메뉴 건너뛰기




Volumn 85, Issue 8, 2013, Pages 1162-1170

Signaling of an allosteric, nanomolar potent, low molecular weight agonist for the follicle-stimulating hormone receptor

Author keywords

Agonist; Allosterism; FSH receptor; Infertility; Ovary

Indexed keywords

ADENYLATE CYCLASE; CYCLIC AMP; DIHYDROPYRIDINE DERIVATIVE; ESTRADIOL; FERTILITY PROMOTING AGENT; FOLLICLE STIMULATING HORMONE RECEPTOR AGONIST; FOLLITROPIN; LUTEINIZING HORMONE RECEPTOR; ORG 2144440; PHOSPHOLIPASE C; RECOMBINANT FOLLITROPIN; THYROTROPIN RECEPTOR; UNCLASSIFIED DRUG;

EID: 84875212528     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2013.02.001     Document Type: Article
Times cited : (44)

References (42)
  • 1
    • 0033711033 scopus 로고    scopus 로고
    • Mutations of gonadotropins and gonadotropin receptors: Elucidating the physiology and pathophysiology of pituitary-gonadal function
    • A.P.N. Themmen, and I.T. Huhtaniemi Mutations of gonadotropins and gonadotropin receptors: elucidating the physiology and pathophysiology of pituitary-gonadal function Endocr Rev 21 2000 551 583
    • (2000) Endocr Rev , vol.21 , pp. 551-583
    • Themmen, A.P.N.1    Huhtaniemi, I.T.2
  • 3
    • 84874452235 scopus 로고    scopus 로고
    • The molecular basis of impaired follicle-stimulating hormone asction: Evidence from human mutations and mouse models
    • 10.1177/1933719112461184
    • E.T. Siegel, H.-G. Kim, H.K. Nishimoto, and L.C. Layman The molecular basis of impaired follicle-stimulating hormone asction: evidence from human mutations and mouse models Reprod Sci 2013 10.1177/1933719112461184
    • (2013) Reprod Sci
    • Siegel, E.T.1    Kim, H.-G.2    Nishimoto, H.K.3    Layman, L.C.4
  • 4
    • 0029118115 scopus 로고
    • Mutation in the follicle-stimulating hormone receptor gene causes hereditary hypergonadotropic ovarian failure
    • K. Aittomaki, J.L.D. Lucena, P. Pakarinen, P. Sistonen, J. Tapanainen, and J. Gromoll Mutation in the follicle-stimulating hormone receptor gene causes hereditary hypergonadotropic ovarian failure Cell 82 1995 959 968
    • (1995) Cell , vol.82 , pp. 959-968
    • Aittomaki, K.1    Lucena, J.L.D.2    Pakarinen, P.3    Sistonen, P.4    Tapanainen, J.5    Gromoll, J.6
  • 5
    • 0032190476 scopus 로고    scopus 로고
    • A novel phenotype related to partial loss of function mutations of the follicle stimulating hormone receptor
    • I. Beau, P. Touraine, G. Meduri, A. Gougeon, A. Desroches, and C. Matuchansky A novel phenotype related to partial loss of function mutations of the follicle stimulating hormone receptor J Clin Invest 102 1998 1352 1359
    • (1998) J Clin Invest , vol.102 , pp. 1352-1359
    • Beau, I.1    Touraine, P.2    Meduri, G.3    Gougeon, A.4    Desroches, A.5    Matuchansky, C.6
  • 6
    • 0033305435 scopus 로고    scopus 로고
    • New natural inactivating mutations of the follicle-stimulating hormone receptor: Correlations between receptor function and phenotype
    • P. Touraine, I. Beau, A. Gougeon, G. Meduri, A. Desroches, and C. Pichard New natural inactivating mutations of the follicle-stimulating hormone receptor: correlations between receptor function and phenotype Mol Endocrinol 13 1999 1844 1854
    • (1999) Mol Endocrinol , vol.13 , pp. 1844-1854
    • Touraine, P.1    Beau, I.2    Gougeon, A.3    Meduri, G.4    Desroches, A.5    Pichard, C.6
  • 8
    • 0036214841 scopus 로고    scopus 로고
    • Functional characterization of the human FSH receptor with an inactivating Ala189Val mutation
    • A. Rannikko, P. Pakarinen, P.R. Manna, I. Beau, M. Misrahi, and K. Aittomaki Functional characterization of the human FSH receptor with an inactivating Ala189Val mutation Mol Hum Reprod 8 2002 311 317
    • (2002) Mol Hum Reprod , vol.8 , pp. 311-317
    • Rannikko, A.1    Pakarinen, P.2    Manna, P.R.3    Beau, I.4    Misrahi, M.5    Aittomaki, K.6
