-
1
-
-
2342625424
-
Increasing prevalence of type 2 diabetes in adolescents
-
Hotu S., Carter B., Watson P., Cutfield W., and Cundy T. Increasing prevalence of type 2 diabetes in adolescents. J Paediatr Child Health 40 (2004) 201-204
-
(2004)
J Paediatr Child Health
, vol.40
, pp. 201-204
-
-
Hotu, S.1
Carter, B.2
Watson, P.3
Cutfield, W.4
Cundy, T.5
-
2
-
-
10744228850
-
Relation of serial changes in childhood body-mass index to impaired glucose tolerance in young adulthood
-
Bhargava S.K., Sachdev H.S., Fall C.H., Osmond C., Lakshmy R., Barker D.J., Biswas S.K., Ramji S., Prabhakaran D., and Reddy K.S. Relation of serial changes in childhood body-mass index to impaired glucose tolerance in young adulthood. N Engl J Med 350 (2004) 865-875
-
(2004)
N Engl J Med
, vol.350
, pp. 865-875
-
-
Bhargava, S.K.1
Sachdev, H.S.2
Fall, C.H.3
Osmond, C.4
Lakshmy, R.5
Barker, D.J.6
Biswas, S.K.7
Ramji, S.8
Prabhakaran, D.9
Reddy, K.S.10
-
3
-
-
2642568613
-
Obesity: an overview on its current perspectives and treatment options
-
Nammi S., Koka S., Chinnala K.M., and Boini K.M. Obesity: an overview on its current perspectives and treatment options. Nutr J 3 (2004) 3
-
(2004)
Nutr J
, vol.3
, pp. 3
-
-
Nammi, S.1
Koka, S.2
Chinnala, K.M.3
Boini, K.M.4
-
4
-
-
0031613806
-
Drug treatment of obesity: don't throw the baby out with the bath water
-
Bray G. Drug treatment of obesity: don't throw the baby out with the bath water. Am J Clin Nutr 67 (1998) 1-2
-
(1998)
Am J Clin Nutr
, vol.67
, pp. 1-2
-
-
Bray, G.1
-
5
-
-
0032543869
-
Obesity: a time bomb to be defused
-
Bray G.A. Obesity: a time bomb to be defused. Lancet 352 (1998) 160-161
-
(1998)
Lancet
, vol.352
, pp. 160-161
-
-
Bray, G.A.1
-
6
-
-
0034611784
-
Medicinal strategies in the treatment of obesity
-
Bray G.A., and Tartaglia L.A. Medicinal strategies in the treatment of obesity. Nature 404 (2000) 672-677
-
(2000)
Nature
, vol.404
, pp. 672-677
-
-
Bray, G.A.1
Tartaglia, L.A.2
-
7
-
-
0035565495
-
Pro-opiomelanocortin and weight regulation: from mice to men
-
Boston B.A. Pro-opiomelanocortin and weight regulation: from mice to men. J Pediatr Endocrinol Metab 14 Suppl 6 (2001) 1409-1416
-
(2001)
J Pediatr Endocrinol Metab
, vol.14
, Issue.SUPPL. 6
, pp. 1409-1416
-
-
Boston, B.A.1
-
9
-
-
10244235259
-
Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior
-
Hu Y., Bloomquist B.T., Cornfield L.J., DeCarr L.B., Flores-Riveros J.R., Friedman L., Jiang P., Lewis-Higgins L., Sadlowski Y., Schaefer J., Velazquez N., and McCaleb M.L. Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior. J Biol Chem 271 (1996) 26315-26319
-
(1996)
J Biol Chem
, vol.271
, pp. 26315-26319
-
-
Hu, Y.1
Bloomquist, B.T.2
Cornfield, L.J.3
DeCarr, L.B.4
Flores-Riveros, J.R.5
Friedman, L.6
Jiang, P.7
Lewis-Higgins, L.8
Sadlowski, Y.9
Schaefer, J.10
Velazquez, N.11
McCaleb, M.L.12
-
10
-
-
0027049534
-
Molecular characterization of the mouse agouti locus
-
Bultman S.J., Michaud E.J., and Woychik R.P. Molecular characterization of the mouse agouti locus. Cell 71 (1992) 1195-1204
-
(1992)
Cell
, vol.71
, pp. 1195-1204
-
-
Bultman, S.J.1
Michaud, E.J.2
Woychik, R.P.3
-
11
-
-
0028139089
-
Positional cloning of the mouse obese gene and its human homologue
-
Zhang Y., Proenca R., Maffei M., Barone M., Leopold L., and Friedman J.M. Positional cloning of the mouse obese gene and its human homologue. Nature 372 (1994) 425-432
-
(1994)
Nature
, vol.372
, pp. 425-432
-
-
Zhang, Y.1
Proenca, R.2
Maffei, M.3
Barone, M.4
Leopold, L.5
Friedman, J.M.6
-
12
-
-
0032489093
-
Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior
-
[1 page following 696]
-
Sakurai T., Amemiya A., Ishii M., Matsuzaki I., Chemelli R.M., Tanaka H., Williams S.C., Richarson J.A., Kozlowski G.P., Wilson S., Arch J.R., Buckingham R.E., Haynes A.C., Carr S.A., Annan R.S., McNulty D.E., Liu W.S., Terrett J.A., Elshourbagy N.A., Bergsma D.J., et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell 92 (1998) [1 page following 696]
-
(1998)
Cell
, vol.92
-
-
Sakurai, T.1
Amemiya, A.2
Ishii, M.3
Matsuzaki, I.4
Chemelli, R.M.5
Tanaka, H.6
Williams, S.C.7
Richarson, J.A.8
Kozlowski, G.P.9
Wilson, S.10
Arch, J.R.11
Buckingham, R.E.12
Haynes, A.C.13
Carr, S.A.14
Annan, R.S.15
McNulty, D.E.16
Liu, W.S.17
Terrett, J.A.18
Elshourbagy, N.A.19
Bergsma, D.J.20
more..
