Zobrazeno 1 - 10
of 56
pro vyhledávání: '"Roy J. Vaz"'
Autor:
Isaac Yi Kim, Roy J. Vaz, Naoya Nagaya, Hatem E. Sabaawy, Wun-Jae Kim, Gabriele Cruciani, Jenny Desantis, Kiran Madura, Geun Taek Lee
Publikováno v:
Molecular Cancer Therapeutics. 20:490-499
Although second-line antiandrogen therapy (SAT) is the standard of care in men with castration-resistant prostate cancer (CRPC), resistance inevitably occurs. One major proposed mechanism of resistance to SAT involves the emergence of androgen recept
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e2e8855da577ea72c1dabb094e69a8c
https://doi.org/10.1158/1535-7163.mct-20-0417
https://doi.org/10.1158/1535-7163.mct-20-0417
Publikováno v:
European Journal of Organic Chemistry. 2020:5828-5832
The addition of electron deficient radicals to the C2 position of indoles has been described in the literature as opposed to electrophilic addition at the C3 position. Density functional theory calculations were used to understand the switch in regio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::793be05dd835a38c24b43967b1fbc434
https://doi.org/10.1002/ejoc.201901784
https://doi.org/10.1002/ejoc.201901784
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3681-3684
Our internal casein kinase 1ε lead inhibitor, compound 1 was partially cleared by the polymorphic cytochrome P450 2D6. CYP2D6 involvement in metabolism implies more extensive clinical trials. We therefore wanted to reduce the contribution to clearan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77be464c4900f4c7b639f05a1727f4f2
https://doi.org/10.1016/j.bmcl.2018.10.031
https://doi.org/10.1016/j.bmcl.2018.10.031
Publikováno v:
European J Org Chem
The addition of electron deficient radicals to the C2 position of indoles has been described in the literature as opposed to electrophilic addition at the C3 position. Density functional theory calculations were used to understand the switch in regio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::9af6281cb1c8fc740f0b402d91fb1e0d
https://pubmed.ncbi.nlm.nih.gov/33692651
https://pubmed.ncbi.nlm.nih.gov/33692651
Autor:
Nick A. Paras, Daniel G Droege, Takao Ohyama, Jay Conrad, Shimpei Hirano, Roy J. Vaz, Stanley B. Prusiner, Sasaki Koji, Steven H. Olson, Alexander Y Jiu, John W West, Masahiro Inoue, Makoto Hirasawa, Benjamin C Tang, Jean-Marc M Grandjean, Manuel Elepano, Ryo Murakami, Joanne Lee, Masakazu Hirouchi, Atsushi Aoyagi
Publikováno v:
ACS medicinal chemistry letters, vol 11, iss 2
ACS Med Chem Lett
ACS Med Chem Lett
[Image: see text] Tau prions feature in the brains of patients suffering from Alzheimer’s disease and other tauopathies. For the development of therapeutics that target the replication of tau prions, a high-content, fluorescence-based cell assay wa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08f91271b5afcc886791b89cc2cad0e9
https://escholarship.org/uc/item/4cz02519
https://escholarship.org/uc/item/4cz02519
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3046-3049
This work describes the rational amelioration of mechanism-based inactivation (MBI) of Cytochrome P450 (CYP) 3A4 in a human hematopoietic prostaglandin D synthase (hH-PGDS) inhibitor (cpd 1). We utilized metabolism reports in order to check if patter
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ee6320c5ebc14f7ef9e8e4b668151bb
https://doi.org/10.1016/j.bmcl.2018.07.049
https://doi.org/10.1016/j.bmcl.2018.07.049
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:446-451
Abuse of the common anti-diarrheal loperamide is associated with QT interval prolongation as well as development of the potentially fatal arrhythmia torsades de pointes. The mechanism underlying this cardiotoxicity is high affinity inhibition of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcc46fd2ce619143a94f4c900ecad85e
https://doi.org/10.1016/j.bmcl.2017.12.020
https://doi.org/10.1016/j.bmcl.2017.12.020
Autor:
Roy J. Vaz, Donglai Yang, Hong Shen, Xin Chen, Stephan Reiling, Raymond Kosley, Theresa A. Kuntzweiler, Joseph D. Batchelor, Ying Zhang, Yi Li, Vinolia Chellaraj, Larry R. McLean
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3194-3196
This work describes the rational amelioration of Cytochrome P450 4/5 (CYP3A4/5) induction through the Pregnane-X Receptor (PXR) pathway in a series of compounds that modulate the metabotropic glutamate Receptor 2 (mGluR2) via an allosteric mechanism.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::223ef5c9e1949c1ea3dc68860707b446
https://doi.org/10.1016/j.bmcl.2018.08.022
https://doi.org/10.1016/j.bmcl.2018.08.022
Publikováno v:
Journal of Biological Chemistry. 290:11041-11051
The chemokine receptors CCR5 and CCR2b share 89% amino acid homology. CCR5 is a co-receptor for HIV and CCR5 antagonists have been investigated as inhibitors of HIV infection. We describe the use of two CCR5 antagonists, Schering-C (SCH-C), which is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3260292980f8cf023af8a0d06f05e55b
https://doi.org/10.1074/jbc.m115.640169
https://doi.org/10.1074/jbc.m115.640169
With its focus on emerging concerns of kinase and GPCR-mediated antitarget effects, this vital reference for drug developers addresses one of the hot topics in drug safety now and in future. Divided into three major parts, the first section deals wit