  • 9
    • 0042384795 scopus 로고    scopus 로고
    • Delayed puberty and primary amenorrhea associated with a novel mutation of the human follicle-stimulating hormone receptor: Clinical, histological, and molecular studies
    • G. Meduri, P. Touraine, I. Beau, O. Lahuna, A. Desroches, and M.C. Vacher-Lavenu Delayed puberty and primary amenorrhea associated with a novel mutation of the human follicle-stimulating hormone receptor: clinical, histological, and molecular studies J Clin Endocrinol Metab 88 2003 3491 3498
    • (2003) J Clin Endocrinol Metab , vol.88 , pp. 3491-3498
    • Meduri, G.1    Touraine, P.2    Beau, I.3    Lahuna, O.4    Desroches, A.5    Vacher-Lavenu, M.C.6
  • 10
    • 0037323640 scopus 로고    scopus 로고
    • A novel loss of function mutation in exon 12 of the FSH receptor gene causing hypergonadotrophic hypogonadoism: Clinical and molecular characteristics
    • L.A. Allen, J.C. Achermann, P. Pakarinen, T.J. Kotlar, I.T. Huhtaniemi, and J.L. Jameson A novel loss of function mutation in exon 12 of the FSH receptor gene causing hypergonadotrophic hypogonadoism: clinical and molecular characteristics Hum Reprod 18 2003 251 256
    • (2003) Hum Reprod , vol.18 , pp. 251-256
    • Allen, L.A.1    Achermann, J.C.2    Pakarinen, P.3    Kotlar, T.J.4    Huhtaniemi, I.T.5    Jameson, J.L.6
  • 11
    • 1842376911 scopus 로고    scopus 로고
    • Men homozygous for an inactivating mutation of the follicle-stimulating hormone (FSH) receptor gene present variable suppression of spermatogenesis and fertility
    • J.S. Tapanainen, K. Aittimaki, J. Min, T. Vaskivou, and I.T. Huhtaniemi Men homozygous for an inactivating mutation of the follicle-stimulating hormone (FSH) receptor gene present variable suppression of spermatogenesis and fertility Nat Genet 15 1997 205 206
    • (1997) Nat Genet , vol.15 , pp. 205-206
    • Tapanainen, J.S.1    Aittimaki, K.2    Min, J.3    Vaskivou, T.4    Huhtaniemi, I.T.5
  • 13
    • 24944502148 scopus 로고    scopus 로고
    • Specificity and primiscuity of gonadotropin receptors
    • S. Costagliola, E. Urizar, F. Mendive, and G. Vassart Specificity and primiscuity of gonadotropin receptors Reproduction 130 2005 275 281
    • (2005) Reproduction , vol.130 , pp. 275-281
    • Costagliola, S.1    Urizar, E.2    Mendive, F.3    Vassart, G.4
  • 14
    • 1542316313 scopus 로고    scopus 로고
    • A molecular dissection of the glycoprotein hormone receptors
    • G. Vassart, L. Pardo, and S. Costagliola A molecular dissection of the glycoprotein hormone receptors Trends Biochem Sci 29 2004 119 126
    • (2004) Trends Biochem Sci , vol.29 , pp. 119-126
    • Vassart, G.1    Pardo, L.2    Costagliola, S.3
  • 15
    • 75249105588 scopus 로고    scopus 로고
    • The hinge region: An important receptor component for GPHR function
    • S. Müller, H. Jaeschke, R. Günther, and R. Paschke The hinge region: an important receptor component for GPHR function Trends Pharmacol Sci 21 2009 111 122
    • (2009) Trends Pharmacol Sci , vol.21 , pp. 111-122
    • Müller, S.1    Jaeschke, H.2    Günther, R.3    Paschke, R.4
  • 16
    • 84864502784 scopus 로고    scopus 로고
    • Structure of follicle-stimulating hormone in complex with the entire ectodomain of its receptor
    • X. Jiang, H. Liu, X. Chen, D. Fischer, V. Sriraman, and H.N. Yu Structure of follicle-stimulating hormone in complex with the entire ectodomain of its receptor Proc Natl Acad Sci USA 109 2012 12491 12496
    • (2012) Proc Natl Acad Sci USA , vol.109 , pp. 12491-12496
    • Jiang, X.1    Liu, H.2    Chen, X.3    Fischer, D.4    Sriraman, V.5    Yu, H.N.6
  • 17
    • 0034455591 scopus 로고    scopus 로고
    • Differentiation of granulosa cell line: Follicle stimulating hormone induces formation of lamellipodia and filopodia via the adenylyl cyclase/cyclic adenosine monophosphate signal