-
13
-
-
0032542294
-
Mice lacking melanin-concentrating hormone are hypophagic and lean
-
Shimada M., Tritos N.A., Lowell B.B., Flier J.S., and Maratos-Flier E. Mice lacking melanin-concentrating hormone are hypophagic and lean. Nature 396 (1998) 670-674
-
(1998)
Nature
, vol.396
, pp. 670-674
-
-
Shimada, M.1
Tritos, N.A.2
Lowell, B.B.3
Flier, J.S.4
Maratos-Flier, E.5
-
14
-
-
49349085730
-
Neuropeptide Y and alpha-melanocyte-stimulating hormone: interaction in obesity and possible role in the development of hypertension
-
Baltatzi M., Hatzitolios A., Tziomalos K., Iliadis F., and Zamboulis C. Neuropeptide Y and alpha-melanocyte-stimulating hormone: interaction in obesity and possible role in the development of hypertension. Int J Clin Pract 62 (2008) 1432-1440
-
(2008)
Int J Clin Pract
, vol.62
, pp. 1432-1440
-
-
Baltatzi, M.1
Hatzitolios, A.2
Tziomalos, K.3
Iliadis, F.4
Zamboulis, C.5
-
15
-
-
58149523595
-
New ligands for melanocortin receptors
-
Kaelin C.B., Candille S.I., Yu B., Jackson P., Thompson D.A., Nix M.A., Binkley J., Millhauser G.L., and Barsh G.S. New ligands for melanocortin receptors. Int J Obes (Lond) 32 Suppl 7 (2008) S19-S27
-
(2008)
Int J Obes (Lond)
, vol.32
, Issue.SUPPL. 7
-
-
Kaelin, C.B.1
Candille, S.I.2
Yu, B.3
Jackson, P.4
Thompson, D.A.5
Nix, M.A.6
Binkley, J.7
Millhauser, G.L.8
Barsh, G.S.9
-
16
-
-
35348848018
-
The role of proopiomelanocortin (POMC) neurones in feeding behaviour
-
Millington G.W. The role of proopiomelanocortin (POMC) neurones in feeding behaviour. Nutr Metab (Lond) 4 (2007) 18
-
(2007)
Nutr Metab (Lond)
, vol.4
, pp. 18
-
-
Millington, G.W.1
-
17
-
-
36048955043
-
The central melanocortin system directly controls peripheral lipid metabolism
-
Nogueiras R., Wiedmer P., Perez-Tilve D., Veyrat-Durebex C., Keogh J.M., Sutton G.M., Pfluger P.T., Castaneda T.R., Neschen S., Hofmann S.M., Howles P.N., Morgan D.A., Benoit S.C., Szanto I., Schrott B., Schurmann A., Joost H.G., Hammond C., Hui D.Y., Woods S.C., et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest 117 (2007) 3475-3488
-
(2007)
J Clin Invest
, vol.117
, pp. 3475-3488
-
-
Nogueiras, R.1
Wiedmer, P.2
Perez-Tilve, D.3
Veyrat-Durebex, C.4
Keogh, J.M.5
Sutton, G.M.6
Pfluger, P.T.7
Castaneda, T.R.8
Neschen, S.9
Hofmann, S.M.10
Howles, P.N.11
Morgan, D.A.12
Benoit, S.C.13
Szanto, I.14
Schrott, B.15
Schurmann, A.16
Joost, H.G.17
Hammond, C.18
Hui, D.Y.19
Woods, S.C.20
more..
