Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Matthew R. Yudt"'
Autor:
Thomas J. Berrodin, Leonard P. Freedman, Elaine Quinet, Qi Shen, Matthew R. Yudt, Sunil Nagpal
Publikováno v:
Molecular Pharmacology. 78:1046-1058
The liver X receptors (LXRα and LXRβ) are members of the nuclear receptor superfamily that function as key transcriptional regulators of a number of biological processes, including cholesterol homeostasis, lipid metabolism, and keratinocyte differe
Autor:
Richard C. Winneker, Thomas J. Berrodin, Nilsa Graciani, Zhiming Zhang, Matthew R. Yudt, Sunil Nagpal, John A. Butera, Scott A. Jelinsky
Publikováno v:
Biochemical Pharmacology. 77:204-215
Progesterone receptor (PR) modulators are used in contraception and post-menopausal hormone therapy, and are under clinical development for reproductive disorders such as uterine fibroids and endometriosis. Development of tissue selective PR modulato
Autor:
Richard C. Winneker, Puwen Zhang, Terefenko Eugene Anthony, Zhiming Zhang, Andrew Fensome, Jeffrey I. Cohen, Ray Unwalla, Jay E. Wrobel, Matthew R. Yudt, Thomas J. Berrodin, Jeffrey Curtis Kern
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:6589-6600
Novel 7-aryl benzo[1,4]oxazepin-2-ones were synthesized and evaluated as non-steroidal progesterone receptor (PR) modulators. The structure activity relationship of 7-aryl benzo[1,4]oxazepinones was examined using the T47D cell alkaline phosphatase a
Autor:
John A. Cidlowski, Matthew R. Yudt
Publikováno v:
Molecular Endocrinology. 15:1093-1103
The human glucocorticoid receptor (hGRalpha) is a ligand-activated transcription factor that mediates the physiological effects of corticosteroid hormones and is essential for life. Originally cloned in 1986, the transcriptionally active hGRalpha was
Autor:
Zhiming Zhang, Jeffrey Cohen, Puwen Zhang, Terefenko Eugene Anthony, Richard C. Winneker, Eugene John Trybulski, Yuan Zhu, Jeffrey Curtis Kern, Thomas J. Berrodin, Matthew R. Yudt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4816-4818
Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase assay. Moderate to potent PR
Autor:
Matthew R. Yudt, Daphne M. Bofetiado, Robert H. Oakley, John A. Cidlowski, Christine M. Jewell
Publikováno v:
Journal of Biological Chemistry. 274:27857-27866
Alternative splicing of the human glucocorticoid receptor gene generates a nonhormone binding splice variant (hGRbeta) that differs from the wild-type receptor (hGRalpha) only at the carboxyl terminus. Previously we have shown that hGRbeta inhibits t
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 52:159-171
We report here that the human estrogen receptor (hER) overexpressed in Sf9 insect cells is phosphorylated similarly to hER from the human MCF-7 mammary carcinoma cell line. The recombinant and native hER labeled to steady-state with [32P]phosphate we
Autor:
Michael Marella, Christine Huselton, Edward Melenski, Casey C. McComas, Richard C. Winneker, Cheryl Mugford, Jeffrey Cohen, Andrew Fensome, Matthew R. Yudt, Ov D. Slayden, Jay Wrobel
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(23)
We have developed a new series of progesterone receptor modulators based upon the 4-aryl-phenylsulfonamide. Initial work in the series afforded potent compounds with good properties, however an advanced intermediate proved to be genotoxic in a non-GL
A mutation in the D-loop of the second zinc finger of the DNA-binding domain of the human glucocorticoid receptor (hGR), A458T (GR(dim)), has been suggested to be essential for dimerization and DNA binding of the GR, and genetically altered GR(dim) m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be2e35e26462a818b805030a37351836
https://europepmc.org/articles/PMC3275167/
https://europepmc.org/articles/PMC3275167/
Autor:
Matthew R. Yudt, Elizabeth Haglund, Scott A. Jelinsky, Louise A. Russo, Sunil Nagpal, Andrew Fensome, Raymond J. Unwalla, Jeffrey Cohen, Thomas J. Berrodin, Zhiming Zhang, Debra Ellis, Richard C. Winneker, Neil Cooch, Jay Wrobel
Publikováno v:
Biochemical pharmacology. 82(11)
WAY-255348 is a potent nonsteroidal progesterone receptor (PR) antagonist previously characterized in rodents and nonhuman primates. This report describes the novel mechanism by which WAY-255348 inhibits the activity of progesterone. Most PR antagoni