    • N.A. Grieshaber, S. Boitano, I. Ji, J.P. Mather, and T.H. Ji Differentiation of granulosa cell line: follicle stimulating hormone induces formation of lamellipodia and filopodia via the adenylyl cyclase/cyclic adenosine monophosphate signal Endocrinology 141 2000 3461 3470
    • (2000) Endocrinology , vol.141 , pp. 3461-3470
    • Grieshaber, N.A.1    Boitano, S.2    Ji, I.3    Mather, J.P.4    Ji, T.H.5
  • 18
    • 48249155876 scopus 로고    scopus 로고
    • Constitutively active protein kinase A qualitatively mimics the effects of follicle-stimulating hormone on granulosa cells
    • R. Escamilla-Hernandez, L. Little-Ihrig, K.E. Orwig, J. Yue, U. Chandran, and A.J. Zelznik Constitutively active protein kinase A qualitatively mimics the effects of follicle-stimulating hormone on granulosa cells Mol Endocrinol 22 2008 1842 1852
    • (2008) Mol Endocrinol , vol.22 , pp. 1842-1852
    • Escamilla-Hernandez, R.1    Little-Ihrig, L.2    Orwig, K.E.3    Yue, J.4    Chandran, U.5    Zelznik, A.J.6
  • 19
    • 33751509646 scopus 로고    scopus 로고
    • A phosphorylation cluster of five serine and threonine residues in the C-terminus of the follicle-stimulating hormone receptor is important for desensitization but not for β-arrestin-mediated ERK activation
    • E. Kara, P. Crepieux, C. Gauthier, N. Martinat, V. Piketty, and F. Guiilou A phosphorylation cluster of five serine and threonine residues in the C-terminus of the follicle-stimulating hormone receptor is important for desensitization but not for β-arrestin-mediated ERK activation Mol Endocrinol 20 2006 3014 3026
    • (2006) Mol Endocrinol , vol.20 , pp. 3014-3026
    • Kara, E.1    Crepieux, P.2    Gauthier, C.3    Martinat, N.4    Piketty, V.5    Guiilou, F.6
  • 20
    • 23844456672 scopus 로고    scopus 로고
    • The differential effects of the gonadotropin receptors on aromatase expression in primary cultures of immature rat granulosa cells are highly dependent on the density of receptors expressed and the activation of the inositol phosphate cascade
    • F.X. Donadeu, and M. Ascoli The differential effects of the gonadotropin receptors on aromatase expression in primary cultures of immature rat granulosa cells are highly dependent on the density of receptors expressed and the activation of the inositol phosphate cascade Endocrinology 146 2005 3907 3916
    • (2005) Endocrinology , vol.146 , pp. 3907-3916
    • Donadeu, F.X.1    Ascoli, M.2
  • 21
    • 0029774791 scopus 로고    scopus 로고
    • The C-terminal third of the human luteinizing hormone (LH) receptor is important for inositol phosphate release: Analysis using chimeric human LH/follicle-stimulating hormone receptors
    • B. Hirsch, M. Kudo, F. Naro, M. Conti, and A.J.W. Hsueh The C-terminal third of the human luteinizing hormone (LH) receptor is important for inositol phosphate release: analysis using chimeric human LH/follicle-stimulating hormone receptors Mol Endocrinol 10 1996 1127 1137
    • (1996) Mol Endocrinol , vol.10 , pp. 1127-1137
    • Hirsch, B.1    Kudo, M.2    Naro, F.3    Conti, M.4    Hsueh, A.J.W.5
  • 23
    • 12144286406 scopus 로고    scopus 로고
    • Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis
    • T. Guo, A.E. Adang, R.E. Dolle, G. Dong, D. Fitzpatrick, and P. Geng Small molecule biaryl FSH receptor agonists. Part 1: lead discovery via encoded combinatorial synthesis Bioorg Med Chem Lett 14 2004 1713 1716
    • (2004) Bioorg Med Chem Lett , vol.14 , pp. 1713-1716
    • Guo, T.1    Adang, A.E.2    Dolle, R.E.3    Dong, G.4    Fitzpatrick, D.5    Geng, P.6
  • 24
    • 12144290509 scopus 로고    scopus 로고
    • Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis
