Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Airu S. Chen"'
Autor:
Palucki Brenda, Patrick G. Pollard, Liangqin Guo, Tung M. Fong, Matthew J. Wyvratt, Randy R. Miller, Shuwen He, Constantin Tamvakopoulos, Iyassu K. Sebhat, Qianping Peng, Ravi P. Nargund, Zhixiong Ye, Airu S. Chen, Doreen E. Cashen, David H. Weinberg, Min K. Park, Raman K. Bakshi, D. Euan MacIntyre, Howard Y. Chen, Rui Tang, Tanya MacNeil, Qingmei Hong, Alison M. Strack, Ralph A. Stearns, Jian Liu, William J. Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2330-2334
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99aea0aa624d82cc9bc8f3cfa4bdb369
https://doi.org/10.1016/j.bmcl.2011.02.090
https://doi.org/10.1016/j.bmcl.2011.02.090
Autor:
Yingjie Lai, Ralph A. Stearns, Qianping Peng, Ravi P. Nargund, Qingmei Hong, Jian Liu, Rui Tang, Matthew J. Wyvratt, Raman K. Bakshi, Randy R. Miller, Tianying Jian, Alison M. Strack, Tanya MacNeil, Liangqin Guo, Howard Y. Chen, James Dellureficio, Iyassu K. Sebhat, Peter H. Dobbelaar, Airu S. Chen, Constantin Tamvakopoulos, David H. Weinberg, Tung M. Fong, Christopher L. Franklin, Shuwen He, Zhixiong Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4399-4405
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b04db1e6e6855a321002bb787613d21e
https://doi.org/10.1016/j.bmcl.2010.06.062
https://doi.org/10.1016/j.bmcl.2010.06.062
Autor:
Howard Y. Chen, William J. Martin, D. Euan MacIntyre, Zhixiong Ye, Raman K. Bakshi, Alison M. Strack, Doreen E. Cashen, Jian Liu, Yingjie Lai, Tianying Jian, Constantin Tamvakopoulos, Nancy N. Tsou, Shuwen He, James Dellureficio, Tung M. Fong, Peter H. Dobbelaar, David H. Weinberg, Airu S. Chen, Qingmei Hong, Iyassu K. Sebhat, Tanya MacNeil, Christopher L. Franklin, Ravi P. Nargund, Ralph A. Stearns, Rui Tang, Richard G. Ball, Matthew J. Wyvratt, Randy R. Miller, Liangqin Guo, Qianping Peng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2106-2110
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ecb491322cadefd63c62faedffb60b8
https://doi.org/10.1016/j.bmcl.2010.02.058
https://doi.org/10.1016/j.bmcl.2010.02.058
Publikováno v:
The FASEB Journal. 20:2234-2241
In this study we have characterized the anti-inflammatory profile of a selective melanocortin type 3 receptor (MC3-R) ligand [D-Trp8]-gamma-MSH, validating in vitro results with analyses in mice deficient for this receptor subtype. In wild-type (WT)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61bf18fcee1944ba42a69e75457b860a
https://doi.org/10.1096/fj.06-6339com
https://doi.org/10.1096/fj.06-6339com
Autor:
Doreen E. Cashen, Constantin Tamvakopoulos, Qianping Peng, William J. Martin, David H. Weinberg, Charles Rosenblum, Arthur A. Patchett, Tanya MacNeil, Patrick G. Pollard, Zhixiong Ye, Raman K. Bakshi, Ralph A. Stearns, Rubana N. Kalyani, Palucki Brenda, Joseph M. Metzger, Alison M. Strack, Lex H.T. Van der Ploeg, D. Euan MacIntyre, Iyassu K. Sebhat, Aurawan Vongs, Airu S. Chen, Ravi P. Nargund, Liangqin Guo, Matthew J. Wyvratt, Randy R. Miller, Rui Tang, Howard Y. Chen, Khaled J. Barakat
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3501-3505
A novel isoquinuclidine containing selective melanocortin subtype-4 receptor small molecule agonist, 3 (RY764), is reported. Its in vivo characterization revealed mechanism-based food intake reduction and erectile activity augmentation in rodents.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eec96b03aa1e5f2ba3d3c429b0a51544
https://doi.org/10.1016/j.bmcl.2005.05.109
https://doi.org/10.1016/j.bmcl.2005.05.109
Autor:
George R. Breese, Donald J. Marsh, Montserrat Navarro, Todd E. Thiele, Darin J. Knapp, Airu S. Chen, Inmaculada Cubero, Howard Y. Chen
Publikováno v:
