Literature DB >> 24944740

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Michael F T Koehler1, Philippe Bergeron1, Edna F Choo1, Kevin Lau1, Chudi Ndubaku1, Danette Dudley1, Paul Gibbons1, Brad E Sleebs2, Carl S Rye2, George Nikolakopoulos2, Chinh Bui2, Sanji Kulasegaram2, Wilhelmus J A Kersten2, Brian J Smith2, Peter E Czabotar2, Peter M Colman2, David C S Huang2, Jonathan B Baell2, Keith G Watson2, Lisa Hasvold3, Zhi-Fu Tao3, Le Wang3, Andrew J Souers3, Steven W Elmore3, John A Flygare1, Wayne J Fairbrother1, Guillaume Lessene2.   

Abstract

Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin's lymphoma (NHL), interest in additional selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-XL antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallography were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds.

Entities:  

Keywords:  BCL-2; BCL-XL; apoptosis; cancer

Year:  2014        PMID： 24944740      PMCID： PMC4060937          DOI： 10.1021/ml500030p

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  18 in total

Review 1.  Bcl-2 family proteins as therapeutic targets.

Authors:  Peter E Czabotar; Guillaume Lessene
Journal:  Curr Pharm Des       Date:  2010       Impact factor: 3.116

2.  Bcl-2 family proteins are essential for platelet survival.

Authors:  H Zhang; P M Nimmer; S K Tahir; J Chen; R M Fryer; K R Hahn; L A Iciek; S J Morgan; M C Nasarre; R Nelson; L C Preusser; G A Reinhart; M L Smith; S H Rosenberg; S W Elmore; C Tse
Journal:  Cell Death Differ       Date:  2007-01-05       Impact factor: 15.828

3.  Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

Authors:  Milan Bruncko; Thorsten K Oost; Barbara A Belli; Hong Ding; Mary K Joseph; Aaron Kunzer; Darlene Martineau; William J McClellan; Michael Mitten; Shi-Chung Ng; Paul M Nimmer; Tilman Oltersdorf; Cheol-Min Park; Andrew M Petros; Alexander R Shoemaker; Xiaohong Song; Xilu Wang; Michael D Wendt; Haichao Zhang; Stephen W Fesik; Saul H Rosenberg; Steven W Elmore
Journal:  J Med Chem       Date:  2007-01-26       Impact factor: 7.446

Review 4.  BCL-2 family antagonists for cancer therapy.

Authors:  Guillaume Lessene; Peter E Czabotar; Peter M Colman
Journal:  Nat Rev Drug Discov       Date:  2008-12       Impact factor: 84.694

5.  Mcl-1 deficiency results in peri-implantation embryonic lethality.

Authors:  J L Rinkenberger; S Horning; B Klocke; K Roth; S J Korsmeyer
Journal:  Genes Dev       Date:  2000-01-01       Impact factor: 11.361

6.  ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.

Authors:  Andrew J Souers; Joel D Leverson; Erwin R Boghaert; Scott L Ackler; Nathaniel D Catron; Jun Chen; Brian D Dayton; Hong Ding; Sari H Enschede; Wayne J Fairbrother; David C S Huang; Sarah G Hymowitz; Sha Jin; Seong Lin Khaw; Peter J Kovar; Lloyd T Lam; Jackie Lee; Heather L Maecker; Kennan C Marsh; Kylie D Mason; Michael J Mitten; Paul M Nimmer; Anatol Oleksijew; Chang H Park; Cheol-Min Park; Darren C Phillips; Andrew W Roberts; Deepak Sampath; John F Seymour; Morey L Smith; Gerard M Sullivan; Stephen K Tahir; Chris Tse; Michael D Wendt; Yu Xiao; John C Xue; Haichao Zhang; Rod A Humerickhouse; Saul H Rosenberg; Steven W Elmore
Journal:  Nat Med       Date:  2013-01-06       Impact factor: 53.440

Review 7.  Targeting the extrinsic apoptosis signaling pathway for cancer therapy.

Authors:  Thomas J Sayers
Journal:  Cancer Immunol Immunother       Date:  2011-04-06       Impact factor: 6.968

8.  Testicular degeneration in Bclw-deficient mice.

Authors:  A J Ross; K G Waymire; J E Moss; A F Parlow; M K Skinner; L D Russell; G R MacGregor
Journal:  Nat Genet       Date:  1998-03       Impact factor: 38.330

9.  Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer.

