Zobrazeno 1 - 10
of 36
pro vyhledávání: '"David J Sweeny"'
Autor:
Simon J. Shaw, Dane A. Goff, David C. Carroll, Rajinder Singh, David J. Sweeny, Gary Park, Yonchu Jenkins, Vadim Markovtsov, Tian-Qiang Sun, Sarkiz D. Issakani, Yasumichi Hitoshi, Donald G. Payan
Publikováno v:
Bioorganicmedicinal chemistry. 71
Using an in-cell AMPK activation assay, we have developed structure-activity relationships around a hit pyridine dicarboxamide 5 that resulted in 40 (R419). A particular focus was to retain the on-target potency while also improving microsomal stabil
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f03c4a77facd19ad502468c47cae4910
https://pubmed.ncbi.nlm.nih.gov/35973281
https://pubmed.ncbi.nlm.nih.gov/35973281
Autor:
Yonchu Jenkins, Tian-Qiang Sun, Vadim Markovtsov, Marc Foretz, Wei Li, Henry Nguyen, Yingwu Li, Alison Pan, Gerald Uy, Lisa Gross, Kristen Baltgalvis, Stephanie L Yung, Tarikere Gururaja, Taisei Kinoshita, Alexander Owyang, Ira J Smith, Kelly McCaughey, Kathy White, Guillermo Godinez, Raniel Alcantara, Carmen Choy, Hong Ren, Rachel Basile, David J Sweeny, Xiang Xu, Sarkiz D Issakani, David C Carroll, Dane A Goff, Simon J Shaw, Rajinder Singh, Laszlo G Boros, Marc-André Laplante, Bruno Marcotte, Rita Kohen, Benoit Viollet, André Marette, Donald G Payan, Todd M Kinsella, Yasumichi Hitoshi
Publikováno v:
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein kinase (AMPK). Activation of AMPK results in the mobilization of nutrient uptake and cataboli
Externí odkaz:
https://doaj.org/article/9f3bbe0f39b0498d932c53dbf27c0985
Autor:
David J. Sweeny, Robert B. Diasio
Publikováno v:
Hepatotoxicology
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::90179610dc8aaf7f0ac9f916779e3c6a
https://doi.org/10.1201/9780367812041-6
https://doi.org/10.1201/9780367812041-6
Autor:
Stuart Oliver, David Millson, Paul D. Martin, Philip T. Leese, Michael Gillen, Dominic Surry, Clive Brealey, David Lau, David J. Sweeny
Publikováno v:
Clinical Pharmacology in Drug Development. 5:170-179
Fostamatinib is a prodrug that undergoes gastrointestinal tract dephosphorylation to form the active metabolite, R406. Here we report its cytochrome P450-inducing potential. In vitro, R406 3 and 10 μM induced CYP2C8 to levels representing 53% and 75
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::351e92f4de8689a4ec9b21b7dd42b8ef
https://doi.org/10.1002/cpdd.243
https://doi.org/10.1002/cpdd.243
Autor:
Paul D. Martin, Clive Brealey, Tim Mant, David J. Sweeny, Kelli Craven, Elliott B. Grossbard, Stuart Oliver, David Millson, Muhammad Baluom, David Lau, Michael Gillen
Publikováno v:
Drugs in R&D
Background Fostamatinib (R788) is a spleen tyrosine kinase (SYK) inhibitor. The active metabolite of fostamatinib, R406, is primarily metabolized by CYP3A4. Objectives The aim of this study was to characterize hepatic microsomal metabolism of R406 an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::500247c9fefb954306521b3088336334
https://pubmed.ncbi.nlm.nih.gov/26739683
https://pubmed.ncbi.nlm.nih.gov/26739683
Autor:
Jeffrey Clough, Elliott B. Grossbard, Gary Park, David Lau, Somasekhar Bhamidipati, Weiqun Li, Rajinder Singh, Muhammad Baluom, David J. Sweeny
Publikováno v:
Drug Metabolism and Disposition. 38:1166-1176
The metabolism of the spleen tyrosine kinase inhibitor N4-(2,2-dimethyl-3-oxo-4-pyrid[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethyoxyphenyl)-2,4-pyrimidinediamine (R406) and its oral prodrug N4-(2,2-dimethyl-4-[(dihydrogenphosphonoxy)methyl]-3-oxo-5-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10f17de5a50d548212e2c06ef6191f1a
