Literature DB >> 25695766

The discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity.

Benjamin A Seigal1, William H Connors1, Andrew Fraley1, Robert M Borzilleri, Percy H Carter, Stuart L Emanuel, Joseph Fargnoli, Kyoung Kim, Ming Lei, Joseph G Naglich, Matthew E Pokross, Shana L Posy, Henry Shen, Neha Surti, Randy Talbott, Yong Zhang, Nicholas K Terrett1.   

Abstract

Affinity selection screening of macrocycle libraries derived from DNA-programmed chemistry identified XIAP BIR2 and BIR3 domain inhibitors that displace bound pro-apoptotic caspases. X-ray cocrystal structures of key compounds with XIAP BIR2 suggested potency-enhancing structural modifications. Optimization of dimeric macrocycles with similar affinity for both domains were potent pro-apoptotic agents in cancer cell lines and efficacious in shrinking tumors in a mouse xenograft model.

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Year:  2015        PMID： 25695766     DOI： 10.1021/jm501892g

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  22 in total

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

Authors:  Yong Zhang; Benjamin A Seigal; Nicholas K Terrett; Randy L Talbott; Joseph Fargnoli; Joseph G Naglich; Charu Chaudhry; Shana L Posy; Ragini Vuppugalla; Georgia Cornelius; Ming Lei; Chunlei Wang; Yingru Zhang; Robert J Schmidt; Donna D Wei; Michael M Miller; Martin P Allen; Ling Li; Percy H Carter; Gregory D Vite; Robert M Borzilleri
Journal:  ACS Med Chem Lett       Date:  2015-05-27       Impact factor: 4.345

2.  Development of a Platform To Enable Efficient Permeability Evaluation of Novel Organo-Peptide Macrocycles.

Authors:  Brett A Hopkins; Hyelee Lee; Sookhee Ha; Lisa Nogle; Berengere Sauvagnat; Spencer McMinn; Graham F Smith; Nunzio Sciammetta
Journal:  ACS Med Chem Lett       Date:  2019-05-09       Impact factor: 4.345

Review 3.  DNA-encoded chemistry: enabling the deeper sampling of chemical space.

Authors:  Robert A Goodnow; Christoph E Dumelin; Anthony D Keefe
Journal:  Nat Rev Drug Discov       Date:  2016-12-09       Impact factor: 84.694

4.  Kinetically guided radical-based synthesis of C(sp3)-C(sp3) linkages on DNA.

Authors:  Jie Wang; Helena Lundberg; Shota Asai; Pedro Martín-Acosta; Jason S Chen; Stephen Brown; William Farrell; Russell G Dushin; Christopher J O'Donnell; Anokha S Ratnayake; Paul Richardson; Zhiqing Liu; Tian Qin; Donna G Blackmond; Phil S Baran
Journal:  Proc Natl Acad Sci U S A       Date:  2018-06-26       Impact factor: 11.205

Review 5.  Macrocycles as protein-protein interaction inhibitors.

Authors:  Patrick G Dougherty; Ziqing Qian; Dehua Pei
Journal:  Biochem J       Date:  2017-03-15       Impact factor: 3.857

Review 6.  Chronic hepatitis B: A wave of new therapies on the horizon.

Authors:  Timothy M Block; Siddhartha Rawat; Carol L Brosgart
Journal:  Antiviral Res       Date:  2015-06-22       Impact factor: 5.970

7.  New Frontiers in Druggability.

Authors:  Dima Kozakov; David R Hall; Raeanne L Napoleon; Christine Yueh; Adrian Whitty; Sandor Vajda
Journal:  J Med Chem       Date:  2015-08-11       Impact factor: 7.446

8.  Azidoethoxyphenylalanine as a Vibrational Reporter and Click Chemistry Partner in Proteins.

Authors:  Elise M Tookmanian; Christine M Phillips-Piro; Edward E Fenlon; Scott H Brewer
Journal:  Chemistry       Date:  2015-11-26       Impact factor: 5.236

Review 9.  DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information.

Authors:  Dario Neri; Richard A Lerner
Journal:  Annu Rev Biochem       Date:  2018-01-12       Impact factor: 23.643

10.  Automated screening for small organic ligands using DNA-encoded chemical libraries.

Authors:  Willy Decurtins; Moreno Wichert; Raphael M Franzini; Fabian Buller; Michael A Stravs; Yixin Zhang; Dario Neri; Jörg Scheuermann
Journal:  Nat Protoc       Date:  2016-03-17       Impact factor: 13.491
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