Alcoholism: Clinical & Experimental Research. 29:949-957
THE MELANOCORTIN (MC) system is composed of peptides that are cleaved from the polypeptide precursor proopiomelanocortin (POMC). Central MC peptides are produced by neurons within the hypothalamic arcuate nucleus and the medulla (Dores et al., 1986;
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83888f6e3360c76c3b4fc9c92accbb69
https://doi.org/10.1097/01.alc.0000167740.19702.8c
https://doi.org/10.1097/01.alc.0000167740.19702.8c
Autor:
Michael R. Tota, Ravi P. Nargund, Xiao-Ming Guan, Howard Y. Chen, Douglas J. MacNeil, David H. Weinberg, Tanya MacNeil, Euan Macintyre, Alison M. Strack, Charles Rosenblum, Maria A. Bednarek, Andrew D. Howard, Chun-Pyn Shen, Tung M. Fong, Mark T. Goulet, Lex H.T. Van der Ploeg, Airu S. Chen, Donald J. Marsh
Publikováno v:
European Journal of Pharmacology. 440:141-157
Five G-protein-coupled melanocortin receptors (MC(1)-MC(5)) are expressed in mammalian tissues. The melanocortin receptors support diverse physiological functions, including the regulation of hair color, adrenal function, energy homeostasis, feed eff
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ebcc6d63b6793976d33c04bbd680bdb
https://doi.org/10.1016/s0014-2999(02)01425-5
https://doi.org/10.1016/s0014-2999(02)01425-5
Autor:
Patricia Brown, Anthony Sanfiz, Ann E. Weber, Richard A. Berger, Liping Wang, Katherine L. Villa, Scott D. Edmondson, Christopher Moyes, Amanda L. Hurley, Andra S. Stevenson, Aileen Fitzmaurice, Dong-Ming Shen, Stephen D. Goble, Nina Jochnowitz, Karen H. Dingley, Jerry Di Salvo, Mary Struthers, Loise Gichuru, Randall R. Miller, Hiroshi Nagabukuro, Gino Salituro, Airu S. Chen, Beata Zamlynny, Alka Bansal, Bart Harper, Shruty Mistry
Publikováno v:
Journal of medicinal chemistry. 57(4)
A series of conformationally restricted acetanilides were synthesized and evaluated as β3-adrenergic receptor agonists (β3-AR) for the treatment of overactive bladder (OAB). Optimization studies identified a five-membered ring as the preferred conf
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc1d1a538eaf74c7d6dfb1e647bd93e6
https://pubmed.ncbi.nlm.nih.gov/24437735
https://pubmed.ncbi.nlm.nih.gov/24437735
Autor:
Xiao-Ming Guan, Charles Rosenblum, Hong Yu, Yue Feng, D. Euan MacIntyre, Alison M. Strack, Lex H.T. Van der Ploeg, Christian N. Nunes, Airu S. Chen, Joseph M. Metzger, Linhai Cao, Easter G. Frazier, Jill K. Fisher, Ramon E. Camacho, William Min, Shobhna Gopal-Truter, Aurawan Vongs, Howard Y. Chen, Theodore N. Mellin, Donald J. Marsh, Myrna E. Trumbauer
Publikováno v:
Nature Genetics. 26:97-102
Genetic and pharmacological studies have defined a role for the melanocortin-4 receptor (Mc4r) in the regulation of energy homeostasis. The physiological function of Mc3r, a melanocortin receptor expressed at high levels in the hypothalamus, has rema
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d4ce2d771382f4fed6e69e47dad7818
https://doi.org/10.1038/79254
https://doi.org/10.1038/79254
Autor:
Donald J. Marsh, D. E. Macintyre, Xiao-Ming Guan, Michael J. Forrest, Easter G. Frazier, Airu S. Chen, Theodore N. Mellin, Ramon E. Camacho, Hong Yu, Jill K. Fisher, Van der Ploeg Lh, Joe Metzger, Alison M. Strack, Myrna E. Trumbauer, Howard Y. Chen, Shobhna Gopal-Truter
Publikováno v:
Transgenic Research. 9:145-154
We evaluated the role of the melanocortin-4 receptor (MC-4R) in the control of metabolic rate and food intake in mice. Intraperitoneal administration of the non-selective MC-R agonist melanotan II (MT-II; a cyclic heptapeptide) increases metabolic ra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::586a7faedae2998056546759a33e76a8
https://doi.org/10.1023/a:1008983615045
https://doi.org/10.1023/a:1008983615045