Authors:  Charles M Rudin; Christine L Hann; Edward B Garon; Moacyr Ribeiro de Oliveira; Philip D Bonomi; D Ross Camidge; Quincy Chu; Giuseppe Giaccone; Divis Khaira; Suresh S Ramalingam; Malcolm R Ranson; Caroline Dive; Evelyn M McKeegan; Brenda J Chyla; Barry L Dowell; Arunava Chakravartty; Cathy E Nolan; Niki Rudersdorf; Todd A Busman; Mack H Mabry; Andrew P Krivoshik; Rod A Humerickhouse; Geoffrey I Shapiro; Leena Gandhi
Journal:  Clin Cancer Res       Date:  2012-04-11       Impact factor: 12.531

10.  Structure-guided design of a selective BCL-X(L) inhibitor.

Authors:  Guillaume Lessene; Peter E Czabotar; Brad E Sleebs; Kerry Zobel; Kym N Lowes; Jerry M Adams; Jonathan B Baell; Peter M Colman; Kurt Deshayes; Wayne J Fairbrother; John A Flygare; Paul Gibbons; Wilhelmus J A Kersten; Sanji Kulasegaram; Rebecca M Moss; John P Parisot; Brian J Smith; Ian P Street; Hong Yang; David C S Huang; Keith G Watson
Journal:  Nat Chem Biol       Date:  2013-04-21       Impact factor: 15.040
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  16 in total

1.  Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Authors:  Zhi-Fu Tao; Lisa Hasvold; Le Wang; Xilu Wang; Andrew M Petros; Chang H Park; Erwin R Boghaert; Nathaniel D Catron; Jun Chen; Peter M Colman; Peter E Czabotar; Kurt Deshayes; Wayne J Fairbrother; John A Flygare; Sarah G Hymowitz; Sha Jin; Russell A Judge; Michael F T Koehler; Peter J Kovar; Guillaume Lessene; Michael J Mitten; Chudi O Ndubaku; Paul Nimmer; Hans E Purkey; Anatol Oleksijew; Darren C Phillips; Brad E Sleebs; Brian J Smith; Morey L Smith; Stephen K Tahir; Keith G Watson; Yu Xiao; John Xue; Haichao Zhang; Kerry Zobel; Saul H Rosenberg; Chris Tse; Joel D Leverson; Steven W Elmore; Andrew J Souers
Journal:  ACS Med Chem Lett       Date:  2014-08-26       Impact factor: 4.345

2.  Screening-based translation of public research encounters painful problems.

Authors:  Jonathan B Baell
Journal:  ACS Med Chem Lett       Date:  2015-02-09       Impact factor: 4.345

Review 3.  Small-molecule inhibitors of protein-protein interactions: progressing toward the reality.

Authors:  Michelle R Arkin; Yinyan Tang; James A Wells
Journal:  Chem Biol       Date:  2014-09-18

Review 4.  From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors.

Authors:  Avi Ashkenazi; Wayne J Fairbrother; Joel D Leverson; Andrew J Souers
Journal:  Nat Rev Drug Discov       Date:  2017-02-17       Impact factor: 84.694

Review 5.  The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs.

Authors:  Sarah T Diepstraten; Mary Ann Anderson; Peter E Czabotar; Guillaume Lessene; Andreas Strasser; Gemma L Kelly
Journal:  Nat Rev Cancer       Date:  2021-10-18       Impact factor: 60.716

Review 6.  What can we learn from mice lacking pro-survival BCL-2 proteins to advance BH3 mimetic drugs for cancer therapy?

Authors:  Kerstin Brinkmann; Ashley P Ng; Carolyn A de Graaf; Andreas Strasser
Journal:  Cell Death Differ       Date:  2022-04-06       Impact factor: 12.067

Review 7.  Targeting apoptosis in cancer therapy.

Authors:  Benedito A Carneiro; Wafik S El-Deiry
Journal:  Nat Rev Clin Oncol       Date:  2020-03-23       Impact factor: 66.675

8.  Apoptotic Ablation of Platelets Reduces Atherosclerosis in Mice With Diabetes.

Authors:  Man K S Lee; Michael J Kraakman; Dragana Dragoljevic; Nordin M J Hanssen; Michelle C Flynn; Annas Al-Sharea; Gopalkrishna Sreejit; Camilla Bertuzzo-Veiga; Olivia D Cooney; Fatima Baig; Elizabeth Morriss; Mark E Cooper; Emma C Josefsson; Benjamin T Kile; Prabhakara R Nagareddy; Andrew J Murphy
Journal:  Arterioscler Thromb Vasc Biol       Date:  2021-01-14       Impact factor: 8.311

Review 9.  Intrinsically Connected: Therapeutically Targeting the Cathepsin Proteases and the Bcl-2 Family of Protein Substrates as Co-regulators of Apoptosis.

Authors:  Surinder M Soond; Maria V Kozhevnikova; Lyudmila V Savvateeva; Paul A Townsend; Andrey A Zamyatnin
Journal:  Int J Mol Sci       Date:  2021-04-28       Impact factor: 5.923

10.  Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor.

Authors:  Zhi-Fu Tao; Xilu Wang; Jun Chen; Justin P Ingram; Sha Jin; Russell A Judge; Peter J Kovar; Chang Park; Chaohong Sun; Brian D Wakefield; Li Zhou; Haichao Zhang; Steven W Elmore; Darren C Phillips; Andrew S Judd; Joel D Leverson; Andrew J Souers
Journal:  ACS Med Chem Lett       Date:  2021-05-12       Impact factor: 4.632
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