Influence of Transporter Polymorphisms on Drug Disposition and Response: A Perspective From the International Transporter Consortium

Autor: Aleksandra Galetin, Deanna J. Brackman, Landry K. Kamdem, Lei Zhang, Kathleen M. Giacomini, Rebecca Blanchard, Elizabeth A. Ennis, Sook Wah Yee, Yuichi Sugiyama

Publikováno v: Yee, S W, Brackman, D J, Ennis, E A, Sugiyama, Y, Kamdem, L K, Blanchard, R, Galetin, A, Zhang, L & Giacomini, K M 2018, ' Influence of Transporter Polymorphisms on Drug Disposition and Response : A Perspective From the International Transporter Consortium ', Clinical Pharmacology and Therapeutics . https://doi.org/10.1002/cpt.1098
Clinical pharmacology and therapeutics, vol 104, iss 5

Advances in genomic technologies have led to a wealth of information identifying genetic polymorphisms in membrane transporters, specifically how these polymorphisms affect drug disposition and response. This review describes the current perspective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fe3505ae50d815f26acf42de958cdf0
https://doi.org/10.1002/cpt.1098

Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound

Autor: Anna L. Blobaum, Jane Wright, Jerri M. Rook, Christopher J. Tarr, Jeanette L. Bertron, Jonathan W. Dickerson, Elizabeth A. Ennis, Charles W. Locuson, Craig W. Lindsley, Randy D. Blakely

Publikováno v: Bioorganicmedicinal chemistry letters. 26(19)

This Letter describes the further lead optimization of the CHT inhibitor probe, ML352 (VU0476201), and the development of VU6001221, an improved in vivo tool. A multi-dimensional optimization effort encountered steep SAR, and ultimately, subtle tunin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38e22c48d72fc37a6a8b33b40b2f1515
https://pubmed.ncbi.nlm.nih.gov/27575469

Nonoisotopic Assay for the Presynaptic Choline Transporter Reveals Capacity for Allosteric Modulation of Choline Uptake

Autor: Hideki Iwamoto, Jane Wright, Randy D. Blakely, Elizabeth A. Ennis, Shawn M. Ferguson, Ericka C. Holmstrand, C. David Weaver, Katie S. Emerson, Alicia M. Ruggiero, Michael T. Ivy, Michelle Lewis

Publikováno v: ACS Chemical Neuroscience. 3:767-781

Current therapies to enhance CNS cholinergic function rely primarily on extracellular acetylcholinesterase (AChE) inhibition, a pharmacotherapeutic strategy that produces dose-limiting side effects. The Na(+)-dependent, high-affinity choline transpor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ee38531e39345a30bb9d1e93fc29f0f
https://doi.org/10.1021/cn3000718

Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter

Autor: Darren W. Engers, Jane Wright, Bollinger Sean R, Corey R. Hopkins, Elizabeth A. Ennis, Charles W. Locuson, Randy D. Blakely, Craig W. Lindsley

Publikováno v: Bioorganicmedicinal chemistry letters. 25(8)

The synthesis and SAR of 4-methoxy-3-(piperidin-4-yl) benzamides identified after a high-throughput screen of the MLPCN library is reported. SAR was explored around the 3-piperidine substituent as well as the amide functionality of the reported compo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::812800eca45c77d393ac5d93e22acbbb
https://pubmed.ncbi.nlm.nih.gov/25801932

Hypercalcemia caused by iatrogenic hypervitaminosis A

Autor: Elizabeth D. Ennis, Karan Bhalla, David M. Ennis

Publikováno v: Journal of the American Dietetic Association. 105(1)

Vitamin A toxicity produces protean clinical manifestations involving a wide variety of tissues and systems. Hypercalcemia can occasionally be associated with high vitamin A levels, but is rare. In this report we describe a patient who was receiving

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6b2d6d03e2befc97e0d66ee38b3fb75
https://pubmed.ncbi.nlm.nih.gov/15635357