-
18
-
-
0030889192
-
Targeted disruption of the melanocortin-4 receptor results in obesity in mice
-
Huszar D., Lynch C.A., Fairchild-Huntress V., Dunmore J.H., Fang Q., Berkemeier L.R., Gu W., Kesterson R.A., Boston B.A., Cone R.D., Smith F.J., Campfield L.A., Burn P., and Lee F. Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell 88 (1997) 131-141
-
(1997)
Cell
, vol.88
, pp. 131-141
-
-
Huszar, D.1
Lynch, C.A.2
Fairchild-Huntress, V.3
Dunmore, J.H.4
Fang, Q.5
Berkemeier, L.R.6
Gu, W.7
Kesterson, R.A.8
Boston, B.A.9
Cone, R.D.10
Smith, F.J.11
Campfield, L.A.12
Burn, P.13
Lee, F.14
-
19
-
-
0030614331
-
Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
-
Fan W., Boston B.A., Kesterson R.A., Hruby V.J., and Cone R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 385 (1997) 165-168
-
(1997)
Nature
, vol.385
, pp. 165-168
-
-
Fan, W.1
Boston, B.A.2
Kesterson, R.A.3
Hruby, V.J.4
Cone, R.D.5
-
20
-
-
0032476779
-
Feeding effects of hypothalamic injection of melanocortin 4 receptor ligands
-
Giraudo S.Q., Billington C.J., and Levine A.S. Feeding effects of hypothalamic injection of melanocortin 4 receptor ligands. Brain Res 809 (1998) 302-306
-
(1998)
Brain Res
, vol.809
, pp. 302-306
-
-
Giraudo, S.Q.1
Billington, C.J.2
Levine, A.S.3
-
21
-
-
0032772960
-
The central melanocortin system and energy homeostasis
-
Cone R.D. The central melanocortin system and energy homeostasis. Trends Endocrinol Metab 10 (1999) 211-216
-
(1999)
Trends Endocrinol Metab
, vol.10
, pp. 211-216
-
-
Cone, R.D.1
-
22
-
-
0032990469
-
Melanocortin-4 receptor: a novel signalling pathway involved in body weight regulation
-
Fisher S.L., Yagaloff K.A., and Burn P. Melanocortin-4 receptor: a novel signalling pathway involved in body weight regulation. Int J Obes Relat Metab Disord 23 Suppl 1 (1999) 54-58
-
(1999)
Int J Obes Relat Metab Disord
, vol.23
, Issue.SUPPL. 1
, pp. 54-58
-
-
Fisher, S.L.1
Yagaloff, K.A.2
Burn, P.3
-
24
-
-
0031589551
-
ART (protein product of agouti-related transcript) as an antagonist of MC-3 and MC-4 receptors
-
Fong T.M., Mao C., MacNeil T., Kalyani R., Smith T., Weinberg D., Tota M.R., and Van der Ploeg L.H. ART (protein product of agouti-related transcript) as an antagonist of MC-3 and MC-4 receptors. Biochem Biophys Res Commun 237 (1997) 629-631
-
(1997)
Biochem Biophys Res Commun
, vol.237
, pp. 629-631
-
-
Fong, T.M.1
Mao, C.2
MacNeil, T.3
Kalyani, R.4
Smith, T.5
Weinberg, D.6
Tota, M.R.7
Van der Ploeg, L.H.8
-
25
-
-
0030764741
-
Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
-
Ollmann M.M., Wilson B.D., Yang Y.K., Kerns J.A., Chen Y., Gantz I., and Barsh G.S. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science 278 (1997) 135-138
-
(1997)
Science
, vol.278
, pp. 135-138
-
-
Ollmann, M.M.1
Wilson, B.D.2
Yang, Y.K.3
Kerns, J.A.4
Chen, Y.5
Gantz, I.6
Barsh, G.S.7
-
26
-
-
0026800892
-
The cloning of a family of genes that encode the melanocortin receptors
-
Mountjoy K.G., Robbins L.S., Mortrud M.T., and Cone R.D. The cloning of a family of genes that encode the melanocortin receptors. Science 257 (1992) 1248-1251
-
(1992)
Science
, vol.257
, pp. 1248-1251
-
-
Mountjoy, K.G.1
Robbins, L.S.2
Mortrud, M.T.3
Cone, R.D.4
-
27
-
-
0027456619
-
Molecular cloning of a novel melanocortin receptor
-
Gantz I., Konda Y., Tashiro T., Shimoto Y., Miwa H., Munzert G., Watson S.J., DelValle J., and Yamada T. Molecular cloning of a novel melanocortin receptor. J Biol Chem 268 (1993) 8246-8250
-
(1993)
J Biol Chem
, vol.268
, pp. 8246-8250
-
-
Gantz, I.1
Konda, Y.2
Tashiro, T.3
Shimoto, Y.4
Miwa, H.5
Munzert, G.6
Watson, S.J.7
DelValle, J.8
Yamada, T.9
-
28
-
-
0027227288
-
Molecular cloning, expression, and gene localization of a fourth melanocortin receptor
-
