Zobrazeno 1 - 10
of 113
pro vyhledávání: '"Kaleeckal G. Harikumar"'
Autor:
Robert Ardecky, Daniela G. Dengler, Kaleeckal G. Harikumar, Mathew M. Abelman, Jiwen Zou, Bryan A. Kramer, Santhi Reddy Ganji, Steve Olson, Alina Ly, Nikhil Puvvula, Chen-Ting Ma, Raghuveer Ramachandra, Eduard A. Sergienko, Laurence J. Miller
Publikováno v:
SLAS Discovery, Vol 29, Iss 6, Pp 100176- (2024)
Agonists of the secretin receptor have potential applications for diseases of the cardiovascular, gastrointestinal, and metabolic systems, yet no clinically-active non-peptidyl agonists of this receptor have yet been developed. In the current work, w
Externí odkaz:
https://doaj.org/article/3eddfc13db42404aa4f87b29244f0ab2
Autor:
Kaleeckal G. Harikumar, Sarah J. Piper, Arthur Christopoulos, Denise Wootten, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-12 (2024)
Abstract Class B G protein-coupled receptors can form dimeric complexes important for high potency biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques to cells and membranes expressing the prototypic secretin r
Externí odkaz:
https://doaj.org/article/03bd6139abd74708a85a68f98f562b73
Autor:
Daniela G. Dengler, Qing Sun, Kaleeckal G. Harikumar, Laurence J. Miller, Eduard A. Sergienko
Publikováno v:
SLAS Discovery, Vol 27, Iss 7, Pp 384-394 (2022)
Obesity has become a prevailing health burden globally and particularly in the US. It is associated with many health problems, including cardiovascular disease, diabetes and poorer mental health. Hence, there is a high demand to find safe and effecti
Externí odkaz:
https://doaj.org/article/422a6a6075cb48808eb30e6c246e9ece
Autor:
Maoqing Dong, Giuseppe Deganutti, Sarah J. Piper, Yi-Lynn Liang, Maryam Khoshouei, Matthew J. Belousoff, Kaleeckal G. Harikumar, Christopher A. Reynolds, Alisa Glukhova, Sebastian G. B. Furness, Arthur Christopoulos, Radostin Danev, Denise Wootten, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-17 (2020)
The class B secretin GPCR (SecR) has broad physiological effects, with target potential for treatment of metabolic and cardiovascular disease. Here, authors present a cryo-EM structure and biochemical studies of secretin binding to the SecR:Gs comple
Externí odkaz:
https://doaj.org/article/35d3a9f45d2f49f5b92ff1e2f30c175a
Autor:
Daniela G. Dengler, Kaleeckal G. Harikumar, Alice Yen, Eduard A. Sergienko, Laurence J. Miller
Publikováno v:
Membranes, Vol 13, Iss 2, p 150 (2023)
As part of an ongoing effort to develop a drug targeting the type 1 cholecystokinin receptor (CCK1R) to help prevent and/or treat obesity, we recently performed a high throughput screening effort of small molecules seeking candidates that enhanced th
Externí odkaz:
https://doaj.org/article/12fce92a66594ac0a74ef2c42448a870
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
Publikováno v:
Frontiers in Endocrinology, Vol 12 (2021)
Cholecystokinin is a gastrointestinal peptide hormone with important roles in metabolic physiology and the maintenance of normal nutritional status, as well as potential roles in the prevention and management of obesity, currently one of the dominant
Externí odkaz:
https://doaj.org/article/de858ba8761e49a7b6412a8eb69243fb
Autor:
Parijat Sarkar, Kaleeckal G. Harikumar, Satinder S. Rawat, Sanjib Das, Tushar K. Chakraborty, Amitabha Chattopadhyay
Publikováno v:
Molecules, Vol 26, Iss 13, p 3848 (2021)
Serotonin is a neurotransmitter that plays a crucial role in the regulation of several behavioral and cognitive functions by binding to a number of different serotonin receptors present on the cell surface. We report here the synthesis and characteri
Externí odkaz:
https://doaj.org/article/4a835f0a39fa4633b16bed90baa89ac2
Publikováno v:
Journal of Lipid Research, Vol 53, Iss 1, Pp 137-148 (2012)
Recent studies indicate that membrane cholesterol can associate with G protein-coupled receptors (GPCRs) and affect their function. Previously, we reported that manipulation of membrane cholesterol affects ligand binding and signal transduction of th
Externí odkaz:
https://doaj.org/article/7f6030f3524045e1bfa9fe6a12b84637
Autor:
Michael D. Holsey, Grant T. Gilmore, Adam W. Smith, Jonathan A. Javitch, Avik Kumar Pati, Kaleeckal G. Harikumar, Zhou Zhou, Jozsef Meszaros, Laurence J. Miller, Khuloud Jaqaman, Peter Geggier, Signe Mathiasen, Wesley B. Asher, Megan J. Kaliszewski, Mitchell D. McCauley, Scott C. Blanchard, Daniel S. Terry, Alekhya Govindaraju
Publikováno v:
Nature Methods. 18:397-405
Class C G protein-coupled receptors (GPCRs) are known to form stable homodimers or heterodimers critical for function, but the oligomeric status of class A and B receptors, which constitute >90% of all GPCRs, remains hotly debated. Single-molecule fl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5b1d5af5024e5772f7bfbd0e90f26b66
https://doi.org/10.1038/s41592-021-01081-y
https://doi.org/10.1038/s41592-021-01081-y