메뉴 건너뛰기




Volumn 8, Issue 8, 2012, Pages 725-730

Mechanism of N-terminal modulation of activity at the melanocortin-4 receptor GPCR

Author keywords

[No Author keywords available]

Indexed keywords

AGOUTI RELATED PROTEIN; ALPHA INTERMEDIN; G PROTEIN COUPLED RECEPTOR; MELANOCORTIN 4 RECEPTOR;

EID: 84864290272     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.1008     Document Type: Article
Times cited : (55)

References (40)
  • 1
    • 3042798261 scopus 로고    scopus 로고
    • 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, 21-80 (2004).
    • (2004) Pharmacol. Ther. , vol.103 , pp. 21-80
    • Kristiansen, K.1
  • 2
    • 33947356279 scopus 로고    scopus 로고
    • G protein-coupled receptor structure and activation
    • Kobilka, B.K. G protein-coupled receptor structure and activation. Biochim. Biophys. Acta 1768, 794-807 (2007).
    • (2007) Biochim. Biophys. Acta , vol.1768 , pp. 794-807
    • Kobilka, B.K.1
  • 3
    • 42149181885 scopus 로고    scopus 로고
    • Structural diversity of G protein-coupled receptors and significance for drug discovery
    • Lagerström, M.C. & Schiöth, H.B. Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat. Rev. Drug Discov. 7, 339-357 (2008).
    • (2008) Nat. Rev. Drug Discov. , vol.7 , pp. 339-357
    • Lagerström, M.C.1    Schiöth, H.B.2
  • 4
    • 0026629249 scopus 로고
    • Tethered ligand agonist peptides Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function
    • Scarborough, R.M. et al. Tethered ligand agonist peptides. Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function. J. Biol. Chem. 267, 13146-13149 (1992).
    • (1992) J. Biol. Chem. , vol.267 , pp. 13146-13149
    • Scarborough, R.M.1
  • 5
    • 1542316313 scopus 로고    scopus 로고
    • A molecular dissection of the glycoprotein hormone receptors
    • Vassart, G., Pardo, L. & Costagliola, S. A molecular dissection of the glycoprotein hormone receptors. Trends Biochem. Sci. 29, 119-126 (2004).
    • (2004) Trends Biochem. Sci. , vol.29 , pp. 119-126
    • Vassart, G.1    Pardo, L.2    Costagliola, S.3
  • 6
    • 78650273555 scopus 로고    scopus 로고
    • Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling
    • Breit, A. et al. Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling. Mol. Cell. Endocrinol. 331, 232-240 (2011).
    • (2011) Mol. Cell. Endocrinol. , vol.331 , pp. 232-240
    • Breit, A.1
  • 7
    • 70349334681 scopus 로고    scopus 로고
    • In silico mutagenesis: A case study of the melanocortin 4 receptor
    • Bromberg, Y., Overton, J., Vaisse, C., Leibel, R.L. & Rost, B. In silico mutagenesis: A case study of the melanocortin 4 receptor. FASEB J. 23, 3059-3069 (2009).
    • (2009) FASEB J. , vol.23 , pp. 3059-3069
    • Bromberg, Y.1    Overton, J.2    Vaisse, C.3    Leibel, R.L.4    Rost, B.5
  • 8
    • 9644279627 scopus 로고    scopus 로고
    • Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans
    • Srinivasan, S. et al. Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans. J. Clin. Invest. 114, 1158-1164 (2004).
    • (2004) J. Clin. Invest. , vol.114 , pp. 1158-1164
    • Srinivasan, S.1
  • 9
    • 0036033424 scopus 로고    scopus 로고
    • Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors
    • Seifert, R. & Wenzel-Seifert, K. Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors. Naunyn Schmiedebergs Arch. Pharmacol. 366, 381-416 (2002).
    • (2002) Naunyn Schmiedebergs Arch. Pharmacol. , vol.366 , pp. 381-416
    • Seifert, R.1    Wenzel-Seifert, K.2
  • 10
    • 38449087113 scopus 로고    scopus 로고
    • In vivo evidence for inverse agonism of Agouti-related peptide in the central nervous system of proopiomelanocortin-deficient mice
