Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Michael Gulianello"'
Autor:
Guanglin Luo, Ling Chen, Walter A. Kostich, Brian Hamman, Jason Allen, Amy Easton, Clotilde Bourin, Michael Gulianello, Jonathan Lippy, Susheel Nara, 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, Linda Bristow, Charles F. Albright, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba
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
https://doi.org/10.1021/acs.jmedchem.1c02132
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
https://doi.org/10.1021/acs.jmedchem.1c02131
Autor:
Richard A. Hartz, Vijay T. Ahuja, Susheel J. Nara, C. M. Vijaya Kumar, Raju K. V. L. P. Manepalli, Sarat Kumar Sarvasiddhi, Swarnamba Honkhambe, Vidya Patankar, Bireshwar Dasgupta, Ramkumar Rajamani, Jodi K. Muckelbauer, Daniel M. Camac, Kaushik Ghosh, Matthew Pokross, Susan E. Kiefer, Jeffrey M. Brown, Lisa Hunihan, Michael Gulianello, Martin Lewis, Jonathan S. Lippy, Neha Surti, Brian D. Hamman, Jason Allen, Walter A. Kostich, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba
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
https://doi.org/10.1021/acs.jmedchem.1c01966
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
https://pubmed.ncbi.nlm.nih.gov/35257579
Autor:
Jodi K. Muckelbauer, Ramkumar Rajamani, Jeffrey M. Brown, C M Vijaya Kumar, Kumaran Dandapani, Jonathan Lippy, Saravanan Elavazhagan, Vijay T. Ahuja, John E. Macor, Carolyn Diane Dzierba, Brian D. Hamman, Walter Kostich, Michael Gulianello, Manoj Dokania, Susan E. Kiefer, Susheel J. Nara, Joanne J. Bronson, Amy Easton, Richard A. Hartz, Linda J. Bristow, Martin A. Lewis, Jason Allen, Sreenivasulu N Pattipati, Neha Surti, Lisa Hunihan, Daniel M. Camac
Publikováno v:
Journal of medicinal chemistry. 64(15)
Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a874893d7c1ec730ba639d989c3f7ccd
https://pubmed.ncbi.nlm.nih.gov/34270254
https://pubmed.ncbi.nlm.nih.gov/34270254
Autor:
Valerie J. Whiterock, Xiang-Jun Jiang, Guanglin Luo, Carl D. Davis, Charles M. Conway, Deborah Keavy, Kimberly A. Widmann, Laura J. Signor, Walter Kostich, Ling Chen, John E. Macor, Gene M. Dubowchik, Richard Schartman, Ping Chen, Michael Gulianello
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 43:128077
In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available azepinone derivatives that unfortunately also exhibited the unwanted property of potent time-dependent human CYP3A4
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5245d552bf5dda42383d5d101e10c53c
https://doi.org/10.1016/j.bmcl.2021.128077
https://doi.org/10.1016/j.bmcl.2021.128077
Autor:
Valerie J. Whiterock, Amy Easton, Regina Miller, Lawrence R. Marcin, Meredith Ferrante, Bradley C. Pearce, John B. Hogan, Joanne J. Bronson, Clotilde Bourin, Mendi A. Higgins, Robert G. Gentles, F. Christopher Zusi, Walter Kostich, John E. Macor, Michael Gulianello, Min Ding, Linda J. Bristow, Adam Hendricson, Kim A. Johnson, Andrew Alt, Yanling Huang, Matthew A. Seager
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:496-513
Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d4fbbfea4e7fe10fc6e8c858a57219bd
https://doi.org/10.1016/j.bmc.2016.11.018
https://doi.org/10.1016/j.bmc.2016.11.018
Autor:
Andrew P. Degnan, Valerie J. Whiterock, Darrell Maxwell, Umesh Hanumegowda, Digavalli V. Sivarao, Anand Balakrishnan, Eric Shields, Joanne J. Bronson, Jeffrey M. Brown, Ryan Westphal, Amy Easton, Arun K. Senapati, Xiaoliang Zhuo, John E. Macor, Kenneth S. Santone, Michael Gulianello, Regina Miller, Melissa Hill-Drzewi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5871-5876
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6efc9c8447ba3a2d03837196eeccc095
https://doi.org/10.1016/j.bmcl.2016.11.014
https://doi.org/10.1016/j.bmcl.2016.11.014
Autor:
Valerie J. Whiterock, John E. Macor, Joanne J. Bronson, Melissa Hill-Drzewi, Regina Miller, Lizbeth Gallagher, Thaddeus F. Molski, Amy Easton, Xiaoliang Zhuo, Matthew D. Hill, Andrew P. Degnan, Xiaojun Han, Jeffrey M. Brown, Robert L. Bertekap, Haiquan Fang, Michael Gulianello, Michele Matchett, Kenneth S. Santone, Anand Balakrishnan
Publikováno v:
ACS Medicinal Chemistry Letters. 7:1082-1086
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-d-aspartate receptor (NMDAR). We describe the synthesis o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d90ae309c4691d80df7686005bbf768d
https://doi.org/10.1021/acsmedchemlett.6b00292
https://doi.org/10.1021/acsmedchemlett.6b00292
Autor:
James E. Grace, Brian Zambrowicz, Pradeep Vattikundala, Kenneth G. Carson, Jonathan Lippy, Clotilde Bourin, Alan Main, Alan Wilson, Sreenivasulu Naidu, Sandhya Mandlekar, Carolyn Diane Dzierba, Saravanan Elavazhagan, Walter Kostich, Gauri Shankar, Jeffrey M. Brown, Charles M. Conway, Charles F. Albright, Justin Vijay Louis, Yu-Wen Li, Vivek Sharma, Yanling Huang, Laszlo Kiss, Amr Nouraldeen, Susheel J. Nara, Martin A. Lewis, Ryan Westphal, Vinay K. Holenarsipur, Anand Balakrishnan, Amy Easton, Robert Zaczek, Jonathan C. Swaffield, Ted Molski, Rick L. Pieschl, Kevin Baker, Katerina Savelieva, Yingzhi Bi, Kenneth S. Santone, Linda J. Bristow, John E. Macor, Jianlin Feng, Guilan Ye, Joanne J. Bronson, Manish Lal Das, Reeba K. Vikramadithyan, Kevin O’Malley, Jason W. Allen, Brian D. Hamman, Michael Gulianello, Yifeng Lu, Thomas H. Lanthorn, Kimberley A. Lentz, Anoop Kumar, Manoj Dokania, Kumaran Dandapani, Rex Denton
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics
To identify novel targets for neuropathic pain, 3097 mouse knockout lines were tested in acute and persistent pain behavior assays. One of the lines from this screen, which contained a null allele of the adapter protein-2 associated kinase 1 (AAK1) g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04b1480bd30607a9fe64d0e01fbd6b27
http://europepmc.org/articles/PMC4998676
http://europepmc.org/articles/PMC4998676