Substrate specificity and screening of the integral membrane protease Pla

被引:13
作者
Agarkov, Anton [1 ]
Chauhan, Sadhana [2 ,3 ]
Lory, Pedro J. [1 ]
Gilbertson, Scott R. [1 ]
Motin, Vladimir L. [2 ,3 ]
机构
[1] Univ Texas Galveston, Med Branch, Dept Pharmacol & Toxicol, Chem Biol Program, Galveston, TX 77555 USA
[2] Univ Texas Galveston, Med Branch, Dept Pathol, Galveston, TX 77555 USA
[3] Univ Texas Galveston, Med Branch, Dept Microbiol & Immunol, Galveston, TX 77555 USA
关键词
D O I
10.1016/j.bmcl.2007.09.104
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper reports a study to find small peptide substrates for the important virulence factor of Yersinia pestis, plasminogen activator, Pla. The method used to find small substrates for this protease is reported along with studies examining the ability of these peptides to inhibit activity of the enzyme. Through the use of parallel synthesis and positional scanning, small tripeptides were identified that are viable substrates for the protease. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:427 / 431
页数:5
相关论文
共 17 条
[1]   PESTICINS .3. EXPRESSION OF COAGULASE AND MECHANISM OF FIBRINOLYSIS [J].
BEESLEY, ED ;
BRUBAKER, RR ;
JANSSEN, WA ;
SURGALLA, MJ .
JOURNAL OF BACTERIOLOGY, 1967, 94 (01) :19-+
[2]   Role of the pleiotropic effects of plasminogen deficiency in infection experiments with plasminogen-deficient mice [J].
Goguen, JD ;
Bugge, T ;
Degen, JL .
METHODS-A COMPANION TO METHODS IN ENZYMOLOGY, 2000, 21 (02) :179-183
[3]   Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries [J].
Harris, JL ;
Backes, BJ ;
Leonetti, F ;
Mahrus, S ;
Ellman, JA ;
Craik, CS .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2000, 97 (14) :7754-7759
[4]   GENERATION AND USE OF SYNTHETIC PEPTIDE COMBINATORIAL LIBRARIES FOR BASIC RESEARCH AND DRUG DISCOVERY [J].
HOUGHTEN, RA ;
PINILLA, C ;
BLONDELLE, SE ;
APPEL, JR ;
DOOLEY, CT ;
CUERVO, JH .
NATURE, 1991, 354 (6348) :84-86
[5]   Protein regions important for plasminogen activation and inactivation of α2-antiplasmin in the surface protease Pla of Yersinia pestis [J].
Kukkonen, M ;
Lähteenmäki, K ;
Suomalainen, M ;
Kalkkinen, N ;
Emödy, L ;
Lång, H ;
Korhonen, TK .
MOLECULAR MICROBIOLOGY, 2001, 40 (05) :1097-1111
[6]  
Lähteenmäki K, 1998, INFECT IMMUN, V66, P5755
[7]   Bacterial plasminogen activators and receptors [J].
Lähteenmäki, K ;
Kuusela, P ;
Korhonen, TK .
FEMS MICROBIOLOGY REVIEWS, 2001, 25 (05) :531-552
[8]   A plasminogen-activating protease specifically controls the development of primary pneumonic plague [J].
Lathem, Wyndham W. ;
Price, Paul A. ;
Miller, Virginia L. ;
Goldman, William E. .
SCIENCE, 2007, 315 (5811) :509-513
[9]   Protease inhibitors: Current status and future prospects [J].
Leung, D ;
Abbenante, G ;
Fairlie, DP .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (03) :305-341
[10]   NOVEL FLUOROGENIC SUBSTRATES FOR ASSAYING RETROVIRAL PROTEASES BY RESONANCE ENERGY-TRANSFER [J].
MATAYOSHI, ED ;
WANG, GT ;
KRAFFT, GA ;
ERICKSON, J .
SCIENCE, 1990, 247 (4945) :954-958