By F Javier Luque; Xavier Barril

Content material: Preface; attractiveness of ligands by means of macromolecular ambitions; thermodynamics of ligand binding; continuum solvation in biomolecular platforms; bioavailability prediction at early drug discovery levels: in vitro assays and straightforward physicochemical ideas; computational suggestions in drug layout; molecular descriptors for database mining; pharmacophore types in drug layout; docking and digital screening; binding unfastened strength calculations and scoring in small-molecule docking; COMparative BINding power (COMBINE) research as a structure-based 3D-QSAR strategy; accounting for goal flexibility in the course of ligand-receptor docking; superior sampling equipment in drug layout; exploring range of drug objective websites; increasing the objective house: druggability overview; computational ideas and demanding situations for concentrating on protein-protein interactions with small molecules; case reports; utilizing molecular simulations and metadynamics to foretell binding loose energies and kinetics; the case of COX and CDK2; Computer-assisted layout of drug-like artificial libraries; index

Show description

Read or Download Physico-chemical and computational approaches to drug discovery PDF

Best chemical books

Monosaccharide Sugars. Chemical Synthesis by Chain Elongation, Degradation, and Epimerization

''This publication offers in-depth, entire entry to an unlimited physique of literature on artificial reactions related to carbohydrates. the quantity is a mine of data both worthwhile for looking a pragmatic procedure for creating a sugar-based beginning fabric and for comprehending the impression of a managed chiral surroundings at the final result of a man-made transformation.

W Tungsten: Metal, Chemical Reactions with Metals Zinc to Lawrencium

The current quantity maintains the outline of the chemical reactions of eiemental tungsten began with "Tungsten" Suppl. Vol. A 7. It covers the reactions with the steel parts from zinc to actinoids. The remedy contains section diagrams, bulk reactions, and floor techniques which back are of remarkable value in such a lot structures.

Modelling of chemical wear : relevance to practice

Modeling of Chemical put on is a one-stop source for college students, researchers and execs looking speedy and potent tribological reviews of environmentally pleasant and effort effective items. This booklet considers optimizing additive mixtures by means of right method, bridging the space among concept and perform.

Additional info for Physico-chemical and computational approaches to drug discovery

Sample text

McCammon, J. Am. Chem. , 2004, 126, 7683. 40. W. F. van Gunsteren and A. E. Mark, Eur. J. , 1992, 204, 947. 41. C. D. Christ, A. E. Mark and W. F. van Gunsteren, J. Comput. , 2010, 31, 1569. 42. See this publication, ch. 11. 43. J. Michel and J. W. Essex, J. Comput. Aided Mol. , 2010, 24, 639. 44. J. W. Ponder, C. Wu, P. Ren, V. S. Pande, J. D. Chodera, M. J. Schnieders, I. Haque, D. L. Mobley, D. S. Lambrecht, R. A. , M. Head-Gordon, G. N. I. Clark, M. E. Johnson and T. HeadGordon, J. Phys. Chem.

89. R. A. Friesner and V. Guallar, Annu. Rev. Phys. , 2005, 56, 389. 22 Chapter 1 90. A. Lodola, C. J. Woods and A. J. Mulholland, Annu. Rep. Comput. , 2008, 4, 155. 91. A. E. Cho, V. Guallar, B. J. Berne and R. Friesner, J. Comput. , 2005, 26, 915. 92. A. E. Cho and D. Rinaldo, J. Comput. , 2009, 30, 2609. 93. C. J. R. Illingworth, G. M. Morris, K. E. B. Parkes, C. R. Snell and C. A. Reynolds, J. Phys. Chem. A, 2008, 112, 12157. 94. A. E. Cho, J. Y. Chung, M. Kim and K. Park, J. Chem. , 2009, 131, 134108.

111. I. S. Ufimtsev and T. J. Martı´nez, J. Chem. , 2009, 5, 1004. 112. I. S. Ufimtsev and T. J. Martı´nez, J. Chem. , 2009, 5, 2619. 113. N. Luehr, I. S. Ufimtsev and T. J. Martı´nez, J. Chem. , 2011, 7, 949. 114. Y. Uejima, T. Terashima and R. Maezomo, J. Comput. , 2011, 32, 2264. CHAPTER 2 Thermodynamics of Ligand Binding ¨ RGY G. FERENCZY*a AND GYO ¨ RGY M. KESERU ˝ *b GYO a Department of Inorganic and Analytical Chemistry, Budapest University of Technology and Economics, 4, Szt. 1 Introduction Ligand binding is a fundamental process in many biological phenomena.

Download PDF sample

Rated 4.93 of 5 – based on 32 votes