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1. Pan AMPK Activation Protects Tubules in Rat Ischemic Acute Kidney Injury

Author

Frikke-Schmidt, Henriette, primary, Albarazanji, Kamal, additional, Qi, Jenson, additional, Frederick, David, additional, Steffen, Janos, additional, Kalyana-Sundaram, Shanker, additional, Meng, Rong, additional, Devine, Zheng Huang, additional, Chen, Tao, additional, Li, Qiu, additional, Du, Fuyong, additional, Ho, George, additional, Liu, Jianying, additional, Riley, Roseann, additional, Gonzalez-Villalobos, Romer A, additional, Camacho, Raul C, additional, Nawrocki, Andrea R, additional, Pryor, Meghan, additional, Lee, Min, additional, Wong, Victoria, additional, Matico, Rosalie, additional, Diaz, Elsie, additional, Krosky, Daniel, additional, Wall, Mark, additional, Gao, Elise, additional, Shah, Akshay A, additional, Leonard, James, additional, Erion, Mark, additional, Pocai, Alessandro, additional, and Player, Mark R, additional

Published
2024
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7. Urotensin II is a nitric oxide-dependent vasodilator and natriuretic peptide in the rat kidney

Author

Zhang, Andrew Y., Chen, Ya-Fei, Zhang, David X., Yi, Fu-Xian, Qi, Jenson, Andrade-Gordon, Patricia, de Garavilla, Lawrence, Li, Pin-Lan, and Zou, Al-Ping

Subjects
Hemodynamics -- Research, Nitric oxide -- Research, Biological sciences
Abstract

Recent studies have indicated that urotensin II (UII), a cyclic peptide, is vasoactive and may be involved in cardiovascular dysfunctions. It remains unknown, however, whether UII plays a role in the control of renal vascular tone and tubular function. In the present study, a continuous infusion of synthetic human UII (hUII) into the renal artery (RA) in anesthetized rats was found to increase renal blood flow (RBF) and urinary water and sodium excretion (UV and [U.sub.Na.]V) in a dose-dependent manner. At a dose of 20 ng*[kg.sup.-1]. [min.sup.-1], it increased RBF by 20% and UV and [U.sub.Na]V by 94 and 109%, respectively. Nitric oxide (NO) synthase inhibitor [N.sup.G]-nitro-L-arginine methyl ester (L-NAME) completely abolished hUII-induced increases in RBF and water/sodium excretion. In isolated, pressurized, and phenylephrine-precontracted small RA with internal diameter of ~200 [micro]m, hUII produced a concentration-dependent vasodilation with a maximal response of 55% at 1.5 [micro]M. L-NAME significantly blocked this hUII-induced vasodilation by 60%. In denuded RA, hUII had neither vasodilator nor vasoconstrictor effect. With the use of 4,5-diaminofluorescein diacetate-based fluorescence imaging analysis of NO levels, hUII (1 [micro]M) was shown to double the NO levels within the endothelium of freshly dissected small RA, and L-NAME blocked this UII-induced production of endothelial NO. These results indicate that UII produces vasodilator and natriuretic effects in the kidney and that UII-induced vasodilation is associated with increased endothelial NO in the RA. natriuretic factor; renal circulation; sodium reabsorption; renal tubule; renal hemodynamics

Published
2003

10. Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination

Author

Huang, Hui, primary, Meegalla, Sanath K., additional, Lanter, James C., additional, Winters, Michael P., additional, Zhao, Shuyuan, additional, Littrell, James, additional, Qi, Jenson, additional, Rady, Brian, additional, Lee, Paul S., additional, Liu, Jianying, additional, Martin, Tonya, additional, Lam, Wing W., additional, Xu, Fran, additional, Lim, Heng Keang, additional, Wilde, Thomas, additional, Silva, Jose, additional, Otieno, Monicah, additional, Pocai, Alessandro, additional, and Player, Mark R., additional

Published
2018
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11. 6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity

Author

Zhang, Yue-Mei, primary, Greco, Michael N., additional, Macielag, Mark J., additional, Teleha, Christopher A., additional, DesJarlais, Renee L., additional, Tang, Yuting, additional, Ho, George, additional, Hou, Cuifen, additional, Chen, Cailin, additional, Zhao, Shuyuan, additional, Kauffman, Jack, additional, Camacho, Raul, additional, Qi, Jenson, additional, Murray, William, additional, Demarest, Keith, additional, and Leonard, James, additional

Published
2018
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12. FFAR1 Agonism Restores Insulin Secretion in Rodents, Human Islets, and Diabetic Monkeys

