Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Siegfried S. F. Leung"'
Autor:
Jonathan W. Choy, Clifford Bryant, Claudia M. Calvet, Patricia S. Doyle, Shamila S. Gunatilleke, Siegfried S. F. Leung, Kenny K. H. Ang, Steven Chen, Jiri Gut, Juan A. Oses-Prieto, Jonathan B. Johnston, Michelle R. Arkin, Alma L. Burlingame, Jack Taunton, Matthew P. Jacobson, James M. McKerrow, Larissa M. Podust, Adam R. Renslo
Publikováno v:
Beilstein Journal of Organic Chemistry, Vol 9, Iss 1, Pp 15-25 (2013)
Inhibition of the Trypanosoma cruzi cysteine protease cruzain has been proposed as a therapeutic approach for the treatment of Chagas’ disease. Among the best-studied cruzain inhibitors to date is the vinylsulfone K777 (1), which has proven effecti
Externí odkaz:
https://doaj.org/article/e62bfad262f447a899c4489a4219fb1f
Autor:
Chiung-Kuang Chen, Siegfried S F Leung, Christophe Guilbert, Matthew P Jacobson, James H McKerrow, Larissa M Podust
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 4, Iss 4, p e651 (2010)
Chagas Disease is the leading cause of heart failure in Latin America. Current drug therapy is limited by issues of both efficacy and severe side effects. Trypansoma cruzi, the protozoan agent of Chagas Disease, is closely related to two other major
Externí odkaz:
https://doaj.org/article/3c8ebb4f64374e618f2ba5c1db8617ba
Autor:
David Price, Melissa Thang, Heather Eng, Spiros Liras, Gilles H. Goetz, Joshua Schwochert, Chris Limberakis, R. Scott Lokey, Bhagyashree Khunte, Kelsie M. Rodriguez, Matthew P. Jacobson, Siegfried S. F. Leung, Alexandra R. Ponkey, Ray F. Berkeley, Michael J. Shapiro, Alan M. Mathiowetz, Rushia A. Turner, Amit S. Kalgutkar
Publikováno v:
Organic Letters. 17:2928-2931
The effect of peptide-to-peptoid substitutions on the passive membrane permeability of an N-methylated cyclic hexapeptide is examined. In general, substitutions maintained permeability but increased conformational heterogeneity. Diversification with
Autor:
Bhagyashree Khunte, Sangwoo Ryu, Jiangli Yan, Markus Boehm, Amit S. Kalgutkar, Kevin Beaumont, Janice A. Brown, Heather Eng, Laurie Tylaska, R. Scott Lokey, David Price, Elnaz Menhaji-Klotz, Chris Limberakis, Michael J. Shapiro, Guoyun Bai, Brian R. Holder, Liying Zhang, Sarah Lazzaro, Matthew P. Jacobson, Spiros Liras, David J. Earp, Alan M. Mathiowetz, Rhys M. Jones, Gilles H. Goetz, Siegfried S. F. Leung, Mahesh Ramaseshan, Rushia A. Turner, Karen Atkinson
Publikováno v:
Journal of medicinal chemistry. 60(23)
The chemokine receptor CXCR7 is an attractive target for a variety of diseases. While several small-molecule modulators of CXCR7 have been reported, peptidic macrocycles may provide advantages in terms of potency, selectivity, and reduced off-target
Publikováno v:
Journal of chemical information and modeling. 56(5)
We investigate the relationship between passive permeability and molecular size, in the context of solubility-diffusion theory, using a diverse compound set with molecular weights ranging from 151 to 828, which have all been characterized in a consis
Publikováno v:
Journal of Medicinal Chemistry. 55:4489-4500
The effects of addition of a methyl group to a lead compound on biological activity are examined. A literature analysis of >2000 cases reveals that an activity boost of a factor of ten or more is found with an 8% frequency, and a 100-fold boost is a
Autor:
Bhagyashree Khunte, David Price, Charles J. Rotter, Heather Eng, Siegfried S. F. Leung, Yizhong Zhang, Manthena V.S. Varma, Chris Limberakis, Spiros Liras, R. Scott Lokey, Amit S. Kalgutkar, Raman Sharma, Matthew P. Jacobson, Alan M. Mathiowetz, Kathleen A. Farley, Arthur C Rand
Publikováno v:
MedChemComm. 3:1282-1289
A series of cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of na
Autor:
Spiros Liras, Cayla M. McEwen, Rushia A. Turner, David Price, Taha Rezai, Amit S. Kalgutkar, Roger G. Linington, Alan M. Mathiowetz, R. Scott Lokey, Matthew P. Jacobson, Arthur C Rand, Yizhong Zhang, Vladimir Gelev, Chad M. Renzelman, Siegfried S. F. Leung, Tina R White, Jonathan N. Bauman
Publikováno v:
Nature chemical biology
Backbone N-methylation is common among peptide natural products and has a substantial impact on both the physical properties and the conformational states of cyclic peptides. However, the specific impact of N-methylation on passive membrane diffusion
Autor:
Christine M. Crane, William L. Jorgensen, Dale L. Boger, Joshua G. Pierce, Julian Tirado-Rives, Siegfried S. F. Leung
Publikováno v:
Journal of Medicinal Chemistry. 53:7229-7235
A select series of methyl ether derivatives of vancomcyin aglycon were prepared and examined for antimicrobial activity against vancomycin-sensitive Staphylococcus aureus and vancomycin-resistant Enterococci faecalis, as well as their binding affinit
Autor:
Larissa M. Podust, Stephanie D. Hopkins, Jonathan B. Johnston, Matthew P. Jacobson, James H. McKerrow, Juan C. Engel, Chiung-Kuang Chen, Patricia S. Doyle, Siegfried S. F. Leung
Publikováno v:
Antimicrobial Agents and Chemotherapy. 54:2480-2488
Chagas’ disease, the leading cause of heart failure in Latin America, is caused by the kinetoplastid protozoan Trypanosoma cruzi. The sterols of T. cruzi resemble those of fungi, both in composition and in biosynthesis. Azole inhibitors of sterol 1