Gonadotropin and TSH Receptors

Roux, Nicolas; Doeker, Beate; Milgröm, Edwin

doi:10.1007/978-1-4757-3600-7_10

Cited by 1 publication

(3 citation statements)

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“…Luteinizing hormone/choriogonadotropin (LH/CG), follicle-stimulating hormone (FSH), and thyroid-stimulating hormone (TSH) are heterodimeric glycoprotein hormones that regulate reproduction and thyroid homeostasis. − LH is responsible for ovulation induction in women and controls testosterone production in men. FSH causes ovarian follicle maturation in women and is involved in spermatogenesis in men.…”

Section: Introductionmentioning

confidence: 99%

“…Disruption of physiological regulation of LHCGR, FSHR, and TSHR by diverse pathogenic mutations has been implicated in a number of human diseases. , The specific and potent control of these multifunctioning receptors could provide important therapeutic advancements. LH and FSH are currently used clinically for the treatment of infertility, and it can be reasoned that synthetic agonists of LHCGR and FSHR have potential as infertility therapeutics.…”

Section: Introductionmentioning

confidence: 99%

“…1 N-benzyl-4-(3-methoxyphenyl)-2-(methylthio)thieno[2,3-d Analysis of 20 at both the TSHR and LHCGR. Comparison of activation of TSHR and LHCGR by compounds 3 and 20 relative to basal activities of both receptors.…”

Section: -Amino-n-(ethyl)-4-(3-methoxyphenyl)-2-(methylthio)thieno[2mentioning

confidence: 99%

See 2 more Smart Citations

Evaluation of Small-Molecule Modulators of the Luteinizing Hormone/Choriogonadotropin and Thyroid Stimulating Hormone Receptors: Structure−Activity Relationships and Selective Binding Patterns

et al. 2006

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The substituted thieno [2,3-d]pyrimidine 3 (Org 41841), a partial agonist for the luteinizing hormone/ choriogonadotropin receptor (LHCGR) and the closely related thyroid-stimulating hormone receptor (TSHR), was fundamentally altered and the resulting analogues were analyzed for their potencies, efficacies and specificities at LHCGR and TSHR. Chemical modification of the parent compound combined with prior mutagenesis of TSHR provided compelling experimental evidence in support of computational models of 3 binding to TSHR and LHCGR within their transmembrane cores. Biochemical analysis of a specific modification to the chemical structure of 3 provides additional evidence of a H-bond between the ligand and a glutamate residue in transmembrane helix 3, which is conserved in both receptors. Several key interactions were surveyed to determine their respective biochemical roles in terms of both van der Waals dimensions and hydrogen bond capacity and the respective relationship to biological activity.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%