Author

LIU, JIANYING, primary, LEE, SEUNGHUN P., additional, MARTIN, TONYA, additional, RADY, BRIAN, additional, MEEGALLA, SANATH, additional, HUANG, HUI, additional, WINTERS, MICHAEL P., additional, NORQUAY, LISA D., additional, QI, JENSON, additional, DU, FUYONG, additional, NAWROCKI, ANDREA R., additional, PLAYER, MARK, additional, and POCAI, ALESSANDRO, additional

Published
2018
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13. GPR40-Mediated Gα12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets

Author

Rives, Marie-Laure, primary, Rady, Brian, additional, Swanson, Nadia, additional, Zhao, Shuyuan, additional, Qi, Jenson, additional, Arnoult, Eric, additional, Bakaj, Ivona, additional, Mancini, Arturo, additional, Breton, Billy, additional, Lee, S. Paul, additional, Player, Mark R., additional, and Pocai, Alessandro, additional

Published
2018
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17. Analysis of the Effect of Canagliflozin on Renal Glucose Reabsorption and Progression of Hyperglycemia in Zucker Diabetic Fatty Rats

Author

Kuriyama, Chiaki, primary, Xu, Jun Zhi, additional, Lee, Seunghun Paul, additional, Qi, Jenson, additional, Kimata, Hirotaka, additional, Kakimoto, Tetsuhiro, additional, Nakayama, Keiko, additional, Watanabe, Yoshinori, additional, Taniuchi, Nobuhiko, additional, Hikida, Kumiko, additional, Matsushita, Yasuaki, additional, Arakawa, Kenji, additional, Saito, Akira, additional, Ueta, Kiichiro, additional, and Shiotani, Masaharu, additional

Published
2014
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20. The use of stable isotope-labeled glycerol and oleic acid to differentiate the hepatic functions of DGAT1 and -2

Author

Qi, Jenson, primary, Lang, Wensheng, additional, Geisler, John G., additional, Wang, Ping, additional, Petrounia, Ioanna, additional, Mai, Selyna, additional, Smith, Charles, additional, Askari, Hossein, additional, Struble, Geoffrey T., additional, Williams, Robyn, additional, Bhanot, Sanjay, additional, Monia, Brett P., additional, Bayoumy, Shariff, additional, Grant, Eugene, additional, Caldwell, Gary W., additional, Todd, Matthew J., additional, Liang, Yin, additional, Gaul, Micheal D., additional, Demarest, Keith T., additional, and Connelly, Margery A., additional

Published
2012
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21. High-content assays for evaluating cellular and hepatic diacylglycerol acyltransferase activity

Author

Qi, Jenson, primary, Lang, Wensheng, additional, Giardino, Edward, additional, Caldwell, Gary W., additional, Smith, Charles, additional, Minor, Lisa K., additional, Darrow, Andrew L., additional, Willemsens, Gustaaf, additional, DeWaepenaert, Katharina, additional, Roevens, Peter, additional, Linders, Joannes T.M., additional, Liang, Yin, additional, and Connelly, Margery A., additional

Published
2010
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22. Nonpeptide Urotensin-II Receptor Antagonists: A New Ligand Class Based on Piperazino-Phthalimide and Piperazino-Isoindolinone Subunits

Author

Lawson, Edward C., primary, Luci, Diane K., additional, Ghosh, Shyamali, additional, Kinney, William A., additional, Reynolds, Charles H., additional, Qi, Jenson, additional, Smith, Charles E., additional, Wang, Yuanping, additional, Minor, Lisa K., additional, Haertlein, Barbara J., additional, Parry, Tom J., additional, Damiano, Bruce P., additional, and Maryanoff, Bruce E., additional

Published
2009
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25. The Nucleotide-binding Site of Human Sphingosine Kinase 1

Author

Pitson, Stuart M., primary, Moretti, Paul A.B., additional, Zebol, Julia R., additional, Zareie, Reza, additional, Derian, Claudia K., additional, Darrow, Andrew L., additional, Qi, Jenson, additional, D'Andrea, Richard J., additional, Bagley, Christopher J., additional, Vadas, Mathew A., additional, and Wattenberg, Binks W., additional

Published
2002
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26. Structure–Function Analysis of Urotensin II and Its Use in the Construction of a Ligand–Receptor Working Model

Author

Kinney, William A., primary, Almond, Jr., Harold R., additional, Qi, Jenson, additional, Smith, Charles E., additional, Santulli, Rosemary J., additional, de Garavilla, Lawrence, additional, Andrade-Gordon, Patricia, additional, Cho, Daniel S., additional, Everson, Anita M., additional, Feinstein, Mark A., additional, Leung, Perry A., additional, and Maryanoff, Bruce E., additional

Published
2002
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28. 6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB 1 ) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity.

