University Of Maryland
1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation.
Shandong University
Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.
Vanderbilt University
X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential.
Rheinische Friedrich-Wilhelms-Universit£T
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Vanderbilt University School Of Medicine
Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
Shenyang Pharmaceutical University
Design, Synthesis, and Experimental Validation of Peptide Ligands Targeting Mycobacterium tuberculosis s Factors.
Indian Institute Of Science