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|Title:||Synthesis and disulfide bond connectivity-activity studies of a kalata B1-inspired cyclopeptide against dengue NS2B-NS3 protease||Authors:||Gao, 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|
|Appears in Collections:||Staff Publications|
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