Author

Zhang YM, Greco MN, Macielag MJ, Teleha CA, DesJarlais RL, Tang Y, Ho G, Hou C, Chen C, Zhao S, Kauffman J, Camacho R, Qi J, Murray W, Demarest K, and Leonard J

Subjects
Animals, Humans, Male, Mice, Mice, Inbred C57BL, Models, Molecular, Protein Conformation, Quinolones metabolism, Quinolones pharmacokinetics, Rats, Receptor, Cannabinoid, CB1 chemistry, Receptor, Cannabinoid, CB1 metabolism, Structure-Activity Relationship, Tissue Distribution, Drug Inverse Agonism, Quinolones chemistry, Quinolones pharmacology, Receptor, Cannabinoid, CB1 agonists
Abstract

A novel series of 6-benzhydryl-4-amino-quinolin-2-ones was discovered as cannabinoid type 1 receptor (CB 1 R) inverse agonists based on the high-throughput screening hit, compound 1a. Structure-activity relationships were studied to improve in vitro/in vivo pharmacology and restrict distribution to the peripheral circulation. We adopted several strategies such as increasing topological polar surface area, incorporating discrete polyethylene glycol side chains, and targeting P-glycoprotein (P-gp) to minimize access to the brain. Compound 6a is a P-gp substrate and a potent and highly selective CB 1 R inverse agonist, demonstrating excellent in vivo metabolic stability and a low brain to plasma ratio. However, brain receptor occupancy studies showed that compound 6a may accumulate in brain with repeat dosing. This was evidenced by compound 6a inhibiting food intake and inducing weight loss in diet-induced obese mice. Thus, a strategy based on P-gp efflux may not be adequate for peripheral restriction of the disclosed quinolinone series.

Published
2018
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29. GPR40-Mediated G α 12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets.

Author

Rives ML, Rady B, Swanson N, Zhao S, Qi J, Arnoult E, Bakaj I, Mancini A, Breton B, Lee SP, Player MR, and Pocai A

Subjects
Animals, Benzofurans pharmacology, CHO Cells, Cell Line, Cricetulus, HEK293 Cells, Humans, Hypoglycemic Agents pharmacology, Insulin Secretion drug effects, Islets of Langerhans drug effects, Protein Kinase C metabolism, Signal Transduction drug effects, Signal Transduction physiology, Sulfones pharmacology, GTP-Binding Protein alpha Subunits, G12-G13 metabolism, Glucose metabolism, Insulin metabolism, Insulin Secretion physiology, Islets of Langerhans metabolism, Receptors, G-Protein-Coupled metabolism
Abstract

GPR40 is a clinically validated molecular target for the treatment of diabetes. Many GPR40 agonists have been identified to date, with the partial agonist fasiglifam (TAK-875) reaching phase III clinical trials before its development was terminated due to off-target liver toxicity. Since then, attention has shifted toward the development of full agonists that exhibit superior efficacy in preclinical models. Full agonists bind to a distinct binding site, suggesting conformational plasticity and a potential for biased agonism. Indeed, it has been suggested that alternative pharmacology may be required for meaningful efficacy. In this study, we described the discovery and characterization of Compound A, a newly identified GPR40 allosteric full agonist highly efficacious in human islets at potentiating glucose-stimulated insulin secretion. We compared Compound A-induced GPR40 activity to that induced by both fasiglifam and AM-1638, another allosteric full agonist previously reported to be highly efficacious in preclinical models, at a panel of G proteins. Compound A was a full agonist at both the G α q and G α i2 pathways, and in contrast to fasiglifam Compound A also induced G α 12 coupling. Compound A and AM-1638 displayed similar activity at all pathways tested. The G α 12 /G α 13 -mediated signaling pathway has been linked to protein kinase D activation as well as actin remodeling, well known to contribute to the release of insulin vesicles. Our data suggest that the pharmacology of GPR40 is complex and that G α 12/G α 13-mediated signaling, which may contribute to GPR40 agonists therapeutic efficacy, is a specific property of GPR40 allosteric full agonists., Competing Interests: The authors declare no conflict of interest., (Copyright © 2018 by The American Society for Pharmacology and Experimental Therapeutics.)

Published
2018
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30. Structure-function analysis of urotensin II and its use in the construction of a ligand-receptor working model.

Author

Kinney WA, Almond HR Jr, Qi J, Smith CE, Santulli RJ, de Garavilla L, Andrade-Gordon P, Cho DS, Everson AM, Feinstein MA, Leung PA, and Maryanoff BE

Subjects
Amino Acid Sequence, Animals, Drug Design, Humans, Ligands, Models, Molecular, Peptide Fragments chemistry, Peptide Fragments metabolism, Protein Conformation, Receptors, Cell Surface metabolism, Urotensins agonists, Urotensins metabolism, Receptors, Cell Surface chemistry, Receptors, G-Protein-Coupled, Urotensins chemistry, Vasoconstrictor Agents chemistry
Published
2002
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