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Review

Small molecule agonists and antagonists for the LH and FSH receptors

Pages 1555-1564 | Published online: 28 Oct 2005

Bibliography

  • PIERCE JG, PARSONS TF: Glycoprotein hormones: structure and function. Ann. Rev. Biochem. (1981) 50:465–495.
  • •Review of glycoprotein hormones.
  • FIDDES JC, TALMADGE K: Structure, expression, and evolution of the genes for the human glycoprotein hormones. Recent Prog Horm. Res. (1984) 40:43–78.
  • WU H, LUSTBADER JW, LIU Y, CANFIELD RE, HENDRICKSON WA: Structure of human chorionic gonadotropin at 2.6 A resolution from MAD analysis of the selenomethionyl protein. Structure (1994) 2:545–558.
  • LAPTHORN AJ, HARRIS DC, LITTLEJOHN A et al.: Crystal structure of human chorionic gonadotropin. Nature (1994) 369:455–461.
  • FOX KM, DIAS JA, VAN ROEY P: Three-dimensional structure of human follicle-stimulating hormone. Mol. Endocrinol. (2001) 15:378–389.
  • SIMONI M, GROMOLL J, NIESCHLAG E: The follicle-stimulating hormone receptor: biochemistry, molecular biology, physiology, and pathophysiology. Endocr. Rev. (1997) 18:739–773.
  • •Review of the FSH signaling pathway.
  • DIAS JA, COHEN BD, LINDAU -SHEPARD B et al.: Molecular, structural, and cellular biology of follitropin and follitropin receptor. vitam. Horm. (2002) 64:249–322.
  • SZKUDLINSKI MW, FREMONT V RONIN C, WEINTRAUB BD: Thyroid -stimulating hormone and thyroid-stimulating hormone receptor structure-function relationships. PhysioL Rev. (2002) 82:473–502.
  • ASCOLI M, FANELLI F, SEGALOFF DL: The lutropin/choriogonadotropin receptor, a 2002 perspective. Endocr. Rev. (2002) 23:141–174.
  • •Review of the LH signaling pathway.
  • STRADER CD, FONG TM, TOTA MR, et al.: Structure and function of G protein coupled receptors. Ann. Rev. Biochem. (1994) 63:101–132.
  • FAN QR, HENDRICKSON WA: Structure of human follicle-stimulating hormone in complex with its receptor. Nature (2005) 433:269–277.
  • BRAUN T, SCHOFIELD PR, SPRENGEL R: Amino-terminal leucine-rich repeats in gonadotropin receptors determine hormone selectivity. EMBO J. (1991) 10:1885–1890.
  • DUFAU ML, CATT KJ: Gonadotropin receptors and regulation of steroidogenesis in the testis and ovary. Vitam. Horm. (1978) 36:461–592.
  • DORRINGTON JH, ARMSTRONG DT: Effects of FSH on gonadal functions. Recent Frog. Horm. Res. (1979) 35:301–342.
  • ERICKSON GF, MAGOFFIN DA, DYER CA, HOFEDITZ C: The ovarian androgen producing cells: a review of structure/function relationships. Endocr. Rev. (1985) 6:371–399.
  • THEMMEN APN, HUHTANIEMI IT: Mutations of gonadotropins and gonadotropin receptors: elucidating the physiology and pathophysiology of pituitary-gonadal function. Endocr. Rev. (2000) 21:551–583.
  • •Review of LH and FSH functions.
  • PLANT TM, MARSHALL GR: The functional significance of FSH in spermatogenesis and the control of its secretion in male primates. Endocr. Rev. (2001) 22:764–786.
  • MAX, DONG Y, MATZUK MM, KUMAR TR: Targeted disruption of luteinizing hormone 0-subunit leads to hypogonadism, defects in gonadal steroidogenesis, and infertility. Proc. Natl Acad. Sci. USA (2004) 101:17294–17299.
  • ZHANG FP, POUTANEN M, WILBERTZ J, HUHTANIEMI I: Normal prenatal but arrested postnatal sexual development of luteinizing hormone receptor knockout (LuRKO) mice. MoL Endocrinol (2001) 15:172–183.
  • LEI ZM, MISHRA S, ZOU Wet al.: Targeted disruption of luteinizing hormone/human chorionic gonadotropin receptor gene. MoL Endocrinol (2001) 15:184–200.
  • ABEL MH, HUHTANIEMI I, PAKARINEN P, KUMAR TR, CHARLTON HM: Age-related uterine and ovarian hypertrophy in FSH receptor knockout and FSH0 subunit knockout mice. Reproduction (2003) 125: 165–173.
