Zobrazeno 1 - 10 of 83 pro vyhledávání: '"Paul G, Pearson"'
1
Akademický článek
Comparative pharmacokinetics and pharmacodynamics of the advanced Retinol-Binding Protein 4 antagonist in dog and cynomolgus monkey.
Autor: Boglarka Racz, Andras Varadi, Paul G Pearson, Konstantin Petrukhin
Publikováno v: PLoS ONE, Vol 15, Iss 1, p e0228291 (2020)
Accumulation of lipofuscin bisretinoids in the retina contributes to pathogenesis of macular degeneration. Retinol-Binding Protein 4 (RBP4) antagonists reduce serum retinol concentrations thus partially reducing retinol delivery to the retina which d
Externí odkaz: https://doaj.org/article/ae0d4bbb4c2f45a2bbeaccc247c1b2af
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2
Akademický článek
ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing’s syndrome
Autor: Daniel K. Langlois, Michele C. Fritz, William D. Schall, N. Bari Olivier, Rebecca C. Smedley, Paul G. Pearson, Marc B. Bailie, Stephen W. Hunt
Publikováno v: BMC Endocrine Disorders, Vol 18, Iss 1, Pp 1-12 (2018)
Abstract Background Cushing’s syndrome in humans shares many similarities with its counterpart in dogs in terms of etiology (pituitary versus adrenal causes), clinical signs, and pathophysiologic sequelae. In both species, treatment of pituitary- a
Externí odkaz: https://doaj.org/article/dc53bfc541ef499c9c915512f2cebf1b
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3
Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors
Autor: Terry, Podoll, Paul G, Pearson, Allard, Kaptein, Jerry, Evarts, Gerjan, de Bruin, Maaike, Emmelot-van Hoek, Anouk, de Jong, Bart, van Lith, Hao, Sun, Stephen, Byard, Adrian, Fretland, Niels, Hoogenboom, Tjeerd, Barf, J Greg, Slatter
Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 384:173-186
Acalabrutinib is a covalent Bruton tyrosine kinase (BTK) inhibitor approved for relapsed/refractory mantle cell lymphoma and chronic lymphocytic leukemia/small lymphocytic lymphoma. A major metabolite of acalabrutinib (M27, ACP-5862) was observed in
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5b51ca94d968a8dbd551ff1f2f6f4a3
https://doi.org/10.1124/jpet.122.001116
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4
Abstract 3332: LNG-451 is a potent, CNS-penetrant, wild-type EGFR sparing inhibitor of EGFR exon 20 insertion mutations
Autor: Brion W. Murray, Anjali Pandey, Bruce Roth, Tracy Saxton, Daniel J. Estes, Himanshu Agrawal, Santosh Vishwakarma, Gurulingappa Hallur, Ishtiyaque Ahmad, Ravi Trivedi, Helen Jenkins, Paul G. Pearson
Publikováno v: Cancer Research. 82:3332-3332
Exon 20 insertion mutations (Ex20ins) are the third most common type of EGFR oncogenic mutation in lung cancer patients. While several small molecules have been approved (mobocertinib) or are in clinical development (e.g. CLN-081, BDTX-189) none have
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3c98fba1e1834e4220525f131f5f82db
https://doi.org/10.1158/1538-7445.am2022-3332
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5
Abstract 3261: LNG-451, a potent inhibitor of EGFR exon 20 insertion mutations with high CNS exposure
Autor: Paul G. Pearson, Anjali Pandey, Bruce Roth, Tracy Saxton, Daniel J. Estes, Ravi Trivedi, Himanshu Agrawal, Gurulingappa Hallur, Ishtiyaque Ahmad, Helen Jenkins, Brion W. Murray
Publikováno v: Cancer Research. 82:3261-3261
Exon 20 insertion mutations (Ex20ins) are the 3rd most common type of EGFR oncogenic mutation in lung cancer patients and are often associated with brain metastases. While several small molecules have been approved (mobocertinib) or are in clinical d
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4554fcb2ad8096165b4f8e4ac43d1dd8
https://doi.org/10.1158/1538-7445.am2022-3261
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6
Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans
Autor: Mark Gohdes, J. Greg Slatter, Tim Ingallinera, Hao Sun, Paul G. Pearson, Jerry Evarts, Terry Podoll, Mitesh Sanghvi, Elena Bibikova, Kristen Cardinal
Publikováno v: Drug Metabolism and Disposition. 47:145-154
Acalabrutinib is a targeted, covalent inhibitor of Bruton tyrosine kinase (BTK) with a unique 2-butynamide warhead that has relatively lower reactivity than other marketed acrylamide covalent inhibitors. A human [14C] microtracer bioavailability stud
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecdd79c4d40f1d5137e0bc6c0ef781ad
https://doi.org/10.1124/dmd.118.084459
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7
A non-retinoid antagonist of retinol-binding protein 4 rescues phenotype in a model of Stargardt disease without inhibiting the visual cycle
Autor: Christopher L. Cioffi, Jian Kong, Graham Johnson, Boglarka Racz, Konstantin Petrukhin, Rando Allikmets, András Váradi, Paul G. Pearson
Publikováno v: Journal of Biological Chemistry. 293:11574-11588
A primary pathological defect in the heritable eye disorder Stargardt disease is excessive accumulation of cytotoxic lipofuscin bisretinoids in the retina. Age-dependent accumulation of lipofuscin in the retinal pigment epithelium (RPE) matches the a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b3cdddde753c6d4b00c50ff582061de
https://doi.org/10.1074/jbc.ra118.002062
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8
ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing’s syndrome
Autor: Rebecca C. Smedley, Michele C. Fritz, Daniel K. Langlois, Marc Bailie, Stephen Hunt, N. Bari Olivier, Paul G. Pearson, W. D. Schall
Publikováno v: BMC Endocrine Disorders, Vol 18, Iss 1, Pp 1-12 (2018)
BMC Endocrine Disorders
Background Cushing’s syndrome in humans shares many similarities with its counterpart in dogs in terms of etiology (pituitary versus adrenal causes), clinical signs, and pathophysiologic sequelae. In both species, treatment of pituitary- and adrena
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17e6b9986f3728d5ab4df592fd42de48
http://link.springer.com/article/10.1186/s12902-018-0251-5
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10
Elektronická kniha
Handbook of Drug Metabolism, Third Edition
Autor: Paul G. Pearson, Larry C. Wienkers
This book continues to be the definitive reference on drug metabolism with an emphasis on new scientific and regulatory developments. It has been updated based on developments that have occurred in the last 5 years, with new chapters on large molecul
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