Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 3, Pages 1331-1336Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.026
Keywords
Dengue NS2B-NS3 protease
Funding
- National University of Singapore [R-143-000-308-112]
- Singapore Toteboard Model Project [11-27801-36-M100, M100]
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Kalata B1 is a plant protein with remarkable thermal, chemical and enzymatic stability. Its potential applications could be centered on the possibility of using its cyclic structure and cystine knot motif as a scaffold for the design of stable pharmaceuticals. To discover potent dengue NS2B-NS3 protease inhibitors, we have prepared various kalata B1 analogues by varying the amino acid sequence. Mass spectrometric and biochemical investigations of these analogues revealed a cyclopeptide whose two fully oxidized forms are substrate-competitive inhibitors of the dengue viral NS2B-NS3 protease. Both oxidized forms showed potent inhibition with Ki of 1.39 +/- 0.35 and 3.03 +/- 0.75 mu M, respectively. (C) 2009 Elsevier Ltd. All rights reserved.
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