PMID

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Article Title

Organization

Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.

Bristol-Myers Squibb 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

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

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

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

Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs.

The University Of Tokyo

Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein.

University Of California Riverside

Optimization of a Series of RIPK2 PROTACs.

Glaxosmithkline

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

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

Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.

Takeda Pharmaceutical

Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.

Universita Degli Studi Di Milano

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists.

Genentech

Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.

Genentech

Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).

University Of Michigan

Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases.

Shanghai Institute Of Organic Chemistry

Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.

University Of Milano

Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.

Genentech

Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.

Princeton University

Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.

University Of Michigan

Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.

University Of Michigan

Non-peptidic small molecule inhibitors of XIAP.

Abbott Laboratories

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.

Abbott Laboratories

Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.

University Of Michigan

Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.

University Of Michigan

Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.

Burnham Institute For Medical Research