    • Tolle, V. & Low, M.J. In vivo evidence for inverse agonism of Agouti-related peptide in the central nervous system of proopiomelanocortin- deficient mice. Diabetes 57, 86-94 (2008).
    • (2008) Diabetes , vol.57 , pp. 86-94
    • Tolle, V.1    Low, M.J.2
  • 11
    • 34447558562 scopus 로고    scopus 로고
    • Antibodies against the melanocortin-4 receptor act as inverse agonists in vitro and in vivo
    • Peter, J.C. et al. Antibodies against the melanocortin-4 receptor act as inverse agonists in vitro and in vivo. Am. J. Physiol. Regul. Integr. Comp. Physiol. 292, R2151-R2158 (2007).
    • (2007) Am. J. Physiol. Regul. Integr. Comp. Physiol. , vol.292
    • Peter, J.C.1
  • 12
    • 0030764741 scopus 로고    scopus 로고
    • Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
    • Ollmann, M.M. et al. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science 278, 135-138 (1997).
    • (1997) Science , vol.278 , pp. 135-138
    • Ollmann, M.M.1
  • 13
    • 0030614331 scopus 로고    scopus 로고
    • Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
    • Fan, W., Boston, B.A., Kesterson, R.A., Hruby, V.J. & Cone, R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 385, 165-168 (1997).
    • (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
  • 14
    • 0035130843 scopus 로고    scopus 로고
    • AgRP 83-132) acts as an inverse agonist on the human-melanocortin-4 receptor
    • Nijenhuis, W.A., Oosterom, J. & Adan, R.A. AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. Mol. Endocrinol. 15, 164-171 (2001).
    • (2001) Mol. Endocrinol. , Issue.15 , pp. 164-171
    • Nijenhuis, W.A.1    Oosterom, J.2    Adan, R.A.3
  • 15
    • 10744221862 scopus 로고    scopus 로고
    • Inverse agonist activity of agouti and agouti-related protein
    • Chai, B.X. et al. Inverse agonist activity of agouti and agouti-related protein. Peptides 24, 603-609 (2003).
    • (2003) Peptides , vol.24 , pp. 603-609
    • Chai, B.X.1
  • 16
    • 0001169515 scopus 로고
    • Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins
    • Costa, T. & Herz, A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86, 7321-7325 (1989).
    • (1989) Proc. Natl. Acad. Sci. USA , vol.86 , pp. 7321-7325
    • Costa, T.1    Herz, A.2
  • 17
    • 1642495639 scopus 로고    scopus 로고
    • Efficacy as a vector: The relative prevalence and paucity of inverse agonism
    • Kenakin, T. Efficacy as a vector: The relative prevalence and paucity of inverse agonism. Mol. Pharmacol. 65, 2-11 (2004).
    • (2004) Mol. Pharmacol. , vol.65 , pp. 2-11
    • Kenakin, T.1
  • 18
    • 78049429422 scopus 로고    scopus 로고
    • Loop-swapped chimeras of the agouti-related protein and the agouti signaling protein identify contacts required for melanocortin 1 receptor selectivity and antagonism
    • Patel, M.P. et al. Loop-swapped chimeras of the agouti-related protein and the agouti signaling protein identify contacts required for melanocortin 1 receptor selectivity and antagonism. J. Mol. Biol. 404, 45-55 (2010).
    • (2010) J. Mol. Biol. , vol.404 , pp. 45-55
    • Patel, M.P.1
  • 19
    • 77957055780 scopus 로고
    • Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors
    • Ballesteros, J.A. & Weinstein, H. Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors. Methods Neurosci. 25, 366-428 (1995).
    • (1995) Methods Neurosci. , vol.25 , pp. 366-428
    • Ballesteros, J.A.1    Weinstein, H.2
  • 20
    • 33646404622 scopus 로고    scopus 로고
    • Melanocortin 4 receptor mutations in a large cohort of severely obese adults: Prevalence, functional classification, genotype-phenotype relationship, and lack of association with binge eating
