Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Walter Trizna"'
Autor:
Donald P. McDonnell, John D. Norris, Dmitri Kazmin, Scott K. Thompson, Jaclyn R. Patterson, Marlys Hammond, Walter Trizna, Nicholas J. Laping, Jeffrey D. Bray, Christine G. Schnackenberg, Daniel E. Frigo, Andrea B. Sherk
Androgens, through their actions on the androgen receptor (AR), are required for the development of the prostate and contribute to the pathologic growth dysregulation observed in prostate cancers. Consequently, androgen ablation has become an essenti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95e83eb3282c67e787f8942ba5a7c35a
https://doi.org/10.1158/0008-5472.c.6498402
https://doi.org/10.1158/0008-5472.c.6498402
Autor:
Donald P. McDonnell, John D. Norris, Dmitri Kazmin, Scott K. Thompson, Jaclyn R. Patterson, Marlys Hammond, Walter Trizna, Nicholas J. Laping, Jeffrey D. Bray, Christine G. Schnackenberg, Daniel E. Frigo, Andrea B. Sherk
Supplementary Data from Development of a Small-Molecule Serum- and Glucocorticoid-Regulated Kinase-1 Antagonist and Its Evaluation as a Prostate Cancer Therapeutic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd34ad071b42869122db0e920ae8004b
https://doi.org/10.1158/0008-5472.22377012.v1
https://doi.org/10.1158/0008-5472.22377012.v1
Autor:
Rakesh Nagilla, Sharada Manns, Eugene L. Stewart, Marlys Hammond, Tram H. Hoang, Scott K. Thompson, Walter Trizna, Chaya Duraiswami, Eugene T. Grygielko, Thuy B. Tran, James S. Frazee, Kevin P. Madauss, Johnson Latisha C, Shawn P. Williams, Lindsay E. Glace, David G. Washburn, Jeffrey D. Bray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4664-4668
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In
Publikováno v:
European Journal of Pharmacology. 345:229-232
[ 125 I]Endothelin-1 bound with high affinity to a single site on both brush border membranes ( K d =192±26 pM, B max =314±49 fmol/mg) and basolateral membranes ( K d =94.7±3.4 pM, B max =612±107 fmol/mg) isolated from rat renal cortex. Competiti
Autor:
Marlys Hammond, David G. Washburn, Angela Smallwood, Tram H. Hoang, Nicholas J. Laping, Rebecca Trejo, Hiroko Nakamura, James S. Frazee, Martha S. Head, Scott K. Thompson, Kendra E. Hightower, Charlene Wu, Rakesh Nagilla, Jaclyn R. Patterson, Melanie Nord, Walter Trizna, Baoguang Zhao, Sharada Manns, Leonard M. Azzarano, Christine G. Schnackenberg
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
The lead serum and glucocorticoid-related kinase 1 (SGK1) inhibitors 4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid (1) and {4-[5-(2-naphthalenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]phenyl}acetic acid (2) suffer from low DNAUC values in rat, due i
Autor:
Eugene T. Grygielko, Shawn P. Williams, Lindsay E. Glace, Jeffrey D. Bray, Chaya Duraiswami, James S. Frazee, Kevin P. Madauss, David G. Washburn, Tram H. Hoang, Leahann Lapinski, Walter Trizna, Nicholas J. Laping, Scott K. Thompson
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrroli
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists
Autor:
Jaclyn R. Patterson, Scott K. Thompson, Harvey E. Fries, Eugene T. Grygielko, Walter Trizna, Tram H. Hoang, Jeffrey D. Bray, Nicholas J. Laping, Douglas J. Minick, Melanie Nord, Lindsay E. Glace, Rakesh Nagilla, Marlys Hammond, Sharada Manns, David G. Washburn
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(10)
Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands behaved as potent partial ag
Autor:
Marlys Hammond, Walter Trizna, Andrea B. Sherk, Donald P. McDonnell, Nicholas J. Laping, Jeffrey D. Bray, Daniel E. Frigo, Dmitri Kazmin, Scott K. Thompson, Christine G. Schnackenberg, John D. Norris, Jaclyn R. Patterson
Publikováno v:
Cancer research. 68(18)
Androgens, through their actions on the androgen receptor (AR), are required for the development of the prostate and contribute to the pathologic growth dysregulation observed in prostate cancers. Consequently, androgen ablation has become an essenti
Autor:
Walter Trizna, Richard M. Edwards
Publikováno v:
Pharmacology. 41:149-152
The effects of endothelin-1, -2 and -3 (ET-1, -2, -3) on lumen diameter of intracerebral arterioles isolated from rat brain were examined. All three ETs produced concentration-dependent decreases in lumen diameter with EC50 values of 0.7, 1.5 and 58
Autor:
Richard M. Edwards, Walter Trizna
Publikováno v:
Journal of the American Society of Nephrology : JASN. 4(5)
The inhibition of nitric oxide production has been shown to reduce RBF. The effects of the nitric oxide synthase inhibitors, N omega-nitro-L-arginine and NG-monomethyl-L-arginine, on afferent and efferent arterioles isolated from rabbit kidneys were