Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin

Dutta, Sansa ; Basak, Amit ; Dasgupta, Swagata (2009) Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin Bioorganic & Medicinal Chemistry, 17 (11). pp. 3900-3908. ISSN 0968-0896

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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S09680...

Related URL: http://dx.doi.org/10.1016/j.bmc.2009.04.019

Abstract

Novel enediyne-amino acid conjugates 1-4 have been synthesized. All of these effectively target the enzyme chymotrypsin inhibiting its proteolytic activity. The conjugate with a directly linked phenyl alanine is the most effective inhibitor with a Ki of 3 μM. The mode of inhibition is mostly competitive or of a mixed type depending on the nature of the inhibitor.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Enediyne; Amino Acid; Trypsin; Proteolytic; Inhibitor; Competitive
ID Code:1748
Deposited On:05 Oct 2010 11:14
Last Modified:12 Jan 2011 12:05

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