Zobrazeno 1 - 10
of 93
pro vyhledávání: '"Maria L, Webb"'
Autor:
Maria L. Webb, Ilana L. Stroke, Laurie J. Sturzenbecker, David W. Hilbert, Brett A. Marinelli, Joan E. Sabalski, Linh Ma, David J. Diller, Philip D. Stein, Jeffrey J. Letourneau, Jorge Quintero
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:756-761
The discovery, synthesis and preliminary structure-activity relationship (SAR) of a novel class of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB) is described. A high throughput screening (HTS) campaign resulted in the identificati
Autor:
Yanfang Li, Jeffrey J. Letourneau, Laurie J. Sturzenbecker, Maria L. Webb, Brett A. Marinelli, Philip D. Stein, Ilana L. Stroke, Linh Ma, Andrew G. Cole, Igor Pechik, Jorge Quintero, David W. Hilbert, Joan E. Sabalski
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(23-24)
Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess improved
Autor:
Joan E. Sabalski, Yan Xu, Philip D. Stein, Laurie J. Sturzenbecker, Jeffrey J. Letourneau, Teresa Miller, Ilana L. Stroke, Maria L. Webb, Diana R. Savoly, David W. Hilbert, Linh Ma, Igor Pechik
Publikováno v:
Antimicrobial agents and chemotherapy. 62(5)
Clostridium difficile infection (CDI) is the leading cause of hospital-acquired infectious diarrhea, with significant morbidity, mortality, and associated health care costs. The major risk factor for CDI is antimicrobial therapy, which disrupts the n
Autor:
Richard Horuk, Ian Henderson, J. Robert Merritt, Belinda Nedjai, Nagarajan Vaidehi, Emma L. Wise, Anthony E. Klon, Ilana L. Stroke, Hubert Li, Maria L. Webb, Andrew G. Cole, James E. Pease
Publikováno v:
British Journal of Pharmacology
BACKGROUND AND PURPOSE The chemokine receptor CXCR3 directs migration of T-cells in response to the ligands CXCL9/Mig, CXCL10/IP-10 and CXCL11/I-TAC. Both ligands and receptors are implicated in the pathogenesis of inflammatory disorders, including a
Autor:
Jack Pick, Mark Craighead, Heather A. Zanetakos, Jeffrey J. Letourneau, Rachel Milne, Hema Desai, Leigh Campbell-Wan, Jeremy Presland, Michael Ohlmeyer, James R. Baker, Nasrin Ansari, Ray Jui-Hsiang Chan, Cliona P MacSweeney, Douglas S. Auld, Maria L. Webb, Jiuqiao Zhao, Chris Riviello, J. Richard Morphy, Stuart A. Best, Irina Neagu, Susan Elizabeth Napier, Koc-Kan Ho
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3813-3817
Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V1b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V1b recept
Autor:
Herman D. Lim, Douglas S. Auld, Maria L. Webb, Jac C. H. M. Wijkmans, Jiuqiao Zhao, Luc Roumen, Rob Leurs, Chris de Graaf, Petra de Kruijf, Martine J. Smit, Véronique A. Renjaän, G.J.R. Zaman
Publikováno v:
Molecular Pharmacology, 80, 1108-1118. American Society for Pharmacology and Experimental Therapeutics
de Kruijf, P, Lim, H D, Roumen, L, Renjaan, V A, Zhao, J, Webb, M J, Auld, D A, Wijkmans, J C H M, Zaman, G J R, Smit, M J, de Graaf, C & Leurs, R 2011, ' Identification of a novel allosteric binding site in the CXCR2 chemokine receptor ', Molecular Pharmacology, vol. 80, pp. 1108-1118 . https://doi.org/10.1124/mol.111.073825
de Kruijf, P, Lim, H D, Roumen, L, Renjaan, V A, Zhao, J, Webb, M J, Auld, D A, Wijkmans, J C H M, Zaman, G J R, Smit, M J, de Graaf, C & Leurs, R 2011, ' Identification of a novel allosteric binding site in the CXCR2 chemokine receptor ', Molecular Pharmacology, vol. 80, pp. 1108-1118 . https://doi.org/10.1124/mol.111.073825
We have shown previously that different chemical classes of small-molecule antagonists of the human chemokine CXCR2 receptor interact with distinct binding sites of the receptor. Although an intracellular binding site for diarylurea CXCR2 antagonists
Autor:
W. Lynn Rogers, Brian F. Mcguinness, Kurt W. Saionz, Steven G. Kultgen, Vikash Srivastava, Hema Desai, Hao Yan, Tara M. Stauffer, Samiran Saha, Koc-Kan Ho, Shengting Zhang, Neelima Mannava, Yan Jiang, Anthony E. Klon, Tailong Li, Juxing Yin, Weiqing Chen, Konghua Jing, Maria L. Webb, Kanak Kanti Majumdar, Laura L. Rokosz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7414-7420
A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features
Autor:
Andrew G. Cole, Douglas S. Auld, Riviello Christopher, Hema Desai, Hong Li, Heather A. Zanetakos, Fiona Thomson, J. Richard Morphy, Jiuqiao Zhao, Susan Elizabeth Napier, Michael Ohlmeyer, Katharine A. Goan, Koc-Kan Ho, Maria L. Webb, Jeffrey J. Letourneau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5394-5397
The discovery, synthesis, and preliminary structure–activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse, three million-member compo
Autor:
Debra G. Goodwin, Tarek S. Mansour, Kenneth C. Appell, Katherine J. Seidl, Amha G. Hewet, Maria L. Webb, Min Gao, James D. Clark, Steve Tam, Martin Hegen, Elizabeth Quadros, Peter T. Symanowicz, Jenny Togias, Jennifer Lussier, Scott H. Schelling, Michael Ohlmeyer, Bojing Wang, Xin Xu, Earl F. Kimble, Mary Collins, Jorge Quintero, Rustem Krykbaev, Dejun Xuan, Cheryl Nickerson-Nutter, Richard Harrison, Yuefei Shao, Christopher Wrocklage, Tsung H. Lin, Andrew G. Cole
Publikováno v:
Arthritis & Rheumatism. 62:2283-2293
Objective All γ-chain cytokines signal through JAK-3 and JAK-1 acting in tandem. We undertook this study to determine whether the JAK-3 selective inhibitor WYE-151650 would be sufficient to disrupt cytokine signaling and to ameliorate autoimmune dis
Autor:
Celia Kingsbury, Irina Neagu, Ming You, Haengsoon Park, Tsung H. Lin, Koc-Kan Ho, Elizabeth Quadros, Maria L. Webb, Michael Ohlmeyer, Yuefei Shao, Matthew Sills, Jeffrey J. Letourneau, Andrew G. Cole, Yingchun Lu, Earl F. Kimble, Jorge Quintero, Riviello Christopher, Ray Anthony James, Bojing Wang, Vidyadhar M. Paradkar, Adolph Bohnstedt, Kenneth C. Appell, David J. Diller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6788-6792
A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was ident