Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Robert L, Bertekap"'
Autor:
Mary Jane Cullen, Qian Xiang, Jeffrey A. Robl, Philip M. Sher, Brian J. Murphy, Keith J. Miller, Timothy M. Harper, Andrew Alt, Emily Luk, Sarah E. Malmstrom, Dean A. Wacker, Ginger Wu, Kimberly A. Foster, John M. Fevig, Joseph Carpenter, Robert L. Bertekap, Mary F. Grubb, Ying Wang, Karen A. Rossi, Gang Wu, Christian L. Morales, Jianxin Feng, Xiang Yang Ye, Anthony V. Azzara, Matthias Broekema
Publikováno v:
Journal of Medicinal Chemistry. 60:6166-6190
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ab408370d6568ec38a8faeab8daced5
https://doi.org/10.1021/acs.jmedchem.7b00385
https://doi.org/10.1021/acs.jmedchem.7b00385
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:
Kelly Krause, Andrew P. Degnan, George O. Tora, Yu-Wen Li, Daniel G. Morgan, Ramkumar Rajamani, Joanna Hu, Ying Han, Rudolph G. Krause, Joanne J. Bronson, Robert L. Bertekap, Sarah J. Taylor, Kevin W. Gillman, Nicholas J. Lodge, Matthew T. Taber, John E. Macor, Gail K. Mattson, Melissa A. Cunningham, Carl D. Davis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3039-3043
Depression is a serious illness that affects millions of patients. Current treatments are associated with a number of undesirable side effects. Neurokinin 1 receptor (NK1R) antagonists have recently been shown to potentiate the antidepressant effects
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b85bad869a118e4a255bfbb6b6ebb60f
https://doi.org/10.1016/j.bmcl.2015.04.098
https://doi.org/10.1016/j.bmcl.2015.04.098
Autor:
Zhi Liang, Alan Wilson, Li Dong, Neil T. Burford, David S. Kimball, Kenneth G. Carson, Yingzhi Bi, Yulian Zhang, Bireshwar Dasgupta, Carolyn Diane Dzierba, Richard A. Hartz, James E. Grace, G. Greg Zipp, Soojin Kwon, Martin A. Lewis, Joanne J. Bronson, Cynthia Anne Fink, Amr Nouraldeen, Saadat Aleem, Giovanni Cianchetta, Jiancheng Wang, Ying Liu, Vijay T. Ahuja, Robert L. Bertekap, Jianxin Han, Michael Alan Green, Angela Cacace, Godwin Kumi, Yudith Garcia, Ying Qiao, Meredith Ferrante, John E. Macor, Ryan Westphal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1448-1452
Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16bf15e7cd2cc6067dbe9746466df095
https://doi.org/10.1016/j.bmcl.2015.01.036
https://doi.org/10.1016/j.bmcl.2015.01.036
Autor:
Joseph, Carpenter, Ying, Wang, Gang, Wu, Jianxin, Feng, Xiang-Yang, Ye, Christian L, Morales, Matthias, Broekema, Karen A, Rossi, Keith J, Miller, Brian J, Murphy, Ginger, Wu, Sarah E, Malmstrom, Anthony V, Azzara, Philip M, Sher, John M, Fevig, Andrew, Alt, Robert L, Bertekap, Mary Jane, Cullen, Timothy M, Harper, Kimberly, Foster, Emily, Luk, Qian, Xiang, Mary F, Grubb, Jeffrey A, Robl, Dean A, Wacker
Publikováno v:
Journal of medicinal chemistry. 60(14)
Agonism of the 5-HT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b4aad16c8dfe5c23e1f667fa571a60d5
https://pubmed.ncbi.nlm.nih.gov/28635286
https://pubmed.ncbi.nlm.nih.gov/28635286
Autor:
Ivar M. McDonald, Robert A. Mate, Debra J. Post-Munson, Meredith Ferrante, David G. Harden, Lizbeth Gallagher, Richard E. Olson, F. Christopher Zusi, Barbara J. Robertson, Steven I. Dworetzky, Daniel G. Morgan, Hong Huang, Ronald J. Knox, Nicholas J. Lodge, John E. Macor, Robert L. Bertekap
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1684-1688
High throughput screening led to the identification of a novel series of quinolone α7 nicotinic acetylcholine receptor (nAChR) agonists. Optimization of an HTS hit (1) led to 4-phenyl-1-(quinuclidin-3-ylmethyl)quinolin-2(1H)-one, which was found to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9746d0f86cd20debcb9cc92ebb146599
https://doi.org/10.1016/j.bmcl.2013.01.070
https://doi.org/10.1016/j.bmcl.2013.01.070
Autor:
Yu-Wen Li, George O. Tora, Snjezana Lelas, Kim A. Johnson, Matthew T. Taber, Joanne J. Bronson, Michael F. Parker, Rudolf G. Krause, Amy Newton, Robert L. Bertekap, Kelly D. Lengyel, Kevin W. Gillman, Nicholas J. Lodge, Rick L. Pieschl, John E. Macor, Andrew P. Degnan, Silva Mark, Sarah J. Taylor
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:407-411
A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK(1)/SERT affinity. Optimization based on NK(1)/SERT binding affinities, and minimization of off-target ion channel activity lead to the discovery of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::357bdb8f1a8f0c5d53b0870959d77c3f
https://doi.org/10.1016/j.bmcl.2012.11.094
https://doi.org/10.1016/j.bmcl.2012.11.094
Autor:
Thaddeus F. Molski, Kevin D. Burris, Tanaz Mistry Kannan, Kelly A. Allers, Shaun Jordan, Tetsuro Kikuchi, Frank D. Yocca, Arlene Stark, Trevor Sharp, Robert L. Bertekap, Ruoyan Chen
BACKGROUND: Aripiprazole (7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydro-2(1H)-quinolinone) is a novel antipsychotic with a mechanism of action that differs from current typical and atypical antipsychotics. Aripiprazole interacts with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f31f87dc2f0b84e111aac6e450c3378d
https://doi.org/10.1007/s00213-006-0621-y
https://doi.org/10.1007/s00213-006-0621-y
Publikováno v:
Biochemical Pharmacology. 81:691-702
Once considered a pharmacological curiosity, allosteric modulation of seven transmembrane domain G-protein-coupled receptors (GPCRs) has emerged as a potentially powerful means to affect receptor function for therapeutic purposes. Allosteric modulato
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cda8683b6baac176dfc2814f15cd89b
https://doi.org/10.1016/j.bcp.2010.12.012
https://doi.org/10.1016/j.bcp.2010.12.012
Autor:
Clotilde Bourin, Charles M. Conway, Kai Xie, Sing-Yuen Sit, Robert L. Bertekap, Kevin D. Burris
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1272-1277
A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biologica
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7ab3277282926f8d4c543787dcb995b
https://doi.org/10.1016/j.bmcl.2009.11.080
https://doi.org/10.1016/j.bmcl.2009.11.080