Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Aditya J. Desai"'
Autor:
Kaleeckal G. Harikumar, Thomas Coudrat, Aditya J. Desai, Maoqing Dong, Daniela G. Dengler, Sebastian G. B. Furness, Arthur Christopoulos, Denise Wootten, Eduard A. Sergienko, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Frontiers in Endocrinology, Vol 12 (2021)
Drugs useful in prevention/treatment of obesity could improve health. Cholecystokinin (CCK) is a key regulator of appetite, working through the type 1 CCK receptor (CCK1R); however, full agonists have not stimulated more weight loss than dieting. We
Externí odkaz:
https://doaj.org/article/895703c860ab400c964a97eea810e55b
Autor:
Kaleeckal G Harikumar, Peishen Zhao, Brian P Cary, Xiaomeng Xu, Aditya J Desai, Maoqing Dong, Jesse I Mobbs, Chirine Toufaily, Sebastian G B Furness, Arthur Christopoulos, Matthew J Belousoff, Denise Wootten, Patrick M Sexton, Laurence J Miller
Publikováno v:
PLoS Biology, Vol 22, Iss 7, p e3002673 (2024)
Development of optimal therapeutics for disease states that can be associated with increased membrane cholesterol requires better molecular understanding of lipid modulation of the drug target. Type 1 cholecystokinin receptor (CCK1R) agonist actions
Externí odkaz:
https://doaj.org/article/897ba52f46f9422aa4eba66be6e9d3a4
Publikováno v:
Journal of Nuclear Medicine Technology. 48:40-45
Cholecystokinin cholescintigraphy is used clinically to quantify gallbladder ejection fraction as an indicator of functional gallbladder disorder. It can also provide the opportunity to quantify an individual's responsiveness to the physiologic stimu
Autor:
Denise Wootten, Patrick M. Sexton, Laurence J. Miller, Ingrid Mechin, Anil Nair, Andrew Orry, Ruben Abagyan, Karthigeyan Nagarajan, Polo C.-H. Lam, Aditya J. Desai, Celine Valant, Arthur Christopoulos
Publikováno v:
Molecular Pharmacology. 95:245-259
Allosteric modulation of receptors provides mechanistic safety while effectively achieving biologic endpoints otherwise difficult or impossible to obtain by other means. The theoretical case has been made for the development of a positive allosteric
Autor:
Aditya J Desai, Laurence J Miller
Publikováno v:
Frontiers in Endocrinology, Vol 3 (2012)
Cholesterol represents a structurally and functionally important component of the eukaryotic cell membrane, where it increases lipid order, affects permeability, and influences the lateral mobility and conformation of membrane proteins. Several G pro
Externí odkaz:
https://doaj.org/article/933989d5da264da5a28d1dbd95f7a6a7
Autor:
Laurence J. Miller, Aditya J. Desai
Publikováno v:
British Journal of Pharmacology. 175:4009-4025
Drug development targeting GPCRs often utilizes model heterologous cell expression systems, reflecting an implicit assumption that the membrane environment has little functional impact on these receptors or on their responsiveness to drugs. However,
Publikováno v:
The American Journal of Clinical Nutrition. 106:447-456
Background: Cholecystokinin (CCK) is an important satiety factor, acting at type 1 receptors (CCK1Rs) on vagal afferent neurons; however, CCK agonists have failed clinical trials for obesity. We postulated that CCK1R function might be defective in su
Publikováno v:
Clinical Nutrition. 35:1374-1379
The type 1 cholecystokinin receptor (CCK1R) mediates the actions of CCK to support nutritional homeostasis, including post-cibal satiety. However, elevated levels of membrane cholesterol, such as have been observed in metabolic syndrome, interfere wi
Publikováno v:
International Journal of Obesity Supplements. 6:S22-S27
The gastrointestinal (GI) tract has a central role in nutritional homeostasis, as location for food ingestion, digestion and absorption, with the gut endocrine system responding to and regulating these events, as well as influencing appetite. One key
Autor:
Laurence J. Miller, Aditya J. Desai
Publikováno v:
Trends in Endocrinology & Metabolism. 27:609-619
Cholecystokinin (CCK) regulates appetite and reduces food intake by activating the type 1 CCK receptor (CCK1R). Attempts to develop CCK1R agonists for obesity have yielded active agents that have not reached clinical practice. Here we discuss why, al