Zobrazeno 1 - 10
of 47
pro vyhledávání: '"Douglas W. Morgan"'
Autor:
Lisa A. Marshall, Douglas W. Morgan
The purpose of this volume in the series Progress in Inflammation Research is to pro vide the biomedical researcher with a description of the state of the art of the devel opment and use of animal models of diseases with components of inflammatio
Autor:
Douglas W. Morgan, Jennifer J. Bouska, H. Robin Heyman, Patrick A. Marcotte, Yujia Dai, Steven K. Davidsen, Carole L. Goodfellow, Carol K. Wada, Daniel H. Albert, Jamie R. Stacey, Robert B. Garland, Douglas H. Steinman, Paul Tapang, Alan S. Florjancic, Michael L. Curtin, James H. Holms, Yan Guo, Michael R. Michaelides, Ildiko Elmore
Publikováno v:
Journal of Medicinal Chemistry. 45:219-232
A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matrix metalloproteinases (MMP) inhibitors. The substitution of the ether linkage of ABT-770 (5) with a sulfone group 13a led to a substantial increase in
Autor:
Michael R. Michaelides, James H. Holms, Douglas W. Morgan, Katherine Mast, Steven K. Davidsen, Ildiko Elmore, Lori J. Pease, Keith B. Glaser, Junling Li, Patrick A. Marcotte
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2907-2910
Modification of the P 1 ′ substituent of macrocyclic matrix metalloproteinase (MMP) inhibitors provided compounds that are selective for inhibition of tumor necrosis factor-α converting enzyme (TACE) over MMP-1 and MMP-2. Several analogues potentl
Autor:
Douglas W. Morgan, H. Robin Heyman, Michael R. Michaelides, Jamie R. Stacey, Patrick A. Marcotte, Yan Guo, Steven K. Davidsen, Michael L. Curtin, Carole L. Goodfellow, Joseph F. Dellaria, Daniel H. Albert, Jane Gong, James H. Holms, Terrance J. Magoc, Jennifer J. Bouska, Ildiko B. Elmore, Carol K. Wada
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1553-1556
A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against MMP-1. Select members of this series exhibit excellent pharmacokinetic properties with lon
Autor:
Yongjing Guo, Douglas W. Morgan, Shafaat A. Rabbani, Steven K. Davidsen, Penelope Harakidas, Douglas H. Steinman
Publikováno v:
International Journal of Cancer. 87:276-282
Members of the matrix metalloprotease (MMP) family are implicated in the progression of several malignancies including prostate cancer due to their ability to break down extracellular matrix (ECM) components. In this study, we have evaluated the abil
Publikováno v:
Biochemical Pharmacology. 57:291-302
The monocytic cell line THP-1 can be induced to express and release tumor necrosis factor alpha (TNFalpha) and both TNFalpha receptors (p55 and p75) upon exposure to bacterial lipopolysaccharide (LPS). The broad-spectrum matrix metalloprotease (MMP)
Autor:
Steven K. Davidsen, Patrick A. Marcotte, Terrance J. Magoc, James H. Holms, Zhiwen Guan, Robert B. Garland, Douglas H. Steinman, Douglas W. Morgan, Daniel H. Albert, Carol K. Wada, Yan Guo, H. Robin Heyman, Michael L. Curtin, George S. Sheppard, Ildiko Elmore
Publikováno v:
Journal of Enzyme Inhibition. 14:425-435
Two series of compounds synthesized as specific matrix metalloproteinase (MMP) inhibitors have been evaluated for their inhibition of non-MMPs. In a series of substituted succinyl hydrox-amic acids, some were found to be significant (IC50 < 1 μM) in
Autor:
L. Gordon Letts, Douglas W. Morgan
In November 1998 many of the key leaders of new drug discovery for inflammatory diseases gathered at Hershey, Pennsylvania for the 9th International Conference of the Inflammation Research Association. The Conference was held over a five day period a
How are cancer and inflammation interrelated mechanistically and clinically? Though extensive literature exists on the topic'Cancer and Inflammation', there are relatively few texts that have truly integrated the two in spite of the many common mecha
Autor:
Terrance J. Magoc, Yan Guo, Patrick A. Marcotte, George S. Sheppard, Carole L. Goodfellow, Steven K. Davidsen, Lianhong Xu, Alan S. Florjancic, Giesler Jamie, Douglas W. Morgan, Jennifer J. Bouska, Daniel H. Albert, Ildiko Elmore, James B. Summers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3251-3256
A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several