Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmc.2009.12.026
Title: Synthesis and disulfide bond connectivity-activity studies of a kalata B1-inspired cyclopeptide against dengue NS2B-NS3 protease
Authors: Gao, Y.
Cui, T.
Lam, Y. 
Keywords: Dengue NS2B-NS3 protease
Issue Date: 1-Feb-2010
Citation: Gao, Y., Cui, T., Lam, Y. (2010-02-01). Synthesis and disulfide bond connectivity-activity studies of a kalata B1-inspired cyclopeptide against dengue NS2B-NS3 protease. Bioorganic and Medicinal Chemistry 18 (3) : 1331-1336. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmc.2009.12.026
Abstract: 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 μM, respectively. © 2009 Elsevier Ltd. All rights reserved.
Source Title: Bioorganic and Medicinal Chemistry
URI: http://scholarbank.nus.edu.sg/handle/10635/95060
ISSN: 09680896
DOI: 10.1016/j.bmc.2009.12.026
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