96 articles for thisTarget
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Article Title
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Modulation of the Inhibitors of Apoptosis Proteins (IAPs) Activities for Cancer Treatment.
Therachem Research Medilab (India)
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.
Bristol-Myers Squibb Research
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
Astex Pharmaceuticals
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 tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists.
Bristol-Myers Squibb Research & Development
Structure-based design and synthesis of tricyclic IAP (Inhibitors of Apoptosis Proteins) inhibitors.
Astrazeneca
Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells.
Takeda Pharmaceutical
Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.
Hoffmann-La Roche
Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.
Hoffmann-La Roche
Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists.
Takeda Pharmaceutical
Solid phase synthesis of Smac/DIABLO-derived peptides using a 'Safety-Catch' resin: identification of potent XIAP BIR3 antagonists.
Queen'S University of Belfast
Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
Sanford-Burnham Medical Research Institute
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
University of Michigan
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic.
Takeda Pharmaceutical
Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
Fondazione Irccs Istituto Nazionale Dei Tumori
Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
University of Michigan
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
University of Michigan
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
Genentech
Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
University of Pittsburgh
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
University of Michigan Comprehensive Cancer Center
Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
Cisi
Discovery of aminopiperidine-based Smac mimetics as IAP antagonists.
Astrazeneca R&D Boston
DNA-instructed acyl transfer reactions for the synthesis of bioactive peptides.
Humboldt Universit£T Zu Berlin
Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
Sanford-Burnham Medical Research Institute
Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
University of Michigan
In silico discovery of acylated flavonol monorhamnosides from Eriobotrya japonica as natural, small-molecular weight inhibitors of XIAP BIR3.
University of Innsbruck
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
University of Michigan
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Genentech
Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.
Institute For Medical Research
Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
Chinese Academy of Sciences
Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein.
University of California Riverside
Design, synthesis and biological evaluation of new bivalent quinazoline analogues as IAP antagonists.
Chung-Ang University
Dual action Smac mimetics-zinc chelators as pro-apoptotic antitumoral agents.
Istituto Di Scienze E Tecnologie Molecolari (Istm)
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
TBA
Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
Ningxia Medical University
Clinical candidates modulating protein-protein interactions: The fragment-based experience.
Taros Chemicals
Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).
Astrazeneca
Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
TBA
Exploration of carboxy pyrazole derivatives: Synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile.
Quaid-I-Azam University
Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
University of California Riverside
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Csir-National Chemical Laboratory
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one
Astex Pharmaceuticals
Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.
Takeda Pharmaceutical
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Astex Pharmaceuticals
Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84.
University of Bonn
Discovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents.
Msa University
Development of novel pyrazolone derivatives as inhibitors of aldose reductase: an eco-friendly one-pot synthesis, experimental screening and in silico analysis.
Swami Ramanand Teerth Marathwada University
5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.
National Institute On Drug Abuse
Cellular inhibition of protein tyrosine phosphatase 1B by uncharged thioxothiazolidinone derivatives.
Mcgill University
Characterization of high affinity [3H]pirenzepine and (-)-[3H] quinuclidinyl benzilate binding to muscarinic cholinergic receptors in rabbit peripheral lung.
University of Arizona
Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative.
Wyeth Laboratories
The binding of L-[3H]nicotine to a single class of high affinity sites in rat brain membranes.
R. J. Reynolds Tobacco
Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers.
Organon International
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.
Nagoya Institute of Technology
Chiral Recognition Thermodynamics of β-Cyclodextrin: The Thermodynamic Origin of Enantioselectivity and the Enthalpy-Entropy Compensation Effect
Japan Science and Technology Agency
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
Purdue University
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Astrazeneca
Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.
Virginia Commonwealth University