Stabilization of protein–protein interactions by small molecules

•Protein–protein interactions (PPIs) are ever increasingly targets for drug discovery.•Targeted small molecule inhibition of PPIs has repeatedly been shown to be successful.•Targeted small molecule stabilization of PPIs is however an underexplored concept.•We review the current status of small molec...

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Published in:Drug discovery today Vol. 19; no. 11; pp. 1812 - 1821
Main Authors: Giordanetto, Fabrizio, Schäfer, Anja, Ottmann, Christian
Format: Journal Article
Language:English
Published: England Elsevier Ltd 01.11.2014
Subjects:
Drug Discovery
Humans
Pharmaceutical Preparations - metabolism
Protein Stability - drug effects
Proteins - metabolism
ISSN:1359-6446, 1878-5832, 1878-5832
Online Access:Get full text
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Abstract •Protein–protein interactions (PPIs) are ever increasingly targets for drug discovery.•Targeted small molecule inhibition of PPIs has repeatedly been shown to be successful.•Targeted small molecule stabilization of PPIs is however an underexplored concept.•We review the current status of small molecule PPI stabilization as a fruitful concept. Protein–protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.
AbstractList •Protein–protein interactions (PPIs) are ever increasingly targets for drug discovery.•Targeted small molecule inhibition of PPIs has repeatedly been shown to be successful.•Targeted small molecule stabilization of PPIs is however an underexplored concept.•We review the current status of small molecule PPI stabilization as a fruitful concept. Protein–protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.
Protein-protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.Protein-protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.
Protein-protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.
Author Ottmann, Christian
Giordanetto, Fabrizio
Schäfer, Anja
Author_xml – sequence: 1
  givenname: Fabrizio
  surname: Giordanetto
  fullname: Giordanetto, Fabrizio
  organization: Medicinal Chemistry, Taros Chemicals, Emil-Figge-Str. 76a, 44227 Dortmund, Germany
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  givenname: Anja
  surname: Schäfer
  fullname: Schäfer, Anja
  organization: Laboratory of Chemical Biology and Institute of Complex Molecular Systems, Department of Biomedical Engineering, Technische Universiteit Eindhoven, Den Dolech 2, 5612 AZ Eindhoven, The Netherlands
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  givenname: Christian
  surname: Ottmann
  fullname: Ottmann, Christian
  email: c.ottmann@tue.nl
  organization: Laboratory of Chemical Biology and Institute of Complex Molecular Systems, Department of Biomedical Engineering, Technische Universiteit Eindhoven, Den Dolech 2, 5612 AZ Eindhoven, The Netherlands
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Snippet •Protein–protein interactions (PPIs) are ever increasingly targets for drug discovery.•Targeted small molecule inhibition of PPIs has repeatedly been shown to...
Protein-protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge...
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SubjectTerms Drug Discovery
Humans
Pharmaceutical Preparations - metabolism
Protein Stability - drug effects
Proteins - metabolism
Title Stabilization of protein–protein interactions by small molecules
URI https://dx.doi.org/10.1016/j.drudis.2014.08.005
https://www.ncbi.nlm.nih.gov/pubmed/25173701
https://www.proquest.com/docview/1652427592
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