Gantz I., Miwa H., Konda Y., Shimoto Y., Tashiro T., Watson S.J., DelValle J., and Yamada T. Molecular cloning, expression, and gene localization of a fourth melanocortin receptor. J Biol Chem 268 (1993) 15174-15179
-
(1993)
J Biol Chem
, vol.268
, pp. 15174-15179
-
-
Gantz, I.1
Miwa, H.2
Konda, Y.3
Shimoto, Y.4
Tashiro, T.5
Watson, S.J.6
DelValle, J.7
Yamada, T.8
-
29
-
-
0028198975
-
Molecular cloning, expression, and characterization of a fifth melanocortin receptor
-
Gantz I., Shimoto Y., Konda Y., Miwa H., Dickinson C.J., and Yamada T. Molecular cloning, expression, and characterization of a fifth melanocortin receptor. Biochem Biophys Res Commun 200 (1994) 1214-1220
-
(1994)
Biochem Biophys Res Commun
, vol.200
, pp. 1214-1220
-
-
Gantz, I.1
Shimoto, Y.2
Konda, Y.3
Miwa, H.4
Dickinson, C.J.5
Yamada, T.6
-
30
-
-
0034610311
-
Molecular determinants of ligand binding to the human melanocortin-4 receptor
-
Yang Y.K., Fong T.M., Dickinson C.J., Mao C., Li J.Y., Tota M.R., Mosley R., Van Der Ploeg L.H., and Gantz I. Molecular determinants of ligand binding to the human melanocortin-4 receptor. Biochemistry 39 (2000) 14900-14911
-
(2000)
Biochemistry
, vol.39
, pp. 14900-14911
-
-
Yang, Y.K.1
Fong, T.M.2
Dickinson, C.J.3
Mao, C.4
Li, J.Y.5
Tota, M.R.6
Mosley, R.7
Van Der Ploeg, L.H.8
Gantz, I.9
-
31
-
-
0035918601
-
Structure activity studies of the melanocortin-4 receptor by in vitro mutagenesis: identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants
-
Haskell-Luevano C., Cone R.D., Monck E.K., and Wan Y.P. Structure activity studies of the melanocortin-4 receptor by in vitro mutagenesis: identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants. Biochemistry 40 (2001) 6164-6179
-
(2001)
Biochemistry
, vol.40
, pp. 6164-6179
-
-
Haskell-Luevano, C.1
Cone, R.D.2
Monck, E.K.3
Wan, Y.P.4
-
32
-
-
23944512136
-
Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists
-
Pogozheva I.D., Chai B.X., Lomize A.L., Fong T.M., Weinberg D.H., Nargund R.P., Mulholland M.W., Gantz I., and Mosberg H.I. Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists. Biochemistry 44 (2005) 11329-11341
-
(2005)
Biochemistry
, vol.44
, pp. 11329-11341
-
-
Pogozheva, I.D.1
Chai, B.X.2
Lomize, A.L.3
Fong, T.M.4
Weinberg, D.H.5
Nargund, R.P.6
Mulholland, M.W.7
Gantz, I.8
Mosberg, H.I.9
-
33
-
-
19444381366
-
Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states
-
Nickolls S.A., Fleck B., Hoare S.R., and Maki R.A. Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states. J Pharmacol Exp Ther 313 (2005) 1281-1288
-
(2005)
J Pharmacol Exp Ther
, vol.313
, pp. 1281-1288
-
-
Nickolls, S.A.1
Fleck, B.2
Hoare, S.R.3
Maki, R.A.4
-
34
-
-
0037456768
-
Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene
-
Farooqi I.S., Keogh J.M., Yeo G.S., Lank E.J., Cheetham T., and O'Rahilly S. Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene. N Engl J Med 348 (2003) 1085-1095
-
(2003)
N Engl J Med
, vol.348
, pp. 1085-1095
-
-
Farooqi, I.S.1
Keogh, J.M.2
Yeo, G.S.3
Lank, E.J.4
Cheetham, T.5
O'Rahilly, S.6
-
35
-
-
0037413580
-
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding
-
Arasasingham P.N., Fotsch C., Ouyang X., Norman M.H., Kelly M.G., Stark K.L., Karbon B., Hale C., Baumgartner J.W., Zambrano M., Cheetham J., and Tamayo N.A. Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding. J Med Chem 46 (2003) 9-11
-
(2003)
J Med Chem
, vol.46
, pp. 9-11
-
-
Arasasingham, P.N.1
Fotsch, C.2
Ouyang, X.3
Norman, M.H.4
Kelly, M.G.5
Stark, K.L.6
Karbon, B.7
Hale, C.8
Baumgartner, J.W.9
Zambrano, M.10
Cheetham, J.11
Tamayo, N.A.12
-
36
-
-
19944429810
-
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist-design, synthesis, and characterization
-
