Literature DB >> 17631247

Water, water everywhere--except where it matters?

Steve W Homans1.   

Abstract

Biological processes depend on specific recognition between molecules with carefully tuned affinities. Because of the complexity of the problem, binding affinities cannot reliably be computed from molecular structures. Modern biophysical techniques can decompose the problem to determine the thermodynamic contributions from protein, cognate ligand and solvent. Such studies applied to a model protein with a hydrophobic binding pocket have resulted in some surprising findings. For example, binding is not driven by the favourable entropic loss of solvent water from the binding pocket, but rather by favourable dispersion interactions arising from suboptimal hydration of the protein-binding pocket. Under these circumstances, one can anticipate particularly dramatic gains in binding affinity using shape complementarity to optimise solute-solute dispersion interactions, since these will not be offset by opposing solute-solvent dispersion interactions.

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Year:  2007        PMID: 17631247     DOI: 10.1016/j.drudis.2007.05.004

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  36 in total

1.  Long-timescale molecular-dynamics simulations of the major urinary protein provide atomistic interpretations of the unusual thermodynamics of ligand binding.

Authors:  Julie Roy; Charles A Laughton
Journal:  Biophys J       Date:  2010-07-07       Impact factor: 4.033

2.  Ligand binding to protein-binding pockets with wet and dry regions.

Authors:  Lingle Wang; B J Berne; R A Friesner
Journal:  Proc Natl Acad Sci U S A       Date:  2011-01-04       Impact factor: 11.205

Review 3.  Functional aspects of protein flexibility.

Authors:  Kaare Teilum; Johan G Olsen; Birthe B Kragelund
Journal:  Cell Mol Life Sci       Date:  2009-03-24       Impact factor: 9.261

4.  Protein-ligand interactions: probing the energetics of a putative cation-π interaction.

Authors:  James M Myslinski; John H Clements; Stephen F Martin
Journal:  Bioorg Med Chem Lett       Date:  2014-05-09       Impact factor: 2.823

5.  Mechanism of the hydrophobic effect in the biomolecular recognition of arylsulfonamides by carbonic anhydrase.

Authors:  Phillip W Snyder; Jasmin Mecinovic; Demetri T Moustakas; Samuel W Thomas; Michael Harder; Eric T Mack; Matthew R Lockett; Annie Héroux; Woody Sherman; George M Whitesides
Journal:  Proc Natl Acad Sci U S A       Date:  2011-10-19       Impact factor: 11.205

Review 6.  Applying thermodynamic profiling in lead finding and optimization.

Authors:  Gerhard Klebe
Journal:  Nat Rev Drug Discov       Date:  2015-01-23       Impact factor: 84.694

7.  Natural Products and Their Mimics as Targets of Opportunity for Discovery.

Authors:  Stephen F Martin
Journal:  J Org Chem       Date:  2017-09-15       Impact factor: 4.354

Review 8.  Perspectives on NMR in drug discovery: a technique comes of age.

Authors:  Maurizio Pellecchia; Ivano Bertini; David Cowburn; Claudio Dalvit; Ernest Giralt; Wolfgang Jahnke; Thomas L James; Steve W Homans; Horst Kessler; Claudio Luchinat; Bernd Meyer; Hartmut Oschkinat; Jeff Peng; Harald Schwalbe; Gregg Siegal
Journal:  Nat Rev Drug Discov       Date:  2008-09       Impact factor: 84.694

Review 9.  A medicinal chemist's guide to molecular interactions.

Authors:  Caterina Bissantz; Bernd Kuhn; Martin Stahl
Journal:  J Med Chem       Date:  2010-07-22       Impact factor: 7.446

10.  Water in cavity-ligand recognition.

Authors:  Riccardo Baron; Piotr Setny; J Andrew McCammon
Journal:  J Am Chem Soc       Date:  2010-09-01       Impact factor: 15.419

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