Výsledky vyhledávání - "Sarat Kumar, Sarvasiddhi"

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain

Publikováno v: Journal of Medicinal Chemistry. 65:4534-4564

Recent mouse knockout studies identified adapter protein-2-associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. BMS-986176/LX-9211 (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbf11be6e3846cab6b37f029b5b93a8d
https://doi.org/10.1021/acs.jmedchem.1c02132

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Discovery of (S)-1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain

Autor: Guanglin Luo, Ling Chen, Walter A. Kostich, Brian Hamman, Jason Allen, Amy Easton, Clotilde Bourin, Michael Gulianello, Jonathan Lippy, Susheel Nara, Tarun Kumar Maishal, Kamalraj Thiyagarajan, Prasadrao Jalagam, Sreenivasulu Naidu Pattipati, Kumaran Dandapani, Manoj Dokania, Pradeep Vattikundala, Vivek Sharma, Saravanan Elavazhagan, Manoj Kumar Verma, Manish Lal Das, Santosh Wagh, Anand Balakrishnan, Benjamin M. Johnson, Kenneth S. Santone, George Thalody, Rex Denton, Hariharan Saminathan, Vinay K. Holenarsipur, Anoop Kumar, Abhijith Rao, Siva Prasad Putlur, Sarat Kumar Sarvasiddhi, Ganesh Shankar, Justin V. Louis, Manjunath Ramarao, Charles M. Conway, Yu-Wen Li, Rick Pieschl, Yuan Tian, Yang Hong, Jonathan Ditta, Arvind Mathur, Jianqing Li, Daniel Smith, Joseph Pawluczyk, Dawn Sun, Shiuhang Yip, Dauh-Rurng Wu, Muthalagu Vetrichelvan, Anuradha Gupta, Alan Wilson, Suma Gopinathan, Suman Wason, Linda Bristow, Charles F. Albright, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba

Publikováno v: Journal of Medicinal Chemistry. 65:4457-4480

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::38224dcaf3d9ea2fabc4ac6df4a42a84
https://doi.org/10.1021/acs.jmedchem.1c02131

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Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors

Publikováno v: Journal of Medicinal Chemistry. 65:4121-4155

Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of neuropathic pain. Inhibition of AAK1 in the central nervous system, particularly within the spinal co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8405e1499645d3ed53e06501113a564
https://doi.org/10.1021/acs.jmedchem.1c01966

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Discovery of (

Autor: Guanglin, Luo, Ling, Chen, Walter A, Kostich, Brian, Hamman, Jason, Allen, Amy, Easton, Clotilde, Bourin, Michael, Gulianello, Jonathan, Lippy, Susheel, Nara, Tarun Kumar, Maishal, Kamalraj, Thiyagarajan, Prasadrao, Jalagam, Sreenivasulu Naidu, Pattipati, Kumaran, Dandapani, Manoj, Dokania, Pradeep, Vattikundala, Vivek, Sharma, Saravanan, Elavazhagan, Manoj Kumar, Verma, Manish Lal, Das, Santosh, Wagh, Anand, Balakrishnan, Benjamin M, Johnson, Kenneth S, Santone, George, Thalody, Rex, Denton, Hariharan, Saminathan, Vinay K, Holenarsipur, Anoop, Kumar, Abhijith, Rao, Siva Prasad, Putlur, Sarat Kumar, Sarvasiddhi, Ganesh, Shankar, Justin V, Louis, Manjunath, Ramarao, Charles M, Conway, Yu-Wen, Li, Rick, Pieschl, Yuan, Tian, Yang, Hong, Jonathan, Ditta, Arvind, Mathur, Jianqing, Li, Daniel, Smith, Joseph, Pawluczyk, Dawn, Sun, Shiuhang, Yip, Dauh-Rurng, Wu, Muthalagu, Vetrichelvan, Anuradha, Gupta, Alan, Wilson, Suma, Gopinathan, Suman, Wason, Linda, Bristow, Charles F, Albright, Joanne J, Bronson, John E, Macor, Carolyn D, Dzierba

Publikováno v: Journal of medicinal chemistry. 65(6)

Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have been identified and show efficacy in various rodent pain models. (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::1e41976413f9c4afd18a0630ac9bd2a0
https://pubmed.ncbi.nlm.nih.gov/35257579

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[ 3 H]BMT-046091 a potent and selective radioligand to determine AAK1 distribution and target engagement

Autor: Justin Vijay Louis, Kumaran Dandapani, Susheel J. Nara, Yang Hong, Yung Tian, Sarat Kumar Sarvasiddhi, Yifeng Lu, Carolyn Diane Dzierba, Walter Kostich, Yu-Wen Li, Rick L. Pieschl, Sreenivasulu Naidu, Charlie F. Albright, Joanne J. Bronson, John E. Macor, Reeba K. Vikramadithyan

Publikováno v: Neuropharmacology. 118:167-174

Adaptor-associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of serine/threonine kinases, plays a role in modulating clatherin coated endocytosis of specific surface receptors. We have demonstrated that AAK1 inhibitors are efficacious in rode

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f168813c715e6b8c8865371b20f68a5c
https://doi.org/10.1016/j.neuropharm.2017.03.015

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