Literature DB >> 24315455

Hitting a moving target: targeting transient protein states.

Matthias R Bauer1, Frank M Boeckler.   

Abstract

In this issue of Structure, Bista and colleagues report that inhibitors of the MDM2/p53 interaction can be designed to interact with a transiently folded α-helical segment of the MDM2 lid region. This suggests that targeting transient protein states in PPI inhibitor design could be a promising strategy to improve affinity and/or selectivity profiles.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 24315455     DOI: 10.1016/j.str.2013.11.003

Source DB:  PubMed          Journal:  Structure        ISSN: 0969-2126            Impact factor:   5.006


  5 in total

1.  Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.

Authors:  Constantinos G Neochoritis; Jack Atmaj; Aleksandra Twarda-Clapa; Ewa Surmiak; Lukasz Skalniak; Lisa-Maria Köhler; Damian Muszak; Katarzyna Kurpiewska; Justyna Kalinowska-Tłuścik; Barbara Beck; Tad A Holak; Alexander Dömling
Journal:  Eur J Med Chem       Date:  2019-08-06       Impact factor: 6.514

2.  Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists.

Authors:  S Shaabani; C G Neochoritis; A Twarda-Clapa; B Musielak; T A Holak; A Dömling
Journal:  Medchemcomm       Date:  2017-03-15       Impact factor: 3.597

Review 3.  How To Design a Successful p53-MDM2/X Interaction Inhibitor: A Thorough Overview Based on Crystal Structures.

Authors:  Natalia Estrada-Ortiz; Constantinos G Neochoritis; Alexander Dömling
Journal:  ChemMedChem       Date:  2015-12-16       Impact factor: 3.466

4.  2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists.

Authors:  Constantinos G Neochoritis; Kan Wang; Natalia Estrada-Ortiz; Eberhardt Herdtweck; Katarzyna Kubica; Aleksandra Twarda; Krzysztof M Zak; Tad A Holak; Alexander Dömling
Journal:  Bioorg Med Chem Lett       Date:  2015-12-15       Impact factor: 2.823

5.  Artificial Macrocycles as Potent p53-MDM2 Inhibitors.

Authors:  Natalia Estrada-Ortiz; Constantinos G Neochoritis; Aleksandra Twarda-Clapa; Bogdan Musielak; Tad A Holak; Alexander Dömling
Journal:  ACS Med Chem Lett       Date:  2017-09-20       Impact factor: 4.345

  5 in total

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