PMID

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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

Cyclopeptide Smac mimetics as antagonists of IAP 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

Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein.

University of California Riverside

Monomeric Targeted Protein Degraders.

TBA

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

Discovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents.

Msa University

Carbonic anhydrase inhibitors: synthesis and inhibition studies against mammalian isoforms I-XV with a series of 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides.

Istanbul University