37 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
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
The discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity.
Ensemble Therapeutics
Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.
Bristol-Myers Squibb 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
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
University of Michigan
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
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
Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
University of Michigan
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
University of Michigan
Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
Chinese Academy of Sciences
Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.
University of Michigan
Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
The University of Tokyo
Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist.
University of California
E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology.
Astrazeneca
Cyclic tailor-made amino acids in the design of modern pharmaceuticals.
Nanjing Forestry University
Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein.
University of California Riverside
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
Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
University of California Riverside
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
4-Connected azabicyclo[5.3.0]decane Smac mimetics-Zn
Istituto Di Scienze E Tecnologie Molecolari (Istm)
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
Structural analysis of human KDM5B guides histone demethylase inhibitor development.
University of Oxford
Mild and efficient synthesis of new tetraketones as lipoxygenase inhibitors and antioxidants.
Pharmaceutical Research Centre
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.
Vrije Universiteit