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Eric Garver
Researcher at GlaxoSmithKline
Publications - 6
Citations - 453
Eric Garver is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Ex vivo & Glucuronidation. The author has an hindex of 4, co-authored 6 publications receiving 402 citations.
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Journal ArticleDOI
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Juan I. Luengo,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Melody Diamond,Patricia A. Elkins,Christine M. Gardiner,Eric Garver,Seth A. Gilbert,Richard R. Gontarek,Jeffrey R. Jackson,Kevin L. Kershner,Lusong Luo,Kaushik Raha,Christian S. Sherk,Chiu-Mei Sung,David Sutton,Peter J. Tummino,Ronald Wegrzyn,Kurt R. Auger,Dashyant Dhanak +30 more
TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
Journal ArticleDOI
Interaction of macrolide antibiotics with intestinally expressed human and rat organic anion-transporting polypeptides.
TL;DR: Investigation of the interaction of macrolides with rat Oatp1a5, human OATp1A2, and human/rat OATP2B1/Oatp2b1 shows that intestinally expressed OatP/OATp(s) are not responsible for the postulated facilitative uptake of azithromycin and clarithromyc, and alternative facilitative pathways must exist for their intestinal absorption.
Journal ArticleDOI
Involvement of Intestinal Uptake Transporters in the Absorption of Azithromycin and Clarithromycin in the Rat
Eric Garver,Erin D. Hugger,Shawn P. Shearn,Anuradha Rao,Paul A. Dawson,Charles B. Davis,Chao Han +6 more
TL;DR: In vitro and in vivo results suggest that the intestinal Oatps are involved in the p.o. absorption of AZI and CLARI in the rat, and inhibition of an RIF-sensitive uptake transporter such as Oatp along the rat gastrointestinal tract was responsible for reduced p.oing.
Journal ArticleDOI
Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea
Jerry L. Adams,Ravi Shanker Garigipati,Margaret E. Sorenson,Schmidt Stanley J,William Brian,J F Newton,Kathy A. Tyrrell,Eric Garver,Lee Ann P. Yodis,Marie Chabot-Fletcher,M. N. Tzimas,Edward F. Webb,John J. Breton,Don E. Griswold +13 more
TL;DR: In vitro metabolic studies in mouse liver microsomes established enantiospecific glucuronidation as a likely mechanism for the observed differences between the enantiomers of 1a and (-)-1a.
Proceedings ArticleDOI
Abstract C62: Identification of GSK2126458, a highly potent inhibitor of phosphoinositide 3‐kinase (PI3K) and the mammalian target of rapamycin (mTOR)
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Patricia A. Elkins,Melody Diamond,Christine M. Gardiner,Eric Garver,Lusong Luo,Kaushik Raha,Chiu-Mei Sung,Peter J. Tummino,Kurt R. Auger,Dashyant Dhanak +22 more
TL;DR: Following a chemistry lead optimization effort, the pyridylsulfonamide GSK2126458 was identified as a highly potent, orally bioavailable, pan‐PI3K and mTOR inhibitor and is being evaluated currently in human clinical trials for the treatment of cancer.