Chen C., Pontillo J., Fleck B.A., Gao Y., Wen J., Tran J.A., Tucci F.C., Marinkovic D., Foster A.C., and Saunders J. 4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist-design, synthesis, and characterization. J Med Chem 47 (2004) 6821-6830
-
(2004)
J Med Chem
, vol.47
, pp. 6821-6830
-
-
Chen, C.1
Pontillo, J.2
Fleck, B.A.3
Gao, Y.4
Wen, J.5
Tran, J.A.6
Tucci, F.C.7
Marinkovic, D.8
Foster, A.C.9
Saunders, J.10
-
37
-
-
21744461441
-
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]- 1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicycl o[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist
-
Ye Z., Guo L., Barakat K.J., Pollard P.G., Palucki B.L., Sebhat I.K., Bakshi R.K., Tang R., Kalyani R.N., Vongs A., Chen A.S., Chen H.Y., Rosenblum C.I., MacNeil T., Weinberg D.H., Peng Q., Tamvakopoulos C., Miller R.R., Stearns R.A., Cashen D.E., et al. Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]- 1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicycl o[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett 15 (2005) 3501-3505
-
(2005)
Bioorg Med Chem Lett
, vol.15
, pp. 3501-3505
-
-
Ye, Z.1
Guo, L.2
Barakat, K.J.3
Pollard, P.G.4
Palucki, B.L.5
Sebhat, I.K.6
Bakshi, R.K.7
Tang, R.8
Kalyani, R.N.9
Vongs, A.10
Chen, A.S.11
Chen, H.Y.12
Rosenblum, C.I.13
MacNeil, T.14
Weinberg, D.H.15
Peng, Q.16
Tamvakopoulos, C.17
Miller, R.R.18
Stearns, R.A.19
Cashen, D.E.20
more..
-
38
-
-
20144389154
-
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists
-
Palucki B.L., Park M.K., Nargund R.P., Tang R., MacNeil T., Weinberg D.H., Vongs A., Rosenblum C.I., Doss G.A., Miller R.R., Stearns R.A., Peng Q., Tamvakopoulos C., Van der Ploeg L.H., and Patchett A.A. 2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists. Bioorg Med Chem Lett 15 (2005) 1993-1996
-
(2005)
Bioorg Med Chem Lett
, vol.15
, pp. 1993-1996
-
-
Palucki, B.L.1
Park, M.K.2
Nargund, R.P.3
Tang, R.4
MacNeil, T.5
Weinberg, D.H.6
Vongs, A.7
Rosenblum, C.I.8
Doss, G.A.9
Miller, R.R.10
Stearns, R.A.11
Peng, Q.12
Tamvakopoulos, C.13
Van der Ploeg, L.H.14
Patchett, A.A.15
-
39
-
-
9644307848
-
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-pipe ridinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarbo xamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist
-
Palucki B.L., Park M.K., Nargund R.P., Ye Z., Sebhat I.K., Pollard P.G., Kalyani R.N., Tang R., Macneil T., Weinberg D.H., Vongs A., Rosenblum C.I., Doss G.A., Miller R.R., Stearns R.A., Peng Q., Tamvakopoulos C., McGowan E., Martin W.J., Metzger J.M., et al. Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-pipe ridinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarbo xamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett 15 (2005) 171-175
-
(2005)
Bioorg Med Chem Lett
, vol.15
, pp. 171-175
-
-
Palucki, B.L.1
Park, M.K.2
Nargund, R.P.3
Ye, Z.4
Sebhat, I.K.5
Pollard, P.G.6
Kalyani, R.N.7
Tang, R.8
Macneil, T.9
Weinberg, D.H.10
Vongs, A.11
Rosenblum, C.I.12
Doss, G.A.13
Miller, R.R.14
Stearns, R.A.15
Peng, Q.16
Tamvakopoulos, C.17
McGowan, E.18
Martin, W.J.19
Metzger, J.M.20
more..
-
40
-
-
20044395082
-
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides
-
Fotsch C., Han N., Arasasingham P., Bo Y., Carmouche M., Chen N., Davis J., Goldberg M.H., Hale C., Hsieh F.Y., Kelly M.G., Liu Q., Norman M.H., Smith D.M., Stec M., Tamayo N., Xi N., Xu S., Bannon A.W., and Baumgartner J.W. Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides. Bioorg Med Chem Lett 15 (2005) 1623-1627
-
(2005)
Bioorg Med Chem Lett
, vol.15
, pp. 1623-1627
-
-
Fotsch, C.1
Han, N.2
Arasasingham, P.3
Bo, Y.4
Carmouche, M.5
Chen, N.6
Davis, J.7
Goldberg, M.H.8
Hale, C.9
Hsieh, F.Y.10
Kelly, M.G.11
Liu, Q.12
Norman, M.H.13
Smith, D.M.14
Stec, M.15
Tamayo, N.16
Xi, N.17
Xu, S.18
Bannon, A.W.19
Baumgartner, J.W.20
more..
