73 articles for thisTarget
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Article Title
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Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Shandong University
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
Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.
Second Military Medical University
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
Astrazeneca
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Vanderbilt University School Of Medicine
Peptide-based inhibitors of protein-protein interactions.
Wroclaw University Of Technology
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 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
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.
Universit£
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Shandong University
A combination of in silico and SAR studies to identify binding hot spots of Bcl-xL inhibitors.
Bioprojet-Biotech
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
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.
Eutropics Pharmaceuticals
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
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Novartis Institutes For Biomedical Research
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
3D-QSAR pharmacophore modeling and in silico screening of new Bcl-xl inhibitors.
Universit£
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
Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
Unbiased binding assays for discovering small-molecule probes and drugs.
Broad Institute Of Harvard And Mit
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
Discovery, characterization, and structure-activity relationships studies of proapoptotic polyphenols targeting B-cell lymphocyte/leukemia-2 proteins.
Institute
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
Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL.
University Of Washington
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
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
Anti-tumor pyrimidinylpiperazines bind to the prosurvival Bcl-2 protein family member Bcl-XL.
University Of The Pacific
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
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Abbott Laboratories
Rearranged diterpenoids from the biotransformation of ent-trachyloban-18-oic acid by Rhizopus arrhizus.
Centre De Recherche De Gif
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy Of Sciences
Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention.
Institute For Medical Research
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
Institute Of Chemical And Engineering Sciences
Cytotoxic pentacyclic triterpenoids from Combretum sundaicum and Lantana camara as inhibitors of Bcl-xL/BakBH3 domain peptide interaction.
Cnrs
A Dimeric sesquiterpenoid from a Malaysian Meiogyne as a new inhibitor of Bcl-xL/BakBH3 domain peptide interaction.
Cnrs
Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl.
Merlion Pharmaceuticals
Diversity-oriented synthesis of a cytisine-inspired pyridone library leading to the discovery of novel inhibitors of Bcl-2.
Infinity Pharmaceuticals
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.
University Of Montpellier
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
University Of Minnesota
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
Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein.
Yale University
Cytotoxicity and topoisomerase I/II inhibition activity of novel 4-aryl/alkyl-1-(piperidin-4-yl)-carbonylthiosemicarbazides and 4-benzoylthiosemicarbazides.
Medical University
Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.
UniversitÀ
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Merck Research Laboratories
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Smithkline Beecham Pharmaceuticals