    • Lubrano-Berthelier, C. et al. Melanocortin 4 receptor mutations in a large cohort of severely obese adults: Prevalence, functional classification, genotype-phenotype relationship, and lack of association with binge eating. J. Clin. Endocrinol. Metab. 91, 1811-1818 (2006).
    • (2006) J. Clin. Endocrinol. Metab. , vol.91 , pp. 1811-1818
    • Lubrano-Berthelier, C.1
  • 21
    • 61849161252 scopus 로고    scopus 로고
    • Association of functionally significant Melanocortin-4 but not Melanocortin-3 receptor mutations with severe adult obesity in a large North American case-control study
    • Calton, M.A. et al. Association of functionally significant Melanocortin-4 but not Melanocortin-3 receptor mutations with severe adult obesity in a large North American case-control study. Hum. Mol. Genet. 18, 1140-1147 (2009).
    • (2009) Hum. Mol. Genet. , vol.18 , pp. 1140-1147
    • Calton, M.A.1
  • 22
    • 0035918601 scopus 로고    scopus 로고
    • 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. & 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, 6164-6179 (2001).
    • (2001) Biochemistry , vol.40 , pp. 6164-6179
    • Haskell-Luevano, C.1    Cone, R.D.2    Monck, E.K.3    Wan, Y.P.4
  • 23
    • 26444467486 scopus 로고    scopus 로고
    • Linking ligand binding to histamine H1 receptor activation
    • Jongejan, A. et al. Linking ligand binding to histamine H1 receptor activation. Nat. Chem. Biol. 1, 98-103 (2005).
    • (2005) Nat. Chem. Biol. , vol.1 , pp. 98-103
    • Jongejan, A.1
  • 24
    • 63849323943 scopus 로고    scopus 로고
    • Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-HT4 receptors
    • Pellissier, L.P. et al. Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-HT4 receptors. Mol. Pharmacol. 75, 982-990 (2009).
    • (2009) Mol. Pharmacol. , vol.75 , pp. 982-990
    • Pellissier, L.P.1
  • 25
    • 77950505038 scopus 로고    scopus 로고
    • A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors
    • Holst, B. et al. A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors. J. Biol. Chem. 285, 3973-3985 (2010).
    • (2010) J. Biol. Chem. , vol.285 , pp. 3973-3985
    • Holst, B.1
  • 26
    • 79953234218 scopus 로고    scopus 로고
    • Crystal structure of metarhodopsin II
    • Choe, H.W. et al. Crystal structure of metarhodopsin II. Nature 471, 651-655 (2011).
    • (2011) Nature , vol.471 , pp. 651-655
    • Choe, H.W.1
  • 27
    • 79953242234 scopus 로고    scopus 로고
    • The structural basis of agonist-induced activation in constitutively active rhodopsin
    • Standfuss, J. et al. The structural basis of agonist-induced activation in constitutively active rhodopsin. Nature 471, 656-660 (2011).
    • (2011) Nature , vol.471 , pp. 656-660
    • Standfuss, J.1
  • 28
    • 79954782236 scopus 로고    scopus 로고
    • Structure of an agonist-bound human A2A adenosine receptor
    • Xu, F. et al. Structure of an agonist-bound human A2A adenosine receptor. Science 332, 322-327 (2011).
    • (2011) Science , vol.332 , pp. 322-327
    • Xu, F.1
  • 29
    • 78651405537 scopus 로고    scopus 로고
    • The structural basis for agonist and partial agonist action on a β1-adrenergic receptor
    • Warne, T. et al. The structural basis for agonist and partial agonist action on a β1-adrenergic receptor. Nature 469, 241-244 (2011).
    • (2011) Nature , vol.469 , pp. 241-244
    • Warne, T.1
  • 30
    • 78651411166 scopus 로고    scopus 로고
    • Structure of a nanobody-stabilized active state of the β2 adrenoceptor
    • Rasmussen, S.G. et al. Structure of a nanobody-stabilized active state of the β2 adrenoceptor. Nature 469, 175-180 (2011).
