By Ben M. Dunn
This booklet makes a speciality of peptides as medicinal drugs, a growing to be sector of pharmaceutical examine and improvement. It is helping readers clear up difficulties of learning, constructing, generating, and offering peptide-based medicines. * Identifies promising new parts in peptide drug discovery * comprises chapters on discovery from typical resources, metabolic amendment, and drug supply * Overviews separation tools and strategies for research, bond formation, and purification * bargains readers either a qualified reference and a textual content or source for graduate-level scholars
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Extra resources for Peptide Chemistry and Drug Design
Sample text
Lacosamide from Schwarz, which selectively enhances slow inactivation of voltage-gated sodium channels and binds to collapsin response mediator protein 2, is a protected O-methylserine [3]. Even more important than the number of peptides accepted by the FDA is the number of peptides that are in clinical phases. In 2008, 39 were in clinical phase I, 77 in phase II, 39 in phase III, and 4 in preregistration [4]. There are several reasons for this renaissance of peptides. The first one is the fact that the number of classical small molecules is not increasing enormously.
2). 1. PS resins. PS is the most widely used solid support for the synthesis of peptides in solid phase because of its good swelling properties and good level of substitution [6, 7]. 2 ∗ Peptide (b) 2 PS NH2 O ( O )n O NH2 NH2 O ( O )n O NH2 NH2 O ( O )n O NH2 (c) 3 (a) PS supports; (b) PEG-PS supports; and (c) totally PEG based supports. libraries can be prepared on paper membranes as in the SPOT technology [300]. 14 METHODS FOR THE PEPTIDE SYNTHESIS AND ANALYSIS and divinylbenzene. PS swells well in nonpolar solvents such as toluene or CH2 Cl2 , but can be used in combination with other more polar solvents such as N,N-dimethylformamide (DMF), dioxane, and tetrahydrofuran.
The advantage of the Nps-group, except for the cleavage with acids [176], is that it can be selectively removed by nucleophilic reagents [177, 178]. These reagents avoid the problems encountered with protecting groups requiring acids for their cleavage. 12) [179]. 2 Carboxy-Group Protection of the C-terminal Amino-acid Derivative or Fragment The carboxylic group of the C-terminal amino acid or fragment is commonly masked as an alkyl or aryl ester. Alternatively, the C-terminal protecting group can be hydrazides or protected hydrazides.