  • ABEL MH, WOOTTON AN, WILKINS Vet al.: The effect of a null mutation in the follicle-stimulating hormone receptor gene on mouse reproduction. Endocrinology (2000) 141:1795–1803.
  • DANILOVICH N, BABU PS, XING W et al.: Estrogen deficiency, obesity, and skeletal abnormalities in follicle-stimulating hormone receptor knockout (FORKO) female mice. Endocrinology (2000) 141:4295–4308.
  • KUMAR TR, WANG Y, LU N, MATZUK MM: Follicle stimulating hormone is required for ovarian follicle maturation but not male fertility. Nat. Genet. (1997) 15:201–204.
  • KRISHNAMURTHY H, DANILOVICH N, MORALES CR, SAIRAM MR: Qualitative and quantitative decline in spermatogenesis of the follicle-stimulating hormone receptor knockout (FORKO) mouse. Biol. Reprod. (2000) 62:1146–1159.
  • GROVER A, SMITH CE, GREGORY M et al.: Effects of FSH receptor deletion on epididymal tubules and sperm morphology, numbers, and motility. Mol Reprod. Develop. (2005) 72: 135–144.
  • TAPANAINEN JS, AITTOMAKI K, MIN J, VASKIVUO T, HUHTANIEMI IT: Men homozygous for an inactivating mutation of the follicle-stimulating hormone (FSH) receptor gene present variable suppression of spermatogenesis and fertility. Nat. Genet. (1997) 15:205–206.
  • PALAGIANO A, NESTI E, PACE L: FSH: urinary and recombinant. Eur. J. Obstet. Gynecol Reprod. Biol. (2004) 115:S30–S33.
  • INSLER V: Gonadotropin therapy: new trends and insights. Internad j Fertil (1988) 33:85–97.
  • NAVOT D, ROSENWAKS Z: The use of follicle-stimulating hormone for controlled ovarian hyperstimulation in in vitro fertilization. J. In Vitro Fertil Embryo lransfer (1988) 5:3–13.
  • MORSE JH, LUSTBADER JW, HARRINGTON JW, CANFIELD RE: Heterogeneity of proteins in commercial preparations of human chorionic gonadotropin (hCG) demonstrated by western blotting. Am. J. Reprod. Immunol Microbiol (1988) 17:134–140.
  • WIESAK T: Role of LH in controlled ovarian stimulation. Reprod. Biol. (2002) 2:215–227.
  • COHEN J: A short review of ovarian stimulation in assisted reproductive techniques. Reprod. Biomed. (2003) 6:361–366.
  • HULL M: Experience with F.S.H. treatment alone in an I.V.F. program. World Congress on In vitro Fertilization and Assisted Reproduction, 9th. Vienna (3–7 April 1995):77–82.
  • MARRS R, MELDRUM D, MUASHER S et al: Randomized trial to compare the effect of recombinant human FSH (follitropin alfa) with or without recombinant human LH in women undergoing assisted reproduction treatment. Reprod. Biomed. Online (2004) 8:175–182.
  • CHAPPEL S: Biochemical and biological characterization of LH and FSH expressed by recombinant DNA technology. In: Molecular Biology of Brain and Endocrine Peptidergic Systems. Chretien M, McKerns KW (Eds) Plenum Publishing, NY, USA (1988):275–288.
  • GLASIER A: Contraception - past and future. Nat. Cell Biol. Nat. Med. Fend. Suppl. (2002) S3–S6.
  • •Review of contraception.
  • POTTS M: The myth of a male pill. Nat. Med. (1996) 2:398–399.
  • GLASIER AF, ANAKWE R, EVERINGTON D et al: Would women trust their partners to use a male pill? Hum. Reprod. (2000) 15:646–649.
  • BRADY BM, ANDERSON RA: Advances in male contraception. Expert Opin. Investig. Drugs (2002) 11:333–344.
  • SUGG EE: Nonpeptide agonists for peptide receptors: lessons from ligands. Ann. Rep. Med. Chem. (1997) 32:277–283.
  • BEELEY NR: Can peptides be mimicked? Drug Discov. Today (2000) 5:354–363.
  • BRASIER A. TATE J, HABENER J: Optimized use of the firefly luciferase assay as a reporter gene in mammalian cell lines. BioTechniques (1989) 7:1116–1122.
