Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Mary Jane Cullen"'
Autor:
Susanne Neumann, Umesh Padia, Mary Jane Cullen, Elena Eliseeva, Eshel A Nir, Robert F Place, Sarah J Morgan, Marvin C Gershengorn
Publikováno v:
Frontiers in Endocrinology, Vol 7 (2016)
We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer. The agonist C2 (NCGC00161870) that we have studied so far is a racemic mixture containing equal am
Externí odkaz:
https://doaj.org/article/250d1128135641ce84215a1baf2f9171
Autor:
Shu Chang, Anthony V. Azzara, Yi-Xin Li, Marta Dabros, James Kempson, Reshma Panemangelor, Huji Turdi, Kimberly A. Foster, William J. Keim, Jean M. Whaley, Jeffrey A. Robl, Fang Moore, Luping Chen, Mary Jane Cullen, Xiaoping Hou, Atsu Apedo, R. Michael Lawrence, Arvind Mathur, David G. Harden, Wei Meng, Kevin O'Malley, Mary Ann Pelleymounter, Hannguang Chao, Pratik Devasthale, Jon J. Hangeland, Zhengping Ma, Dauh-Rurng Wu, Robert Paul Brigance, Guohua Zhao, Lynn M. Abell, Qi Gao, Susan Harvey, Lisa M. Kopcho, Dong Cheng, Elizabeth A. Dierks, Ching-Hsuen Chu, Suzanne Rooney, Xiang-Yang Ye, Saleem Ahmad, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:14773-14792
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e90999a2854f1a395c0459b5cd876d
https://doi.org/10.1021/acs.jmedchem.1c01356
https://doi.org/10.1021/acs.jmedchem.1c01356
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:
Neil Flynn, Mary Jane Cullen, Hongwei Zhang, Wei Wang, Susan Glick, Lisa Zhang, Jeffrey A. Robl, Pratik Devasthale, Andres S. Hernandez, Christian Caporuscio, Brian J. Murphy, Suzanne Rooney, Ning Huang, Mary Ann Pelleymounter, Kenneth W. Rohrbach, Kishore Renduchintala, Anthony V. Azzara, Helen E. Godonis, Yi-Xin Li, Radhakrishnan Sridhar, Michael Thomas, Susan Harvey, Paul Stetsko, Mary F. Grubb, Chris Freeden, Fang Moore, Christine Huang, James Devenny, Daniel Longhi, William N. Washburn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2793-2799
Our investigation of the structure–activity and structure–liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17121b519c7b9c469d07059362c3d928
https://doi.org/10.1016/j.bmcl.2015.05.008
https://doi.org/10.1016/j.bmcl.2015.05.008
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:
Jeffrey A. Robl, Guohua Zhao, Joel C. Barrish, Bei Wang, Brad D. Maxwell, Christian Caporuscio, Hongwei Zhang, James Devenny, Mary F. Grubb, Zhenghua Wang, Suzanne Rooney, James Mignone, Lisa Zhang, Brian J. Murphy, Wei Wang, Daniel Longhi, William N. Washburn, Kenneth W. Rohrbach, Evan B. Janovitz, Mark C. Manfredi, Mary Ann Pelleymounter, Michael Thomas, Hong Yang, Paul Stetsko, Saleem Ahmad, Atsu Apedo, Mary Jane Cullen, Brian Gemzik, Ning Huang, Chris Freeden, Susan Harvey, Anthony V. Azzara, Khehyong Ngu, Christine Huang, Rulin Zhao, Susan Glick, Neil Flynn, Pratik Devasthale, Andres S. Hernandez, Helen E. Godonis
Publikováno v:
Journal of Medicinal Chemistry. 57:7509-7522
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high affinity allowed us
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d485619df8ba6741a931b9a426eb5aa0
https://doi.org/10.1021/jm500026w
https://doi.org/10.1021/jm500026w
Autor:
Kenneth E. Carlson, Olafur S. Gudmundsson, Bruce A. Ellsworth, Philip M. Sher, Susan Harvey, Eva Zuvich, Michael Thomas, William J. Keim, Gang Wu, Helen E. Godonis, Paul Stetsko, Brian J. Murphy, Richard B. Sulsky, Guixue Yu, William R. Ewing, Mary Jane Cullen, Mary Ann Pelleymounter, Doree F. Sitkoff, Susan Johnghar, Zhengxiang Gu, Ximao Wu, James Devenny, Rose Ann F Baska, Asoka Ranasinghe, Ning Lee, Kamelia Behnia, Anthony V. Azzara, Kenneth W. Rohrbach, Gerry Everlof, Liya Kang, Natesan Murugesan, Yeheng Zhu, Yifan Yang
Publikováno v:
Journal of Medicinal Chemistry. 56:9586-9600
Several strategies have been employed to reduce the long in vivo half-life of our lead CB1 antagonist, triazolopyridazinone 3, to differentiate the pharmacokinetic profile versus the lead clinical compounds. An in vitro and in vivo clearance data set
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::417c836ddf3010c89cd9792afb3349b0
https://doi.org/10.1021/jm4010835
https://doi.org/10.1021/jm4010835
Autor:
Keith J. Miller, Kenneth W. Rohrbach, Jianxin Feng, Mary Ann Pelleymounter, Sarah E. Malmstrom, Jinping Gan, Ge Zhang, Ginger Wu, Thao Ung, Chen-Pin Hung, William J. Keim, Karen A. Rossi, Jeffrey A. Robl, Qinling Qu, John M. Fevig, Mary Jane Cullen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:330-335
A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT(2C) agonism with excellent selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compounds such as 38
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2079c57086a886d54141aa8d75f1c8e7
https://doi.org/10.1016/j.bmcl.2012.10.091
https://doi.org/10.1016/j.bmcl.2012.10.091
Autor:
Suzanne Rooney, James Devenny, Helen E. Godonis, Susan Harvey, Mary Jane Cullen, Mary Ann Pelleymounter
Publikováno v:
Obesity. 20:1645-1652
Dapagliflozin is a potent and selective sodium glucose cotransporter-2 (SGLT2) inhibitor which promotes urinary glucose excretion and induces weight loss. Since metabolic compensation can offset a negative energy balance, we explored the potential fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8888f11ec8c31502f97085bf77346ed6
https://doi.org/10.1038/oby.2012.59
https://doi.org/10.1038/oby.2012.59
Autor:
Evan B. Janovitz, Mary Ann Pelleymounter, Mary F. Malley, Eva Zuvich, Jeffrey G. Varnes, Xueying Cao, Chen-Pin Hung, Karen A. Rossi, Mary Jane Cullen, Thao Ung, William J. Keim, Sarah E. Malmstrom, Michael Thomas, Keith J. Miller, Ginger Wu, Kenneth W. Rohrbach, Ge Zhang, Rangaraj Narayanan, Qinling Qu, Lois D. Lehman-McKeeman, Jeffrey A. Robl, James Devenny, Dean A. Wacker
Publikováno v:
Journal of Medicinal Chemistry. 50:1365-1379
Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the synthesis and optimization of a new class of pyrazinoisoindolone-containing, selective 5-HT2C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af9455a4be4dd87363342b50ad98d204
https://doi.org/10.1021/jm0612968
https://doi.org/10.1021/jm0612968