Literature DB >> 26019371

Tailored fragments of roseophilin selectively antagonize Mcl-1 in vitro.

Jack D Bracken1, Andrew D Carlson1, James H Frederich1, Mai Nguyen2, Gordon C Shore2, Patrick G Harran1.   

Abstract

We have discovered a fragment of the natural product roseophilin, a member of the prodiginine family, that antagonizes Mcl-1 functions in a liposome-based assay for mitochondrial membrane permeabilization. By tailoring this substance such that it can participate in salt bridging with the protein surface, we have prepared the first prodiginine inspired structure that shows direct, saturable binding to a recombinant Bcl-2 family member in vitro.

Entities:  

Keywords:  Bcl-2; Mcl-1; Obatoclax; Roseophilin; Tetrazole

Year:  2015        PMID： 26019371      PMCID： PMC4442084          DOI： 10.1016/j.tetlet.2015.01.191

Source DB:  PubMed          Journal:  Tetrahedron Lett        ISSN： 0040-4039            Impact factor:   2.415


  21 in total

1.  Studies on DNA cleavage by cytotoxic pyrrole alkaloids reveal the distinctly different behavior of roseophilin and prodigiosin derivatives.

Authors:  A Fürstner; E J Grabowski
Journal:  Chembiochem       Date:  2001-09-03       Impact factor: 3.164

Review 2.  BH3-only proteins in apoptosis at a glance.

Authors:  Lina Happo; Andreas Strasser; Suzanne Cory
Journal:  J Cell Sci       Date:  2012-03-01       Impact factor: 5.285

3.  Synthetic prodiginine obatoclax (GX15-070) and related analogues: anion binding, transmembrane transport, and cytotoxicity properties.

Authors:  Borja Díaz de Greñu; Paulina Iglesias Hernández; Margarita Espona; David Quiñonero; Mark E Light; Tomás Torroba; Ricardo Pérez-Tomás; Roberto Quesada
Journal:  Chemistry       Date:  2011-11-09       Impact factor: 5.236

4.  Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.

Authors:  Mai Nguyen; Richard C Marcellus; Anne Roulston; Mark Watson; Lucile Serfass; S R Murthy Madiraju; Daniel Goulet; Jean Viallet; Laurent Bélec; Xavier Billot; Stephane Acoca; Enrico Purisima; Adrian Wiegmans; Leonie Cluse; Ricky W Johnstone; Pierre Beauparlant; Gordon C Shore
Journal:  Proc Natl Acad Sci U S A       Date:  2007-11-26       Impact factor: 11.205

5.  Small-molecule activation of the TRAIL receptor DR5 in human cancer cells.

Authors:  Gelin Wang; Xiaoming Wang; Hong Yu; Shuguang Wei; Noelle Williams; Daniel L Holmes; Randal Halfmann; Jacinth Naidoo; Lai Wang; Lin Li; She Chen; Patrick Harran; Xiaoguang Lei; Xiaodong Wang
Journal:  Nat Chem Biol       Date:  2012-12-23       Impact factor: 15.040

6.  Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosis.

Authors:  Sean L Petersen; Lai Wang; Asligul Yalcin-Chin; Lin Li; Michael Peyton; John Minna; Patrick Harran; Xiaodong Wang
Journal:  Cancer Cell       Date:  2007-11       Impact factor: 31.743

7.  Modular access to complex prodiginines: total synthesis of (+)-roseophilin via its 2-azafulvene prototropisomer.

Authors:  James H Frederich; Patrick G Harran
Journal:  J Am Chem Soc       Date:  2013-03-01       Impact factor: 15.419

8.  A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death.

Authors:  Lin Li; Ranny Mathew Thomas; Hidetaka Suzuki; Jef K De Brabander; Xiaodong Wang; Patrick G Harran
Journal:  Science       Date:  2004-09-03       Impact factor: 47.728

9.  A phase I study of the pan bcl-2 family inhibitor obatoclax mesylate in patients with advanced hematologic malignancies.

Authors:  Aaron D Schimmer; Susan O'Brien; Hagop Kantarjian; Joseph Brandwein; Bruce D Cheson; Mark D Minden; Karen Yee; Farhad Ravandi; Francis Giles; Andre Schuh; Vikas Gupta; Michael Andreeff; Charles Koller; Hong Chang; Suzanne Kamel-Reid; Mark Berger; Jean Viallet; Gautam Borthakur
Journal:  Clin Cancer Res       Date:  2008-12-15       Impact factor: 12.531

10.  The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer.

Authors:  Michelle L Stewart; Emiko Fire; Amy E Keating; Loren D Walensky
Journal:  Nat Chem Biol       Date:  2010-06-20       Impact factor: 15.040
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  3 in total

Review 1.  Inverse Electron Demand Diels-Alder Reactions of Heterocyclic Azadienes, 1-Aza-1,3-Butadienes, Cyclopropenone Ketals, and Related Systems. A Retrospective.

Authors:  Jiajun Zhang; Vyom Shukla; Dale L Boger
Journal:  J Org Chem       Date:  2019-05-23       Impact factor: 4.354

Review 2.  Recent Advances in Bacteria-Based Cancer Treatment.

Authors:  Xianyuan Wei; Meng Du; Zhiyi Chen; Zhen Yuan
Journal:  Cancers (Basel)       Date:  2022-10-09       Impact factor: 6.575

3.  Obatoclax is a direct and potent antagonist of membrane-restricted Mcl-1 and is synthetic lethal with treatment that induces Bim.

Authors:  Mai Nguyen; Regina Cencic; Franziska Ertel; Cynthia Bernier; Jerry Pelletier; Anne Roulston; John R Silvius; Gordon C Shore
Journal:  BMC Cancer       Date:  2015-08-01       Impact factor: 4.430
  3 in total

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