https://doi.org/10.1124/dmd.110.032151
https://doi.org/10.1124/dmd.110.032151
Autor:
Arvinder Sran, Kunbin Qu, Sambaiah Thota, David L. Carroll, Sacha Holland, Tarikere Gururaja, Christian Franci, Vanessa Taylor, D. Wayne Lang, Yonchu Jenkins, Rajinder Singh, George Clemens, Muhammad Baluom, Caroline M. R. Low, Elliott B. Grossbard, Steve Wong, Taisei Kinoshita, Donald G. Payan, Joe Lasaga, John R. McLaughlin, Ankush Argade, Angela Romane, Yanhong Zhu, Betty Chang, David J. Sweeny, Hui Li, Weiduan Xu, Yasumichi Hitoshi, Manjeet Parmer, Polly Pine, Vadim Markovtsov, Feifei Zhao, Erlina Pali, Marina Gelman
Publikováno v:
Journal of Cancer Research and Clinical Oncology. 136:99-113
Aurora kinases play a key role in mitotic progression. Over-expression of Aurora kinases is found in several human cancers and correlated with histological malignancy and clinical outcomes. Therefore, Aurora kinase inhibitors should be useful in the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab479d6b26786855ba421ed04ab73684
https://doi.org/10.1007/s00432-009-0641-1
https://doi.org/10.1007/s00432-009-0641-1
Autor:
Ellen Y. Wu, Qingling Zhang, Juthamas Sukbuntherng, William Speed, Joshua Ö. Haznedar, Shem Patyna, Geoffrey Peng, David J. Sweeny, Carlo L. Bello, Xiaoming Yu, Lida Antonian
Publikováno v:
Cancer Chemotherapy and Pharmacology. 64:691-706
The purpose of these extensive non-clinical studies was to assess pharmacokinetics and dispositional properties of sunitinib and its primary active metabolite (SU12662). Sunitinib was administered in single and repeat oral doses in mice, rats, and mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::984caf182fb27ef2932580d6dec97de9
https://doi.org/10.1007/s00280-008-0917-1
https://doi.org/10.1007/s00280-008-0917-1
Autor:
Andrew Parkinson, Juthamas Sukbuntherng, Christine Ye, Brian W. Ogilvie, Simon Wong, Weiwei Tan, David J. Sweeny, Lida Antonian, Qingling Zhang, Ajay Madan
Publikováno v:
Toxicology in Vitro. 20:154-162
SU5416, 3-(3,5-dimethyl-1H-pyrrol-2-ylmethylene)-1,3-dihydro-indol-2-one, is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase, Flk-1/KDR (fetal liver kinase 1/kinase insert domain-containing receptor), also kno
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ffce88deeea348be95b39b53465518c
https://doi.org/10.1016/j.tiv.2005.06.047
https://doi.org/10.1016/j.tiv.2005.06.047
Autor:
Rajinder Singh, Yonchu Jenkins, Rita Kohen, Gerald Uy, Rachel Basile, Benoit Viollet, Bruno Marcotte, Kristen A. Baltgalvis, Ira J. Smith, Yasumichi Hitoshi, Alexander Owyang, Wei Li, Vadim Markovtsov, Dane Goff, Marc Foretz, David C. Carroll, André Marette, Raniel Alcantara, Carmen Choy, Laszlo G. Boros, Guillermo Godinez, Xiang Xu, Kelly McCaughey, Alison Pan, Tarikere Gururaja, Lisa Gross, Yingwu Li, Kathy White, Todd Kinsella, Donald G. Payan, Hong Ren, Tian-Qiang Sun, Henry Nguyen, Taisei Kinoshita, Simon J. Shaw, Stephanie Yung, David J. Sweeny, Sarkiz D. Issakani, Marc-André Laplante
Publikováno v:
PLoS ONE
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein kinase (AMPK). Activation of AMPK results in the mobilization of nutrient uptake and cataboli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6faef8a70dbbaaa3babac84c0b20d1d4
http://europepmc.org/articles/PMC3855387
http://europepmc.org/articles/PMC3855387