Literature DB >> 29140691

Importance of Rigidity in Designing Small Molecule Drugs To Tackle Protein-Protein Interactions (PPIs) through Stabilization of Desired Conformers.

Alastair D G Lawson1, Malcolm MacCoss2, Jag P Heer1.   

Abstract

Tackling PPIs, particularly by stabilizing clinically favored conformations of target proteins, with orally available, bona fide small molecules remains a significant but immensely worthwhile challenge for the pharmaceutical industry. Success may be more likely through the application of nature's learnings to build intrinsic rigidity into the design of clinical candidates.

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Year:  2017        PMID： 29140691     DOI： 10.1021/acs.jmedchem.7b01120

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


  14 in total

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Authors:  Laurence Leherte; Axel Petit; Denis Jacquemin; Daniel P Vercauteren; Adèle D Laurent
Journal:  J Comput Aided Mol Des       Date:  2018-10-28       Impact factor: 3.686

Review 2.  Applications of Norrish type I and II reactions in the total synthesis of natural products: a review.

Authors:  Sasadhar Majhi
Journal:  Photochem Photobiol Sci       Date:  2021-09-18       Impact factor: 3.982

Review 3.  Teaching an old dog new tricks: Drug discovery by repositioning natural products and their derivatives.

Authors:  Boshi Huang; Yan Zhang
Journal:  Drug Discov Today       Date:  2022-02-16       Impact factor: 8.369

4.  Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment.

Authors:  Camilo E Quevedo; Abimael Cruz-Migoni; Nicolas Bery; Ami Miller; Tomoyuki Tanaka; Donna Petch; Carole J R Bataille; Lydia Y W Lee; Phillip S Fallon; Hanna Tulmin; Matthias T Ehebauer; Narcis Fernandez-Fuentes; Angela J Russell; Stephen B Carr; Simon E V Phillips; Terence H Rabbitts
Journal:  Nat Commun       Date:  2018-08-09       Impact factor: 14.919

5.  Synthesis, Identification, and Structure-Activity Relationship Analysis of GATA4 and NKX2-5 Protein-Protein Interaction Modulators.

Authors:  Mikael Jumppanen; Sini M Kinnunen; Mika J Välimäki; Virpi Talman; Samuli Auno; Tanja Bruun; Gustav Boije Af Gennäs; Henri Xhaard; Ingo B Aumüller; Heikki Ruskoaho; Jari Yli-Kauhaluoma
Journal:  J Med Chem       Date:  2019-09-03       Impact factor: 7.446

Review 6.  Natural products in drug discovery: advances and opportunities.

Authors:  Atanas G Atanasov; Sergey B Zotchev; Verena M Dirsch; Claudiu T Supuran
Journal:  Nat Rev Drug Discov       Date:  2021-01-28       Impact factor: 112.288

Review 7.  Mechanisms of ligand binding.

Authors:  Enrico Di Cera
Journal:  Biophys Rev       Date:  2020-12

8.  Structure-based development of new RAS-effector inhibitors from a combination of active and inactive RAS-binding compounds.

Authors:  Abimael Cruz-Migoni; Peter Canning; Camilo E Quevedo; Carole J R Bataille; Nicolas Bery; Ami Miller; Angela J Russell; Simon E V Phillips; Stephen B Carr; Terence H Rabbitts
Journal:  Proc Natl Acad Sci U S A       Date:  2019-01-25       Impact factor: 11.205

9.  Exploring anticancer activity of structurally modified benzylphenoxyacetamide (BPA); I: Synthesis strategies and computational analyses of substituted BPA variants with high anti-glioblastoma potential.

Authors:  Joanna Stalinska; Lisa Houser; Monika Rak; Susan B Colley; Krzysztof Reiss; Branko S Jursic
Journal:  Sci Rep       Date:  2019-11-19       Impact factor: 4.379

10.  Design, Synthesis and Characterization of HIV-1 CA-Targeting Small Molecules: Conformational Restriction of PF74.

Authors:  Rajkumar Lalji Sahani; Raquel Diana-Rivero; Sanjeev Kumar V Vernekar; Lei Wang; Haijuan Du; Huanchun Zhang; Andres Emanuelli Castaner; Mary C Casey; Karen A Kirby; Philip R Tedbury; Jiashu Xie; Stefan G Sarafianos; Zhengqiang Wang
Journal:  Viruses       Date:  2021-03-15       Impact factor: 5.048
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