-
41
-
-
27644559821
-
Molecular interactions of nonpeptide agonists and antagonists with the melanocortin-4 receptor
-
Fleck B.A., Chen C., Yang W., Huntley R., Markison S., Nickolls S.A., Foster A.C., and Hoare S.R. Molecular interactions of nonpeptide agonists and antagonists with the melanocortin-4 receptor. Biochemistry 44 (2005) 14494-14508
-
(2005)
Biochemistry
, vol.44
, pp. 14494-14508
-
-
Fleck, B.A.1
Chen, C.2
Yang, W.3
Huntley, R.4
Markison, S.5
Nickolls, S.A.6
Foster, A.C.7
Hoare, S.R.8
-
42
-
-
0346729873
-
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core
-
Xi N., Hale C., Kelly M.G., Norman M.H., Stec M., Xu S., Baumgartner J.W., and Fotsch C. Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core. Bioorg Med Chem Lett 14 (2004) 377-381
-
(2004)
Bioorg Med Chem Lett
, vol.14
, pp. 377-381
-
-
Xi, N.1
Hale, C.2
Kelly, M.G.3
Norman, M.H.4
Stec, M.5
Xu, S.6
Baumgartner, J.W.7
Fotsch, C.8
-
43
-
-
12144285830
-
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model
-
Vos T.J., Caracoti A., Che J.L., Dai M., Farrer C.A., Forsyth N.E., Drabic S.V., Horlick R.A., Lamppu D., Yowe D.L., Balani S., Li P., Zeng H., Joseph I.B., Rodriguez L.E., Maguire M.P., Patane M.A., and Claiborne C.F. Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J Med Chem 47 (2004) 1602-1604
-
(2004)
J Med Chem
, vol.47
, pp. 1602-1604
-
-
Vos, T.J.1
Caracoti, A.2
Che, J.L.3
Dai, M.4
Farrer, C.A.5
Forsyth, N.E.6
Drabic, S.V.7
Horlick, R.A.8
Lamppu, D.9
Yowe, D.L.10
Balani, S.11
Li, P.12
Zeng, H.13
Joseph, I.B.14
Rodriguez, L.E.15
Maguire, M.P.16
Patane, M.A.17
Claiborne, C.F.18
-
44
-
-
0037057558
-
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist
-
Sebhat I.K., Martin W.J., Ye Z., Barakat K., Mosley R.T., Johnston D.B., Bakshi R., Palucki B., Weinberg D.H., MacNeil T., Kalyani R.N., Tang R., Stearns R.A., Miller R.R., Tamvakopoulos C., Strack A.M., McGowan E., Cashen D.E., Drisko J.E., Hom G.J., et al. Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. J Med Chem 45 (2002) 4589-4593
-
(2002)
J Med Chem
, vol.45
, pp. 4589-4593
-
-
Sebhat, I.K.1
Martin, W.J.2
Ye, Z.3
Barakat, K.4
Mosley, R.T.5
Johnston, D.B.6
Bakshi, R.7
Palucki, B.8
Weinberg, D.H.9
MacNeil, T.10
Kalyani, R.N.11
Tang, R.12
Stearns, R.A.13
Miller, R.R.14
Tamvakopoulos, C.15
Strack, A.M.16
McGowan, E.17
Cashen, D.E.18
Drisko, J.E.19
Hom, G.J.20
more..
-
45
-
-
0030761093
-
Molecular basis for the interaction of [Nle4,D-Phe7]melanocyte stimulating hormone with the human melanocortin-1 receptor
-
Yang Y., Dickinson C., Haskell-Luevano C., and Gantz I. Molecular basis for the interaction of [Nle4,D-Phe7]melanocyte stimulating hormone with the human melanocortin-1 receptor. J Biol Chem 272 (1997) 23000-23010
-
(1997)
J Biol Chem
, vol.272
, pp. 23000-23010
-
-
Yang, Y.1
Dickinson, C.2
Haskell-Luevano, C.3
Gantz, I.4
-
46
-
-
0030467905
-
Three-dimensional molecular models of the hMC1R melanocortin receptor: complexes with melanotropin peptide agonists
-
Haskell-Luevano C., Sawyer T.K., Trumpp-Kallmeyer S., Bikker J.A., Humblet C., Gantz I., and Hruby V.J. Three-dimensional molecular models of the hMC1R melanocortin receptor: complexes with melanotropin peptide agonists. Drug Des Discov 14 (1996) 197-211
-
(1996)
Drug Des Discov
, vol.14
, pp. 197-211
-
-
Haskell-Luevano, C.1
Sawyer, T.K.2
Trumpp-Kallmeyer, S.3
Bikker, J.A.4
Humblet, C.5
Gantz, I.6
Hruby, V.J.7
-
47
-
-
0027506471
-
The probable arrangement of the helices in G protein-coupled receptors
-
Baldwin J.M. The probable arrangement of the helices in G protein-coupled receptors. EMBO J 12 (1993) 1693-1703
-
(1993)
EMBO J
, vol.12
, pp. 1693-1703
-
-
Baldwin, J.M.1
-
48
-
-
0033553559
-
Contribution of melanocortin receptor exoloops to Agouti-related protein binding
-
Yang Y.K., Dickinson C.J., Zeng Q., Li J.Y., Thompson D.A., and Gantz I. Contribution of melanocortin receptor exoloops to Agouti-related protein binding. J Biol Chem 274 (1999) 14100-14106
