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Akademický článek

GRK Inhibition Potentiates Glucagon-Like Peptide-1 Action

Autor: Seunghun P. Lee, Jenson Qi, Guozhang Xu, Matthew M. Rankin, James Littrell, June Zhi Xu, Ivona Bakaj, Alessandro Pocai

Publikováno v: Frontiers in Endocrinology, Vol 12 (2021)

The glucagon-like peptide-1 receptor (GLP-1R) is a G-protein-coupled receptor (GPCR) whose activation results in suppression of food intake and improvement of glucose metabolism. Several receptor interacting proteins regulate the signaling of GLP-1R

Externí odkaz: https://doaj.org/article/c5c8decb80f8469c94f501e6c8a341ae

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GRK Inhibition Potentiates Glucagon-Like Peptide-1 Action

Autor: June Zhi Xu, James Littrell, Seunghun Paul Lee, Guozhang Xu, Matthew Rankin, Jenson Qi, Ivona Bakaj, Alessandro Pocai

Publikováno v: Frontiers in Endocrinology, Vol 12 (2021)
Frontiers in Endocrinology

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::440f9f5baedcb64f3b7c2909187f7092

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Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor

Autor: Hua-Rong Lu, Ioanna Petrounia, Zhijie Liu, Daniel Jason Krosky, Devine Zheng Huang, Guozhang Xu, John Spurlino, Michael David Gaul, Weixue Wang, An Hermans, June Zhi Xu, Cynthia M. Milligan, Jenson Qi, Renee L. DesJarlais

Publikováno v: Bioorganicmedicinal chemistry letters. 30(23)

G-protein coupled receptor kinase 2 (GRK2), which is upregulated in the failing heart, appears to play a critical role in heart failure (HF) progression in part because enhanced GRK2 activity promotes dysfunction of β-adrenergic signaling and myocyt

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b52110a2ca5137d576a970f201881f77
https://pubmed.ncbi.nlm.nih.gov/33038544

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5,5-Difluoro- and 5-Fluoro-5-methyl-hexose-based C-Glucosides as potent and orally bioavailable SGLT1 and SGLT2 dual inhibitors

Autor: Fuyong Du, Gee-Hong Kuo, Yin Liang, Guozhang Xu, Michael David Gaul, Keith T. Demarest, June Zhi Xu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 30:127387

(2S,3R,4R,5S,6R)-2-Aryl-5,5-difluoro-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diols and (2S,3R,4R,5S,6R)-2-aryl-5-fluoro-5-methyl-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diols were discovered as dual inhibitors of sodium glucose co-transporter prote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e14d3ba29a79979b3a7899ecbf00c8b
https://doi.org/10.1016/j.bmcl.2020.127387

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Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors

Autor: Simon A. Hinke, Jose Silva, Guozhang Xu, Michael David Gaul, Seunghun Paul Lee, William V. Murray, Norman D. Huebert, Thomas Kirchner, Gee-Hong Kuo, Fuyong Du, Keith T. Demarest, June Zhi Xu, Yin Liang, Nathaniel H. Wallace

Publikováno v: Bioorganicmedicinal chemistry letters. 28(21)

A new series of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as dual inhibitors of sodium glucose co-transporter proteins (SGLTs) were disclosed. Two methods were developed to efficiently synthesize C5-fluoro-lacton

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3b1facca7dd2a8982bfbb262f059233
https://pubmed.ncbi.nlm.nih.gov/30268701

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