    • T. Guo, A.E. Adang, G. Dong, D. Fitzpatrick, P. Geng, and K.K. Ho Small molecule biaryl FSH receptor agonists. Part 2: lead optimization via parallel synthesis Bioorg Med Chem Lett 14 2004 1717 1720
    • (2004) Bioorg Med Chem Lett , vol.14 , pp. 1717-1720
    • Guo, T.1    Adang, A.E.2    Dong, G.3    Fitzpatrick, D.4    Geng, P.5    Ho, K.K.6
  • 27
    • 25844499772 scopus 로고    scopus 로고
    • Preparation of highly substituted β-lactam follicle stimulating hormone receptor agonists
    • J.C. Pelletier, J. Rogers, J. Wrobel, M.C. Perez, and E.S. Shen Preparation of highly substituted β-lactam follicle stimulating hormone receptor agonists Bioorg Med Chem 13 2005 5986 5995
    • (2005) Bioorg Med Chem , vol.13 , pp. 5986-5995
    • Pelletier, J.C.1    Rogers, J.2    Wrobel, J.3    Perez, M.C.4    Shen, E.S.5
  • 28
    • 33745608074 scopus 로고    scopus 로고
    • 5-Alkylated thiazolidinones as follicle-stimulating hormone (FSH) receptor agonists
    • J. Wrobel, J. Jetter, W. Kao, J. Rogers, L. Di, and J. Chi 5-Alkylated thiazolidinones as follicle-stimulating hormone (FSH) receptor agonists Bioorg Med Chem 14 2006 5729 5741
    • (2006) Bioorg Med Chem , vol.14 , pp. 5729-5741
    • Wrobel, J.1    Jetter, J.2    Kao, W.3    Rogers, J.4    Di, L.5    Chi, J.6
  • 29
    • 33744964702 scopus 로고    scopus 로고
    • Allosteric activation of the follicle-stimulating hormone (FSH) receptor by selective, nonpeptide agonists
    • S.D. Yanofski, E.S. Shen, F. Holden, E. Whitehorn, B. Aguilar, and E. Tate Allosteric activation of the follicle-stimulating hormone (FSH) receptor by selective, nonpeptide agonists J Biol Chem 281 2006 13226 13233
    • (2006) J Biol Chem , vol.281 , pp. 13226-13233
    • Yanofski, S.D.1    Shen, E.S.2    Holden, F.3    Whitehorn, E.4    Aguilar, B.5    Tate, E.6
  • 30
    • 80055022606 scopus 로고    scopus 로고
    • Non-peptide ligands for the gonadotropin receptors
    • N.C.R. Van Straten, and C.M. Timmers Non-peptide ligands for the gonadotropin receptors Annu Rep Med Chem 44 2009 171 188
    • (2009) Annu Rep Med Chem , vol.44 , pp. 171-188
    • Van Straten, N.C.R.1    Timmers, C.M.2
  • 31
    • 20144367831 scopus 로고    scopus 로고
    • Identification of substituted 6-amino-4 phenytetrahydroquinoline derivatives: Potent antagonists for the follicle-stimulating hormone receptor
    • N.C.R. Van Straten, T.H.J. van Berkel, D.R. Demont, W.J.F. Karstens, R. Merkx, and J. Oosterom Identification of substituted 6-amino-4 phenytetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor J Med Chem 48 2005 1697 1700
    • (2005) J Med Chem , vol.48 , pp. 1697-1700
    • Van Straten, N.C.R.1    Van Berkel, T.H.J.2    Demont, D.R.3    Karstens, W.J.F.4    Merkx, R.5    Oosterom, J.6
  • 33
    • 84858170565 scopus 로고    scopus 로고
    • Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor
    • C.J. Van Koppen, M.E. Gooyer, W.J. Karstens, R. Plate, P. Conti, and T.A.E. Van Achterberg Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor Br J Pharmacol 165 2012 2314 2324
    • (2012) Br J Pharmacol , vol.165 , pp. 2314-2324
    • Van Koppen, C.J.1    Gooyer, M.E.2    Karstens, W.J.3    Plate, R.4    Conti, P.5    Van Achterberg, T.A.E.6
  • 34
    • 77952354490 scopus 로고    scopus 로고
    • Seven transmembrane receptors as shapeshifting protein: The impact of allosteric modulation and functional selectivity on new drug discovery
    • T. Kenakin, and L.J. Miller Seven transmembrane receptors as shapeshifting protein: the impact of allosteric modulation and functional selectivity on new drug discovery Pharmacol Rev 62 2010 265 304
    • (2010) Pharmacol Rev , vol.62 , pp. 265-304
    • Kenakin, T.1    Miller, L.J.2
  • 35
    • 0026042543 scopus 로고
    • Expression of human luteinizing hormone (LH) receptor: Interaction with LH and chorionic gonadotropin from human but not equine, rat and ovine
