Design, synthesis, and characteristics of peptide models of enzyme inhibitors
Read Online

Design, synthesis, and characteristics of peptide models of enzyme inhibitors

  • 141 Want to read
  • ·
  • 1 Currently reading

Published .
Written in English

Book details:

Edition Notes

Statementby Steven E. Shoelson.
LC ClassificationsMicrofilm 85/307 (Q)
The Physical Object
Paginationviii, 212 p.
Number of Pages212
ID Numbers
Open LibraryOL2581876M
LC Control Number85129905

Download Design, synthesis, and characteristics of peptide models of enzyme inhibitors


Peptide deformylase catalyzes the removal of the N-terminal formyl group from newly synthesized polypeptides in eubacteria. Its essential character in bacterial cells makes it an attractive target for antibacterial drug design. In this work, we have rationally designed and synthesized a series of peptide thiols that act as potent, reversible inhibitors of purified recombinant peptide Cited by: Purchase Peptide, Protein and Enzyme Design, Volume - 1st Edition. Print Book & E-Book. ISBN , Price: $ Design and Synthesis of Macrocyclic Peptidyl Hydroxamates as Peptide Deformylase Inhibitors serves as a model enzyme system for inhibitor design. While investigating the structural-functional. Despite this small hydrolytic activity, it is the first time, to our knowledge, that hydrolysis of such a substrate is reported by an enzyme model compound. Contrary, this enzyme model peptide.

The chapter focuses on a few select examples of peptide‐based inhibitors of proteases (angiotensin‐converting enzyme, HIV protease, matrix metalloproteinases, and anthrax lethal factor). Significant peptide‐based studies have been performed with transferase enzymes, namely kinases. The rational discovery of enzyme inhibitors represents a topic of intense interest in medicinal chemistry as they represent a large fraction of the orally active drugs in the current clinical use. This Special Issue will focus on the design, synthesis, and biological evaluation of enzyme inhibitors. Mechanistic insight and structural information provide the starting points for two contrasting approaches to the design of enzyme inhibitors. Phosphorus-containing peptides are inhibitors of the zinc and aspartic peptidases that mimic key geometric and electronic characteristics of the transition states of these enzymes. Enzyme Substrates and Inhibitors; Enzyme Substrates and Inhibitors. Our company has long been distributing enzyme substrates and enzyme inhibitors, with high reputation from many researchers worldwide. In addition, it is a remarkable trend to synthesize custom substrates and inhibitors specific to the newly discovered enzymes in the various.

The proven organization of the work in two parts has been maintained: you can search from enzyme to inhibitor (Part A) and from inhibitor to enzyme (Part B). Useful entries, e.g. on the type of inhibition or the effective concentration are given as well as comments on organisms and products and an extensive documentation of references. Characteristics Each peptide has its own unique structural and biochemical characteristics, such as an isoelectric pH (pI) and ionization behavior. These features are derived from the peptide’s AA components. Therefore, the overall characteristics of a peptide can change depending on the quantity and type of each AA within the chain. Enzyme inhibitors are known which block the formation of noradrenaline, as of course does noradrenaline itself. The activity of tyrosine hydroxylase is inhibited by α-methyl-p-tyrosine (Figure a), which competes for the substance is used in the treatment of phaeochromocytoma (see below).Dopa decarboxylase can be inhibited by drugs such as carbidopa (Figure b) and . Design and Synthesis of Reversible Cysteine Protease Inhibitors 53 Design of Peptidyl Aldehydes 53 Synthesis of Peptidyl Aldehydes 56 Design and Synthesis of Semicarbazones 62 Design and Synthesis of Heterocycles 64 Design and Synthesis of Peptidyl Nitriles 69 Synthesis of the Azide Analogue