By Wolfgang Jahnke, Daniel A. Erlanson (Editors), Raimund Mannhold, Hugo Kubinyi, Gerd Folkers (Series
This primary systematic precis of the effect of fragment-based techniques at the drug improvement approach offers crucial info that used to be formerly unavailable. Adopting a practice-oriented procedure, this represents a publication by means of execs for pros, tailored for drug builders within the pharma and biotech zone who have to retain updated at the most modern applied sciences and techniques in pharmaceutical ligand layout. The ebook is obviously divided into 3 sections on ligand layout, spectroscopic suggestions, and screening and drug discovery, sponsored through various case reports.
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Extra resources for Fragment-based Approaches in Drug Discovery (Methods and Principles in Medicinal Chemistry)
USA 96, 9997–10002. J. 1997, Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23, 3–25. , Oprea, T. 1999, The design of leadlike combinatorial libraries. Angew. Chem. Int. Ed. Engl. 38, 3743–3748. P. 1981, On the attribution and additivity of binding energies. Proc. Natl Acad. Sci. USA 78, 4046–4050. H. 1985, Mode of interaction of beta-hydroxy-betamethylglutaryl coenzyme A reductase with strong binding inhibitors: compactin and related compounds.
5 Conformational Entropy of the Linker between Ligands We [1, 53] and others [17, 32, 38, 40, 46] suggested that the linker for the oligovalent ligand should be rigid in order to minimize the loss in conformational entropy [TDSoconf in Eqs. (3), (4)] that occurs upon binding the receptor (Fig. 7). The intuitive argument is that flexible linkers have more entropy to lose (more accessible conformational states) upon association than rigid ones, and thus should be avoided to achieve tight binding.
Oprea and Blaney outline the concepts of chemical space, lead-likeness, and fragment-like leads, using both de novo calculations and data mining in Chapter 5. This chapter illustrates the difficulty in trying to sample even a relatively small section of “fragment space”, and provides a number of specific examples to direct researchers toward the most fruitful regions. In Chapter 6, Vieth and Siegel “dissect” existing drugs into their component fragments and demonstrate that there are considerable differences between oral and injectable drugs.