    • X.C. Jia, M. Oikawa, M. Bo, T. Tanaka, T. Ny, and I. Boime Expression of human luteinizing hormone (LH) receptor: interaction with LH and chorionic gonadotropin from human but not equine, rat and ovine Mol Endocrinol 5 1991 759 768
    • (1991) Mol Endocrinol , vol.5 , pp. 759-768
    • Jia, X.C.1    Oikawa, M.2    Bo, M.3    Tanaka, T.4    Ny, T.5    Boime, I.6
  • 37
    • 0041966031 scopus 로고    scopus 로고
    • A chorionic gonadotropin-sensitive mutation in the follicle-stimulating hormone receptor as a cause of familial gestational spontaneous ovarian hyperstimulation syndrome
    • C. Vasseur, P. Rodien, I. Beau, A. Desroches, C. Gérard, and L. de Poncheville A chorionic gonadotropin-sensitive mutation in the follicle-stimulating hormone receptor as a cause of familial gestational spontaneous ovarian hyperstimulation syndrome N Engl J Med 349 2003 753 759
    • (2003) N Engl J Med , vol.349 , pp. 753-759
    • Vasseur, C.1    Rodien, P.2    Beau, I.3    Desroches, A.4    Gérard, C.5    De Poncheville, L.6
  • 38
    • 1642294189 scopus 로고    scopus 로고
    • A mutation in the follicle-stimulating hormone receptor as a cause of familial spontaneous ovarian hyperstimulation syndrome
    • L. Montanelli, A. Delbaere, C. Di Carlo, C. Nappi, G. Smits, and G. Vassart A mutation in the follicle-stimulating hormone receptor as a cause of familial spontaneous ovarian hyperstimulation syndrome J Clin Endocrinol Metab 89 2004 1255 1258
    • (2004) J Clin Endocrinol Metab , vol.89 , pp. 1255-1258
    • Montanelli, L.1    Delbaere, A.2    Di Carlo, C.3    Nappi, C.4    Smits, G.5    Vassart, G.6
  • 39
    • 0037077222 scopus 로고    scopus 로고
    • Identification of a short linear sequence present in the C terminal tail of the rat follitropin receptor that modulates arrestin-3 binding in a phosphorylation-independent fashion
    • H. Kishi, H. Krishnamurthy, C. Galet, R.S. Bhaskaran, and M. Ascoli Identification of a short linear sequence present in the C terminal tail of the rat follitropin receptor that modulates arrestin-3 binding in a phosphorylation-independent fashion J Biol Chem 277 2002 21939 21946
    • (2002) J Biol Chem , vol.277 , pp. 21939-21946
    • Kishi, H.1    Krishnamurthy, H.2    Galet, C.3    Bhaskaran, R.S.4    Ascoli, M.5
  • 40
    • 33747890133 scopus 로고    scopus 로고
    • G protein-coupled receptor kinase 2 and β-arrestins are recruited to FSH receptor in stimulated rat primary Sertoli cells
    • S. Marion, E. Kara, P. Crepieux, V. Piketty, N. Martinat, and F. Guillo G protein-coupled receptor kinase 2 and β-arrestins are recruited to FSH receptor in stimulated rat primary Sertoli cells J Endocrinol 190 2006 341 350
    • (2006) J Endocrinol , vol.190 , pp. 341-350
    • Marion, S.1    Kara, E.2    Crepieux, P.3    Piketty, V.4    Martinat, N.5    Guillo, F.6
  • 41
    • 82355164267 scopus 로고    scopus 로고
    • Contraception by induction of luteinized unruptured follicles with short-acting low molecular weight FSH receptor agonists in female animal models
    • R. Van de Lagemaat, C.J. Van Koppen, M.A.M. Krajnc-Franken, B.J.B. Folmer, H.A. Van Diepen, and S.M. Mulders Contraception by induction of luteinized unruptured follicles with short-acting low molecular weight FSH receptor agonists in female animal models Reproduction 142 2011 893 905
    • (2011) Reproduction , vol.142 , pp. 893-905
    • Van De Lagemaat, R.1    Van Koppen, C.J.2    Krajnc-Franken, M.A.M.3    Folmer, B.J.B.4    Van Diepen, H.A.5    Mulders, S.M.6
  • 42
    • 84875228377 scopus 로고    scopus 로고
    • Generic assays in G protein-coupled receptor drug discovery
    • C.J. Van Koppen Generic assays in G protein-coupled receptor drug discovery Drug Discovery 7 2010 69 71
    • (2010) Drug Discovery , vol.7 , pp. 69-71
    • Van Koppen, C.J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.