  • BENZAKOUR 0, KANTHOU C, DENNEHY U et al.: Evaluation of the use of the luciferase-reporter-gene system for gene-regulation studies involving cyclic AMP-elevating agents. Biochem. J. (1995) 309:385–387.
  • DOLLE RE: Comprehensive survey of combinatorial library synthesis: 2003. J. Comb. Chem. (2004) 6:623–679.
  • DOLLE RE: Comprehensive survey of combinatorial library synthesis: 2002. J. Comb. Chem. (2003) 5:693–753.
  • DOLLE RE: Comprehensive survey of combinatorial library synthesis: 2001. J. Comb. Chem. (2002) 4:369–418.
  • DOLLE RE: Comprehensive survey of combinatorial library synthesis: 2000. J. Comb. Chem. (2001) 3:477–517.
  • DOLLE RE: Comprehensive survey of combinatorial library synthesis: 1999. J. Comb. Chem. (2000) 2:383–433.
  • DOLLE RE, NELSON KH JR: Comprehensive survey of combinatorial library synthesis: 1998.1 Comb. Chem. (1999) 1:235–282.
  • DOLLE RE: Comprehensive survey of chemical libraries yielding enzyme inhibitors, receptor agonists and antagonists, and other biologically active agents: 1992 through 1997. Mol Divers. (1998) 3:199–233.
  • VAN STRATEN NC, SCHOONUS -GERRITSMA GG, VAN SOMEREN RG et al.: The first orally active low molecular weight agonists for the LH receptor: thienopyr(im)idines with therapeutic potential for ovulation induction. ChemBioChem (2002) 3:1023–1026.
  • ••First report of low molecular weight orallyactive LHR agonists.
  • JORAND-LEBRUN C, BRUGGER N, SHROFF H et al.: Pyrazole derivatives as new LH receptor agonists. 226th ACS Meeting New York, USA (2003) MEDI320.
  • ALOUSI AA, STANKUS GP, STUART JC, WALTON LH: Characterization of the cardiotonic effects of milrinone, a new and potent cardiac bipyridine, on isolated tissues from several animal species. J. Cardiovasc. Pharmacol. (1983) 5:804–811.
  • KAUFFMAN RF, ROBERTSON DW, FRANKLIN RB et al.: Indolidan: a potent, long-acting cardiotonic and inhibitor of Type IV cyclic AMP phosphodiesterase. Cardiovasc. Drug Rev. (1990) 8:303–322.
  • MCKENNA SD, PIETROPAOLO M, TOS EG et al.: Pharmacological inhibition of phosphodiesterase 4 triggers ovulation in follicle-stimulating hormone-primed rats. Endocrinology (2005) 146:208–214.
  • MACLEAN D, HOLDEN F, DAVIS AM et al.: Agonists of the follicle stimulating hormone receptor from an encoded thiazolidinone library. 1 Comb. Chem. (2004) 6:196–206.
  • JETTER J, KAO W, ROGERS Jet al.: Synthesis and in vitro biology of novel 5-alkylated thiazolidinones as FSH agonists. 226th ACS Meeting, New York, USA (2003) MEDI319.
  • PELLETIER JC, ROGERS J, WROBEL J, SHEN E, MEADE E: Highly substituted gamma lactam follicle stimulating hormone (FSH) agonists from y lactones: a one-pot, two-step stereoselective method involving Weinreb amidation and the Mitsunobu reaction. 226th ACS Meeting, New York, USA (2003) MEDI318.
  • GUO T, ADANG AEP, DOLLE RE et al.: Small molecule biaryl FSH receptor agonists. Part 1. Lead discovery via encoded combinatorial synthesis. Bioorg. Med. Chem. Lett. (2004) 14:1713–1716.
  • GUO T, ADANG AEP, DONG G et ell.: Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis. Bioorg Med. Chem. Lett. (2004) 14:1717–1720.
  • VAN STRATEN NCR, VAN BERKEL TH, DEMONT DR et ell.: Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor. J. Med. Chem. (2005) 48:1697–1700.
  • AREY BJ, DEECHER DC, SHEN ES et al.: Identification and characterization of a selective, nonpeptide follicle-stimulating hormone receptor antagonist. Endocrinology (2002) 143:3822–3829.
  • WROBEL J, GREEN D, JETTER J et al.:Synthesis of (bis)sulfonic acid, (bis)benzamides as follicle-stimulating hormone (FSH) antagonists. Bioorg. Med. Chem. (2002) 10:639–656.

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