    • (2011) Nature , vol.469 , pp. 175-180
    • Rasmussen, S.G.1
  • 31
    • 78651399683 scopus 로고    scopus 로고
    • Structure and function of an irreversible agonist-β2 adrenoceptor complex
    • Rosenbaum, D.M. et al. Structure and function of an irreversible agonist-β2 adrenoceptor complex. Nature 469, 236-240 (2011).
    • (2011) Nature , vol.469 , pp. 236-240
    • Rosenbaum, D.M.1
  • 32
    • 0037174606 scopus 로고    scopus 로고
    • β 2 adrenergic receptor activation modulation of the proline kink in transmembrane 6 by a rotamer toggle switch
    • Shi, L. et al. β2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch. J. Biol. Chem. 277, 40989-40996 (2002).
    • (2002) J. Biol. Chem. , vol.277 , pp. 40989-40996
    • Shi, L.1
  • 33
    • 20444499405 scopus 로고    scopus 로고
    • Probing the 2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists
    • Swaminath, G. et al. Probing the 2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J. Biol. Chem. 280, 22165-22171 (2005).
    • (2005) J. Biol. Chem. , vol.280 , pp. 22165-22171
    • Swaminath, G.1
  • 34
    • 11144246968 scopus 로고    scopus 로고
    • GPCR deorphanizations: The novel, the known and the unexpected transmitters
    • Civelli, O. GPCR deorphanizations: The novel, the known and the unexpected transmitters. Trends Pharmacol. Sci. 26, 15-19 (2005).
    • (2005) Trends Pharmacol. Sci. , vol.26 , pp. 15-19
    • Civelli, O.1
  • 35
    • 31844446495 scopus 로고    scopus 로고
    • Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery
    • Bond, R.A. & Ijzerman, A.P. Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery. Trends Pharmacol. Sci. 27, 92-96 (2006).
    • (2006) Trends Pharmacol. Sci. , vol.27 , pp. 92-96
    • Bond, R.A.1    Ijzerman, A.P.2
  • 36
    • 0033976851 scopus 로고    scopus 로고
    • Use of constitutive G protein-coupled receptor activity for drug discovery
    • Chen, G. et al. Use of constitutive G protein-coupled receptor activity for drug discovery. Mol. Pharmacol. 57, 125-134 (2000).
    • (2000) Mol. Pharmacol. , vol.57 , pp. 125-134
    • Chen, G.1
  • 37
    • 0034812072 scopus 로고    scopus 로고
    • The use of constitutively active receptors for drug discovery at the G protein-coupled receptor gene pool
    • Behan, D.P. & Chalmers, D.T. The use of constitutively active receptors for drug discovery at the G protein-coupled receptor gene pool. Curr. Opin. Drug Discov. Devel. 4, 548-560 (2001).
    • (2001) Curr. Opin. Drug Discov. Devel. , vol.4 , pp. 548-560
    • Behan, D.P.1    Chalmers, D.T.2
  • 38
    • 65549087559 scopus 로고    scopus 로고
    • The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity
    • Toyooka, M., Tujii, T. & Takeda, S. The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity. J. Neurosci. Res. 87, 1329-1333 (2009).
    • (2009) J. Neurosci. Res. , vol.87 , pp. 1329-1333
    • Toyooka, M.1    Tujii, T.2    Takeda, S.3
  • 39
    • 0037439274 scopus 로고    scopus 로고
    • Intracellular retention is a common characteristic of childhood obesity-associated MC4R mutations
    • Lubrano-Berthelier, C. et al. Intracellular retention is a common characteristic of childhood obesity-associated MC4R mutations. Hum. Mol. Genet. 12, 145-153 (2003).
    • (2003) Hum. Mol. Genet. , vol.12 , pp. 145-153
    • Lubrano-Berthelier, C.1
  • 40
    • 0033927916 scopus 로고    scopus 로고
    • Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity
    • Vaisse, C. et al. Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity. J. Clin. Invest. 106, 253-262 (2000).
    • (2000) J. Clin. Invest. , vol.106 , pp. 253-262
    • Vaisse, C.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.