Zobrazeno 1 - 10
of 70
pro vyhledávání: '"MARK E. GOLDMAN"'
Autor:
Daniel Grant, Peter Teriete, John C. Reed, Pooi-San Lee, Anna Dembo, Douglas J. Sheffler, Nicholas D. P. Cosford, Haixia Zou, Gavin Magnuson, Allison S. Limpert, Jiwen Zou, Anthony B. Pinkerton, Mark E. Goldman, Robert Ardecky, Juan Rong
Publikováno v:
ACS Chemical Neuroscience
Endoplasmic reticulum (ER) stress causes neuronal dysfunction followed by cell death and is recognized as a feature of many neurodegenerative diseases. Using a phenotypic screen, we recently identified benzodiazepinone derivatives that reduce ER stre
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
Autor:
James P. Edwards, Todd K. Jones, Keith B. Marschke, Ming-Wei Wang, Pooley Charlotte L F, Mark E. Goldman, Diane L. Crombie
Publikováno v:
Journal of Medicinal Chemistry. 41:3461-3466
A series of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines was synthesized and tested for functional activity on the human progesterone receptor isoform B (hPR-B) in mammalian (CV-1) cells. The lead compound LG001447 (1,2-dihydro-2,2, 4-trimethyl-6-phe
Publikováno v:
SLAS Discovery. 2:213-223
Activated transcription factor AP-1 is composed of c-Jun homodimers or c-Jun/c-Fos heterodimers and mediates expression of several gene products that have been implicated in disease pathogenesis. Activation of AP-1 is dependent on phosphorylation of
Autor:
Todd K. Jones, Robert B. Stein, Teodoro Ianiro, Luc J. Farmer, Mark E. Goldman, Michael G. Johnson, Dale E. Mais, Charles Pathirana, Bender Steven Lee, Lawrence G. Hamann
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 56:61-66
Utilizing the co-transfection assay as a guide to determining structure activity relationships, we have been pursuing the discovery of non-steroidal hPR modulators. Small molecule, non-steroidal lead structures have been identified. Optimization of t
Autor:
Michael G. Johnson, Mark E. Goldman, Diane Crombie, Bender Steven Lee, Dale E. Mais, Luc J. Farmer, Ming-Wei Wang, Todd K. Jones, Lawrence G. Hamann
Publikováno v:
Journal of Medicinal Chemistry. 39:1778-1789
A novel class of nonsteroidal progesterone receptor antagonists has been synthesized and was shown to exhibit moderate binding affinity for hPR-A, the ability to inhibit the transcriptional activity of human progesterone receptor (hPR) in cell-based
Autor:
Richard G. Ball, William C. Lumma, S. F. Britcher, Catherine M. Wiscount, Steven D. Young, William M. Sanders, Mark E. Goldman, Terry A. Lyle, Thomas J. Tucker, Julie A. O'Brien
Publikováno v:
Journal of Medicinal Chemistry. 37:2437-2444
As part of an ongoing effort to prepare novel non-nucleoside inhibitors of human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT), a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin -2(1H)-ones 4aa-l has been pre
Autor:
Mark E. Goldman, Donald P. McDonnell
Publikováno v:
Journal of Biological Chemistry. 269:11945-11949
The human progesterone receptor (hPR) exists in two distinct forms in most cells, hPR-A and hPR-B. Both receptor isoforms exhibit distinct biological functions and demonstrate a cell- and promoter-specific ability to regulate gene transcription. Inte
Autor:
David J. Mangelsdorf, Richard A. Heyman, Marcus F. Boehm, Michael R. McClurg, Jonathan J. Hebert, Charles Pathirana, Steven K. White, David T. Winn, Mark E. Goldman
Publikováno v:
Journal of Medicinal Chemistry. 37:408-414
all-trans-Retinoic acid is known to bind to the retinoic acid receptors (RARs) resulting in an increase in their transcriptional activity. In contrast, recently identified 9-cis-retinoic acid (9-cis-RA), which is an additional endogenous RA isomer, i
Autor:
Donald P. McDonnell, Manouchehr M. Shahbaz, Mark E. Goldman, Elisabetta Vegeto, D. X. Wen, Bert W. O'Malley
Publikováno v:
Molecular Endocrinology. 7:1244-1255
Two distinct isoforms of the human progesterone receptor (hPR-A and hPR-B) have been identified previously. They differ only in that hPR-B contains an additional 164 amino acids at the amino terminus. Among various species these two forms arise as a