Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin.
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 K(i) of 3 microM. The mode of inhibition is mostly competitive or of a mixed type depending on the nature of the inhibitor.
Department of Chemistry, Indian Institute of Technology, Kharagpur 721 302, India.
Sansa
S
Dutta
Amit
A
Basak
Swagata
S
Dasgupta
D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D003500:Cyclization; D015195:Drug Design; D053281:Enediynes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D015394:Molecular Structure; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013379:Substrate Specificity
D053281:Enediynes; D004791:Enzyme Inhibitors; D010455:Peptides; D002918:Chymotrypsin