Zobrazeno 1 - 10
of 95
pro vyhledávání: '"Charles Rosenblum"'
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.
Autor:
George A. Doss, Lex H.T. Van der Ploeg, Qianping Peng, Ravi P. Nargund, Charles Rosenblum, Randall R. Miller, Aurawan Vongs, Palucki Brenda, Tanya MacNeil, Ralph A. Stearns, Min K. Park, David H. Weinberg, Rui Tang, Arthur A. Patchett, Constantin Tamvakopoulos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1993-1996
We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. The 5- and 6-alkylated piperazine compounds exhibit low bioactivation potential as measured by c
Autor:
William J. Martin, D. Euan MacIntyre, Ravi P. Nargund, Rubana N. Kalyani, Rui Tang, George A. Doss, Min K. Park, Alison M. Strack, Erin McGowan, Joseph M. Metzger, Charles Rosenblum, Randall R. Miller, Palucki Brenda, Qianping Peng, Arthur A. Patchett, Ralph A. Stearns, Patrick G. Pollard, Lex H.T. Van der Ploeg, Iyassu K. Sebhat, Constantin Tamvakopoulos, Cherrie Shepherd, Aurawan Vongs, Tanya MacNeil, David H. Weinberg, Zhixiong Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:171-175
We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.
Publikováno v:
Regulatory Peptides. 120:113-118
The melanocortin 4 receptor (MC4-R) is a Galpha s-coupled receptor known to increase cAMP production following agonist stimulation. We demonstrate that the mitogen-activated protein kinases p42 (ERK2) and p44 (ERK1) are also activated by MC4-R follow
Autor:
Mark T. Goulet, Lihu Yang, Aurawan Vongs, David H. Weinberg, Charles Rosenblum, Changyou Zhou, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Tanya MacNeil, Rubana N. Kalyani, Rui Tang, Lex H.T. Van der Ploeg, Warner Daniel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4431-4435
The discovery and optimization of a new class of non-peptidyl, pyridazinone derived melanocortin subtype-4 receptor agonists is disclosed.
Autor:
Christopher P. Austin, Doreen E. Cashen, Sheng-Shung Pong, Brian D. Spar, Brett Connolly, Tung Ming Fong, D. Euan MacIntyre, Carina P. Tan, Michael R. Tota, Ravi P. Nargund, R. S. L. Chang, Oksana C. Palyha, Constantin Tamvakopoulos, Deborah L. Drazen, Anthony G. DiLella, Jennifer E. Drisko, David J. Figueroa, Tanya MacNeil, Andreas W. Sailer, David H. Weinberg, Randy J. Nelson, Charles Rosenblum, Cathy R.-R.C. Huang, Rui Tang, Arthur A. Patchett, Xiao-Ming Guan, Hong Yu, George J. Christ, Andrew D. Howard, Lex H.T. Van der Ploeg, William J. Martin, Aurawan Vongs, Iyassu K. Sebhat, Ralph A. Stearns
Publikováno v:
Proceedings of the National Academy of Sciences. 99:11381-11386
By using a combination of genetic, pharmacological, and anatomical approaches, we show that the melanocortin 4 receptor (MC4R), implicated in the control of food intake and energy expenditure, also modulates erectile function and sexual behavior. Evi
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
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
Autor:
Jeffrey P Varnerin, T. Smith, Aurawan Vongs, Patricia J. Hey, M. Chou, Joseph J. King, Theodore N. Mellin, Easter G. Frazier, Michael R. Tota, D. E. Macintyre, Beth Junker, Beth Ann Murphy, Charles Rosenblum, Christian N. Nunes, B. W. Burgess, L. H. T. Van Der Ploeg
Publikováno v:
Protein Expression and Purification. 14:335-342
A procedure is described for gram-scale refolding of Escherichia coli-derived human leptin inclusion bodies. Refolding was achieved by gradually reducing denaturant using a diafiltration method. Refolded leptin is characterized by in vivo modulation
Autor:
Philip S. Paress, Sheng-Shung Pong, Donna L. Hreniuk, Paul A. Liberator, Michael Rigby, Roy G. Smith, Oksana C. Palyha, Arthur A. Patchett, Michel J. Hamelin, Robert P. Heavens, Andrew D. Howard, Patrick R. Griffin, David G. Melillo, Charles Rosenblum, Lee-Yuh Chaung, Ravi P. Nargund, Michael Chou, Jennifer W. Anderson, Dennis C. Dean, Sunil Gupta, Alex Elbrecht, Scott D. Feighner, Dalip J. S. Sirinathsinghji, Joseph P. Arena, Carmen Diaz, Julie A. DeMartino, Mike Dashkevicz, Doris F. Cully, Karen K. McKee, Lex H.T. Van der Ploeg, James M. Schaeffer, Ken K. Liu
Publikováno v:
Science. 273:974-977
Small synthetic molecules termed growth hormone secretagogues (GHSs) act on the pituitary gland and the hypothalamus to stimulate and amplify pulsatile growth hormone (GH) release. A heterotrimeric GTP-binding protein (G protein)-coupled receptor (GP