Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Lynne Cregar"'
Autor:
Guan-Sheng Jiao, Seongjin Kim, Linda McKasson, Lynne Cregar-Hernandez, Alan T. Johnson, Mahtab Moayeri, Sean O’Malley, Stephen H. Leppla, April Thai
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:134-139
Anthrax is a highly lethal disease caused by the Gram-(+) bacteria Bacillus anthracis. Edema toxin (ET) is a major contributor to the pathogenesis of disease in humans exposed to B. anthracis. ET is a bipartite toxin composed of two proteins secreted
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b6adfc5fae60ef4e440ba736b74aa72
https://doi.org/10.1016/j.bmcl.2017.11.040
https://doi.org/10.1016/j.bmcl.2017.11.040
Autor:
Linda McKasson, Seongjin Kim, April Thai, Stephen A. Margosiak, Sina Sareth, Sean O’Malley, Lynne Cregar-Hernandez, Guan-Sheng Jiao, Alan T. Johnson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:2505-2511
A novel method for applying high-throughput docking to challenging metalloenzyme targets is described. The method utilizes information-based virtual transformation of library carboxylates to hydroxamic acids prior to docking, followed by compound acq
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c36dbee74eed747a17249d37f2dc548c
https://doi.org/10.1016/j.bmcl.2013.03.030
https://doi.org/10.1016/j.bmcl.2013.03.030
Autor:
Lisa Johns, Seongjin Kim, Axel T. Lehrer, Alan T. Johnson, Stephen A. Margosiak, April Thai, Guan-Sheng Jiao, Banumathi Sankaran, Linda McKasson, Teri Wong, Devorah Crown, Stephen H. Leppla, Lynne Cregar-Hernandez, Mahtab Moayeri
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2242-2246
Four core structures capable of providing sub-nanomolar inhibitors of anthrax lethal factor (LF) were evaluated by comparing the potential for toxicity, physicochemical properties, in vitro ADME profiles, and relative efficacy in a rat lethal toxin (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0149d4f3b3b427a4f4c3e025e425da71
https://doi.org/10.1016/j.bmcl.2012.01.095
https://doi.org/10.1016/j.bmcl.2012.01.095
Publikováno v:
FEBS Journal. 273:3054-3062
We report a detailed kinetic investigation of the aminoglycosides neomycin B and neamine as inhibitors of the lethal factor protease from Bacillus anthracis. Both inhibitors display a mixed-type, noncompetitive kinetic pattern, which suggests the exi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::239ac1229701ffdf2a354a7ab291d1f1
https://doi.org/10.1111/j.1742-4658.2006.05316.x
https://doi.org/10.1111/j.1742-4658.2006.05316.x
Autor:
Roopa Rai, Kyle Elrod, William D. Shrader, James W. Janc, Yong Li, Lynne Cregar, Wendy B. Young, Aleksandr Kolesnikov, Thomas E. Jenkins, Paul R. Fatheree, Brad A. Katz, Erik Verner, Paul A. Sprengeler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:710-713
Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::890f430c3bb6f05e6bfb08f3695a2bf1
https://doi.org/10.1016/j.bmcl.2005.10.023
https://doi.org/10.1016/j.bmcl.2005.10.023
Autor:
Roopa Rai, Kyle Elrod, Aleksandr Kolesnikov, Jeff Spencer, William D. Shrader, Jana Burgess-Henry, Wendy B. Young, Lynne Cregar, Ellen M. Leahy, Paul A. Sprengeler, Joan Sangalang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2253-2256
The structure-based design and progression of a screening lead to a 3 nM factor VIIa/TF inhibitor with improved selectivity versus related enzymes is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb6e45f85521988cd634481a34db8e9d
https://doi.org/10.1016/s0960-894x(01)00420-6
https://doi.org/10.1016/s0960-894x(01)00420-6
Autor:
Yong Li, Lynne Cregar, Jana Burgess-Henry, Ellen M. Leahy, Allen Darin Arthur, Erik Verner, Wendy B. Young, Aleksandr Kolesnikov, Roopa Rai, William D. Shrader, Xi Chen, Bradley A. Katz, Paul A. Sprengeler, Kyle Elrod, Christine Luong, Joan Sangalang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1797-1800
The development of potent and selective small molecule inhibitors of factor Xa is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff49a67d4177d7e7b2ee9496efe25ae9
https://doi.org/10.1016/s0960-894x(01)00311-0
https://doi.org/10.1016/s0960-894x(01)00311-0
Publikováno v:
Analytical Biochemistry. 281:62-67
Determination of tight-binding inhibition constants by nonlinear least-squares regression requires sufficiently good initial estimates of the best-fit values. Normally an initial estimate of the inhibition constant must be provided by the investigato
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8f45bdc5942f56a855f36b06763ab43
https://doi.org/10.1006/abio.2000.4501
https://doi.org/10.1006/abio.2000.4501
Publikováno v:
Archives of Biochemistry and Biophysics. 366:125-130
Myeloperoxidase (MPO) is an important component of the neutrophil response to microbial infection. In this paper we report an additional activity of MPO, the potent and selective inhibition of human mast cell tryptase. MPO inhibits human mast cell tr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc34d26b136de02716eaf7eee6283deb
https://doi.org/10.1006/abbi.1999.1220
https://doi.org/10.1006/abbi.1999.1220
Autor:
Axel T. Lehrer, Alan T. Johnson, Stephen A. Margosiak, Teri Ann S. Wong, Guan-Sheng Jiao, Lynne Cregar-Hernandez
Publikováno v:
Antiviral chemistrychemotherapy. 21(5)
Background: Dengue fever, dengue haemorrhagic fever, and dengue shock syndrome are caused by infections with any of the four serotypes of the dengue virus (DENV), and are an increasing global health risk. The related West Nile virus (WNV) causes sign
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9d2b3b14c6402a04bd2b8fcbe6d7ee8
https://pubmed.ncbi.nlm.nih.gov/21566267
https://pubmed.ncbi.nlm.nih.gov/21566267