-
(1999)
J Biol Chem
, vol.274
, pp. 14100-14106
-
-
Yang, Y.K.1
Dickinson, C.J.2
Zeng, Q.3
Li, J.Y.4
Thompson, D.A.5
Gantz, I.6
-
49
-
-
34547608426
-
Contribution of the conserved amino acids of the melanocortin-4 receptor in [corrected] [Nle4,D-Phe7]-alpha-melanocyte-stimulating [corrected] hormone binding and signaling
-
Chen M., Cai M., Aprahamian C.J., Georgeson K.E., Hruby V., Harmon C.M., and Yang Y. Contribution of the conserved amino acids of the melanocortin-4 receptor in [corrected] [Nle4,D-Phe7]-alpha-melanocyte-stimulating [corrected] hormone binding and signaling. J Biol Chem 282 (2007) 21712-21719
-
(2007)
J Biol Chem
, vol.282
, pp. 21712-21719
-
-
Chen, M.1
Cai, M.2
Aprahamian, C.J.3
Georgeson, K.E.4
Hruby, V.5
Harmon, C.M.6
Yang, Y.7
-
50
-
-
0024332759
-
Calculating receptor number from binding experiments using same compound as radioligand and competitor
-
DeBlasi A., O'Reilly K., and Motulsky H.J. Calculating receptor number from binding experiments using same compound as radioligand and competitor. Trends Pharmacol Sci 10 (1989) 227-229
-
(1989)
Trends Pharmacol Sci
, vol.10
, pp. 227-229
-
-
DeBlasi, A.1
O'Reilly, K.2
Motulsky, H.J.3
-
51
-
-
0031051101
-
Effects of recombinant agouti-signaling protein on melanocortin action
-
Yang Y.K., Ollmann M.M., Wilson B.D., Dickinson C., Yamada T., Barsh G.S., and Gantz I. Effects of recombinant agouti-signaling protein on melanocortin action. Mol Endocrinol 11 (1997) 274-280
-
(1997)
Mol Endocrinol
, vol.11
, pp. 274-280
-
-
Yang, Y.K.1
Ollmann, M.M.2
Wilson, B.D.3
Dickinson, C.4
Yamada, T.5
Barsh, G.S.6
Gantz, I.7
-
52
-
-
10844255054
-
Ryanodine receptor signaling is required for anti-CD3-induced T cell proliferation, interleukin-2 synthesis, and interleukin-2 receptor signaling
-
Conrad D.M., Hanniman E.A., Watson C.L., Mader J.S., and Hoskin D.W. Ryanodine receptor signaling is required for anti-CD3-induced T cell proliferation, interleukin-2 synthesis, and interleukin-2 receptor signaling. J Cell Biochem 92 (2004) 387-399
-
(2004)
J Cell Biochem
, vol.92
, pp. 387-399
-
-
Conrad, D.M.1
Hanniman, E.A.2
Watson, C.L.3
Mader, J.S.4
Hoskin, D.W.5
-
53
-
-
0030564894
-
Major pharmacological distinction of the ACTH receptor from other melanocortin receptors
-
Schioth H.B., Chhajlani V., Muceniece R., Klusa V., and Wikberg J.E. Major pharmacological distinction of the ACTH receptor from other melanocortin receptors. Life Sci 59 (1996) 797-801
-
(1996)
Life Sci
, vol.59
, pp. 797-801
-
-
Schioth, H.B.1
Chhajlani, V.2
Muceniece, R.3
Klusa, V.4
Wikberg, J.E.5
-
54
-
-
35048847904
-
Molecular identification of the human melanocortin-2 receptor responsible for ligand binding and signaling
-
Chen M., Aprahamian C.J., Kesterson R.A., Harmon C.M., and Yang Y. Molecular identification of the human melanocortin-2 receptor responsible for ligand binding and signaling. Biochemistry 46 (2007) 11389-11397
-
(2007)
Biochemistry
, vol.46
, pp. 11389-11397
-
-
Chen, M.1
Aprahamian, C.J.2
Kesterson, R.A.3
Harmon, C.M.4
Yang, Y.5
-
55
-
-
0037143744
-
A role for the melanocortin 4 receptor in sexual function
-
Van der Ploeg L.H., Martin W.J., Howard A.D., Nargund R.P., Austin C.P., Guan X., Drisko J., Cashen D., Sebhat I., Patchett A.A., Figueroa D.J., DiLella A.G., Connolly B.M., Weinberg D.H., Tan C.P., Palyha O.C., Pong S.S., MacNeil T., Rosenblum C., Vongs A., et al. A role for the melanocortin 4 receptor in sexual function. Proc Natl Acad Sci U S A 99 (2002) 11381-11386
-
(2002)
Proc Natl Acad Sci U S A
, vol.99
, pp. 11381-11386
-
-
Van der Ploeg, L.H.1
Martin, W.J.2
Howard, A.D.3
Nargund, R.P.4
Austin, C.P.5
Guan, X.6
Drisko, J.7
Cashen, D.8
Sebhat, I.9
Patchett, A.A.10
Figueroa, D.J.11
DiLella, A.G.12
Connolly, B.M.13
Weinberg, D.H.14
Tan, C.P.15
Palyha, O.C.16
Pong, S.S.17
MacNeil, T.18
Rosenblum, C.19
Vongs, A.20
more..
