Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Kevin R. Shreder"'
Autor:
Allister Fraser, Kevin R. Shreder, Junichi Ishiyama, John W. Kozarich, Yi Hu, Yasushi Kohno, Heidi E. Brown, Lingling Du, Eric Okerberg, Christopher M. Amantea, Julia Cajica, Emme C.K. Lin, Lan M. Pham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1553-1556
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn2+-dependent, 27 nM inhibitor of human plasma Lp-PLA2. Structure–activity relationship studies focused on the AX10479 2-phenylamide gro
Autor:
Eric Okerberg, Julia Cajica, Kevin R. Shreder, Yasushi Kohno, Lan M. Pham, Heidi E. Brown, Junichi Ishiyama, Yi Hu, John W. Kozarich, Allister Fraser, Lingling Du, Emme C.K. Lin, Christopher M. Amantea
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:868-871
AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100 nM inhibitor of Lp-PLA2. However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA2 did not change. Subsequent
Autor:
Kevin R. Shreder, Tyzoon K. Nomanbhoy, Ayako Nakamura, Anna Katrin Szardenings, Shigeki Seto, Jonathan S. Rosenblum, Brandon Leen, Oana Cociorva, Kai Nakamura, Bei Li, Marek Liyanage, John W. Kozarich, Qiang Li, Yasushi Kohno, Kazuhiro Yumoto, Kyoko Okada, Masahiro Nomura, Melissa C. Zhang, Arwin Aban
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5948-5951
The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this
Autor:
Wenzhi Gai, Sergio Corral, Jonathan S. Rosenblum, Kevin R. Shreder, Douglas K. Ferris, Yongsheng Liu
Publikováno v:
Chemistry & Biology. 12:99-107
SummaryPolo-like kinases (PLKs) play critical roles throughout mitosis. Here, we report that wortmannin, which was previously thought to be a highly selective inhibitor of phosphoinositide (PI) 3-kinases, is a potent inhibitor of mammalian PLK1. Obse
Publikováno v:
Organic Letters. 6:3715-3718
[structure: see text] The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a protected tetraethyleneglycol linker followed by the attachment of tetramethylrhodamine y
Publikováno v:
Bioconjugate Chemistry. 11:557-563
The electrospray ionization-mass spectrometry (ESI-MS) analysis of three sets of monoclonal antibody-acridinium-9-carboxamide conjugates is described. The conjugates (nine total) were enzymatically digested using papain and the resulting fragments [F
Publikováno v:
Bioconjugate Chemistry. 10:1032-1037
Surface plasmon resonance (SPR) analysis was used to assess the immunoreactivity of anti-biotin (4) and anti-fluorescein (5) monoclonal antibody after conjugation with the N-hydroxysuccinimide ester of acridinium-9-carboxamide 1. Only minor changes i
Autor:
Kai Nakamura, Qiang Li, Tyzoon K. Nomanbhoy, Ann Yu-Jung Shih, Helge Weissig, Oana Cociorva, Lan Pham, John W. Kozarich, Yi Hu, Melissa C. Zhang, Marek Liyanage, Julia Cajica, Kevin R. Shreder, Arwin Aban, Bei Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(18)
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50 = 160 nM) which was co-crystallized with JNK1 to identify key molecular interactio
Autor:
Yi, Hu, Emme C K, Lin, Lan M, Pham, Julia, Cajica, Christopher M, Amantea, Eric, Okerberg, Heidi E, Brown, Allister, Fraser, Lingling, Du, Yasushi, Kohno, Junichi, Ishiyama, John W, Kozarich, Kevin R, Shreder
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(5)
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn(2+)-dependent, 27nM inhibitor of human plasma Lp-PLA(2). Structure-activity relationship studies focused on the AX10479 2-phenylamide gr
Autor:
Kevin R. Shreder, Jonathan S. Rosenblum, Allister Fraser, Ethel McGee, Christopher M. Amantea, Yi Hu, Emme C.K. Lin, Lan M. Pham, John W. Kozarich, Heidi E. Brown, De Michael Chung, Jiangyue Wu, Julia Cajica, Eric Okerberg
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
KIAA1363 is a serine hydrolase whose activity has been shown to be positively associated with tumor cell invasiveness. Thus, inhibitors of KIAA1363 represent a novel targeted therapy approach towards cancer. AX11890 ((1-bromo-2-naphthyl) N,N-dimethyl