Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Richard B. Gilbertsen"'
Autor:
Karen Elaine Sexton, Venkataraman Thanabal, Ann McCarthy, Leroy Lu, Erli Zhang, Maria N. Nguyen, Downs Victoria Leigh, Paul R. Keller, Mark L. Boys, Richard Gowan, Patrick I. McConnell, Edmund L. Ellsworth, Neil Raheja, Richard B. Gilbertsen, Hena Mostafa, Filzen Gary Frederick, N. A. Payne, Feng Bian, Huifen Chen, John D. Knafels, Samarendra N. Maiti, Elena M. Drummond, Stephen Douglas Barrett, Zhi Wang, Larry D. Bratton, Diane Alessi, Deepak S. Lala, Stephen Fakhoury, Sneha Patel, Barry C. Finzel, Susan Ciotti, Iula Donna Michele, Fang Sun, Paul Angell, Xiao Dan Ren, David Pocalyko, Rone Eisma, Kramer James Bernard, Catherine R. Kostlan, Christopher L. Chio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3392-3397
A series of 2-(1H-pyrazol-1-yl)pyridines are described as inhibitors of ALK5 (TGFβ receptor I kinase). Modeling compounds in the ALK5 kinase domain enabled some optimization of potency via substitutions on the pyrazole core. One of these compounds P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::632fe42ba8bb00febbc77151eb92bc8f
https://doi.org/10.1016/j.bmcl.2012.04.013
https://doi.org/10.1016/j.bmcl.2012.04.013
Publikováno v:
Scopus-Elsevier
We characterized the activation of interleukin-1β-converting enzyme (ICE)-like proteases (caspases) in human neuroblastoma cells (SH-SY5Y) following challenge with staurosporine, an established agent known to induce apoptosis. Time course analyses o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10a6c597e6170c4b1d52abf1bdcafc78
https://doi.org/10.1046/j.1471-4159.1997.68062328.x
https://doi.org/10.1046/j.1471-4159.1997.68062328.x
Autor:
Robert V. Talanian, Po-Wai Yuen, Daniel Stafford, Avigail Posner, Kevin K.W. Wang, Hamish Allen, Rathna Nath, Iradj Hajimohammadreza, Kadee J. Raser, Richard B. Gilbertsen
Publikováno v:
Biochemical Journal. 319:683-690
The cytoskeletal protein non-erythroid alpha-spectrin is well documented as an endogenous calpain substrate, especially under pathophysiological conditions. In cell necrosis (e.g. maitotoxin-treated neuroblastoma SH-SY5Y cells), alpha-spectrin breakd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e908c233c5fde806f94cc0a8aa53161
https://doi.org/10.1042/bj3190683
https://doi.org/10.1042/bj3190683
Autor:
W. J. Cetenko, Jagadish C. Sircar, Mary K. Bennett, Richard B. Gilbertsen, Catherine R. Kostlan, M. K. Dong
Publikováno v:
ChemInform. 24
Purine nucleoside phosphorylase (PNP) is a purine-metabolizing enzyme in the purine cascade and has been a target for drug design for sometime. A series of potent human PNP inhibitors, pyrrolo[3,2-d]pyrimidines (9-deazaguanines), has been synthesized
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::83ba6214c733e4215bc467aa466a3ac9
https://doi.org/10.1002/chin.199301206
https://doi.org/10.1002/chin.199301206
Autor:
Jagadish C. Sircar, M. C. Conroy, Usha Josyula, Wu Wen-Shen, David J. Wilburn, Ml K. Dong, Richard B. Gilbertsen
Publikováno v:
Biochemical Pharmacology. 44:996-999
An in-parallel comparison is presented of the in vitro and in vivo properties of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase (PNP), CI-972 [8-amino-9-deaza-9-(3-thienylmethyl)guanine] and PD 141955 [9-deaza-9-(3-thienylmet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aac84b9701932e6cc99a1c6acc05bc3a
https://doi.org/10.1016/0006-2952(92)90135-6
https://doi.org/10.1016/0006-2952(92)90135-6
Autor:
Richard B. Gilbertsen, Jagadish C. Sircar, M. K. Dong, W. J. Cetenko, Catherine R. Kostlan, Mary K. Bennett
Publikováno v:
Journal of Medicinal Chemistry. 35:1605-1609
Purine nucleoside phosphorylase (PNP) is a purine-metabolizing enzyme in the purine cascade and has been a target for drug design for sometime. A series of potent human PNP inhibitors, pyrrolo[3,2-d]pyrimidines (9-deazaguanines), has been synthesized
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9423e1ea24bb1feefd9fcce6fa2238dd
https://doi.org/10.1021/jm00087a015
https://doi.org/10.1021/jm00087a015
Publikováno v:
Journal of Medicinal Chemistry. 35:1451-1457
A series of 3-substituted hypoxanthines (6-10, 14-17) and related analogues (22, 23) have been synthesized as inhibitors of purine nucleoside phosphorylase (PNP), which may conceivably act as T-cell-selective immunosuppressive agents with potential u
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abf030a163c4f004c2413e859ccd4cc2
https://doi.org/10.1021/jm00086a014
https://doi.org/10.1021/jm00086a014
Autor:
M. K. Dong, Richard B. Gilbertsen
Publikováno v:
Agents and Actions. 39:C99-C101
Patients with deficiency in purine nucleoside phosphorylase (PNP) have elevated levels of the PNP substrates inosine, guanosine, and (rarely) 2'-deoxyguanosine (GdR) in their plasma and urine. GdR is critical because it serves as a precursor of dGTP,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2215f2ec9a0543d5aeb2153f0c798a08
https://doi.org/10.1007/bf01972733
https://doi.org/10.1007/bf01972733
Autor:
Eric Auclair, Veronique Fasquelle, Annette M. Doherty, Kam Chan, Stéphane Milano, Emmanuelle Lallier, Bernadette Bertin, Malika Ouagued, Marie-Noelle Rocher, Catherine Burnouf, Christèle Bigot, Brigitte Martin, Roger Wrigglesworth, Marie-Pierre Pruniaux, Richard B. Gilbertsen, Frederic Feru, Jocelyne Puaud, Nadine Avenel, Jacquie Maignel, Yves Pascal, Adel Kebsi, Calvet Alain Pierre, Henry Jacobelli, Christophe Terrasse, Corinne Durand
Publikováno v:
Journal of medicinal chemistry. 43(25)
The synthesis, structure-activity relationships, and biological properties of a novel series of potent and selective phosphodiesterase type 4 (PDE4) inhibitors are described. These new aminodiazepinoindoles displayed in vitro PDE4 activity with submi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e0a99010577cf538d277f8e060d10e
https://pubmed.ncbi.nlm.nih.gov/11123995
https://pubmed.ncbi.nlm.nih.gov/11123995
Publikováno v:
Agents and Actions. 34:53-55
CI-959 (5-methoxy-3-(1-methylethoxy)-N-1H-tetrazol-5-yl-benzo [b]-thiophene-2-carboxamide), an antiallergy compound, blocked release of IL-2 from Con A stimulated rat splenocytes and human lymphocytes with respective IC50s of 19.1 and 23.1 microM. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecd72590b983a7e840d93c1a3e903459
https://doi.org/10.1007/bf01993236
https://doi.org/10.1007/bf01993236