-
56
-
-
0036842081
-
Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula
-
Martin W.J., McGowan E., Cashen D.E., Gantert L.T., Drisko J.E., Hom G.J., Nargund R., Sebhat I., Howard A.D., Van der Ploeg L.H., and MacIntyre D.E. Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula. Eur J Pharmacol 454 (2002) 71-79
-
(2002)
Eur J Pharmacol
, vol.454
, pp. 71-79
-
-
Martin, W.J.1
McGowan, E.2
Cashen, D.E.3
Gantert, L.T.4
Drisko, J.E.5
Hom, G.J.6
Nargund, R.7
Sebhat, I.8
Howard, A.D.9
Van der Ploeg, L.H.10
MacIntyre, D.E.11
-
57
-
-
31544441358
-
Molecular characterization of human melanocortin-3 receptor ligand-receptor interaction
-
Chen M., Aprahamian C.J., Celik A., Georgeson K.E., Garvey W.T., Harmon C.M., and Yang Y. Molecular characterization of human melanocortin-3 receptor ligand-receptor interaction. Biochemistry 45 (2006) 1128-1137
-
(2006)
Biochemistry
, vol.45
, pp. 1128-1137
-
-
Chen, M.1
Aprahamian, C.J.2
Celik, A.3
Georgeson, K.E.4
Garvey, W.T.5
Harmon, C.M.6
Yang, Y.7
-
58
-
-
32344446277
-
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation
-
Hogan K., Peluso S., Gould S., Parsons I., Ryan D., Wu L., and Visiers I. Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. J Med Chem 49 (2006) 911-922
-
(2006)
J Med Chem
, vol.49
, pp. 911-922
-
-
Hogan, K.1
Peluso, S.2
Gould, S.3
Parsons, I.4
Ryan, D.5
Wu, L.6
Visiers, I.7
-
59
-
-
3042798261
-
Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function
-
Kristiansen K. Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function. Pharmacol Ther 103 (2004) 21-80
-
(2004)
Pharmacol Ther
, vol.103
, pp. 21-80
-
-
Kristiansen, K.1
-
60
-
-
0037036419
-
Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activity
-
Yang Y., Chen M., Lai Y., Gantz I., Georgeson K.E., and Harmon C.M. Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activity. J Biol Chem 277 (2002) 20328-20335
-
(2002)
J Biol Chem
, vol.277
, pp. 20328-20335
-
-
Yang, Y.1
Chen, M.2
Lai, Y.3
Gantz, I.4
Georgeson, K.E.5
Harmon, C.M.6
-
61
-
-
4143067936
-
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ"
-
Mutulis F., Yahorava S., Mutule I., Yahorau A., Liepinsh E., Kopantshuk S., Veiksina S., Tars K., Belyakov S., Mishnev A., Rinken A., and Wikberg J.E. New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J Med Chem 47 (2004) 4613-4626
-
(2004)
J Med Chem
, vol.47
, pp. 4613-4626
-
-
Mutulis, F.1
Yahorava, S.2
Mutule, I.3
Yahorau, A.4
Liepinsh, E.5
Kopantshuk, S.6
Veiksina, S.7
Tars, K.8
Belyakov, S.9
Mishnev, A.10
Rinken, A.11
Wikberg, J.E.12
-
62
-
-
0031035850
-
Dual agonistic and antagonistic property of nonpeptide angiotensin AT1 ligands: susceptibility to receptor mutations
-
Perlman S., Costa-Neto C.M., Miyakawa A.A., Schambye H.T., Hjorth S.A., Paiva A.C., Rivero R.A., Greenlee W.J., and Schwartz T.W. Dual agonistic and antagonistic property of nonpeptide angiotensin AT1 ligands: susceptibility to receptor mutations. Mol Pharmacol 51 (1997) 301-311
-
(1997)
Mol Pharmacol
, vol.51
, pp. 301-311
-
-
Perlman, S.1
Costa-Neto, C.M.2
Miyakawa, A.A.3
Schambye, H.T.4
Hjorth, S.A.5
Paiva, A.C.6
Rivero, R.A.7
Greenlee, W.J.8
Schwartz, T.W.9
|