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Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-x(L) binding to Bim

Academic Article
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Overview

related to degree

  • Simmons, Nicholas, Ph.D. in Chemistry, Scripps Research 2009 - 2015

authors

  • Cheng, C.
  • Liu, Y.
  • Balasis, M. E.
  • Simmons, Nicholas
  • Li, J.
  • Song, H.
  • Pan, L.
  • Qin, Y.
  • Nicolaou, K.C.
  • Sebti, S. M.
  • Li, R. S.

publication date

  • March 2014

journal

  • Marine Drugs  Journal

abstract

  • A series of novel cyclic marinopyrroles were designed and synthesized. Their activity to disrupt the binding of the pro-apoptotic protein, Bim, to the pro-survival proteins, Mcl-1 and Bcl-x(L), was evaluated using ELISA assays. Both atropisomers of marinopyrrole A (1) show similar potency. A tetrabromo congener 9 is two-fold more potent than 1. Two novel cyclic marinopyrroles (3 and 4) are two- to seven-fold more potent than 1.

subject areas

  • Apoptosis
  • Apoptosis Regulatory Proteins
  • Blotting, Western
  • Breast Neoplasms
  • Catalysis
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Humans
  • Indicators and Reagents
  • Isomerism
  • Magnetic Resonance Spectroscopy
  • Marine Toxins
  • Membrane Proteins
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Protein Binding
  • Proto-Oncogene Proteins
  • Pyrroles
  • Spectrophotometry, Ultraviolet
  • Structure-Activity Relationship
  • bcl-X Protein
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Research

keywords

  • SAR
  • apoptosis
  • cyclic marinopyrroles
  • protein-protein interaction disruptors
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Identity

PubMed Central ID

  • PMC3967213

International Standard Serial Number (ISSN)

  • 1660-3397

Digital Object Identifier (DOI)

  • 10.3390/md12031335

PubMed ID

  • 24608970
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Additional Document Info

start page

  • 1335

end page

  • 1348

volume

  • 12

issue

  • 3

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