2015
DOI: 10.3389/fendo.2015.00155
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New Frontier in Glycoprotein Hormones and Their Receptors Structure–Function

Abstract: Last two decades of structure–function studies performed in numerous laboratories provided substantial progress in understanding basic science, physiological, pathophysiological, pharmacological, and comparative aspects of glycoprotein hormones (GPHs) and their cognate receptors. Multiple concepts and models developed based on experimental data in the past stood the test of time and have been, at least in part, confirmed and/or remained compatible with the new structures resolved at the atomic level. Major adv… Show more

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Cited by 17 publications
(12 citation statements)
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“…The pituitary gonadotropin hormones, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), are synthesized in gonadotrope cells and play a key role in the control of gonadal function and reproduction (Huhtaniemi et al, 1982;Bousfield et al, 1996;Richards et al, 2002). Both gonadotropins, as well as placental chorionic gonadotropin (CG) and thyroid-stimulating hormone (TSH) produced by pituitary thyrotropes, belong to the family of glycoprotein hormones (GPH) (Pierce and Parsons, 1981; Ulloa-Aguirre and Szkudlinski, 2015).…”
Section: Introductionmentioning
confidence: 99%
“…The pituitary gonadotropin hormones, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), are synthesized in gonadotrope cells and play a key role in the control of gonadal function and reproduction (Huhtaniemi et al, 1982;Bousfield et al, 1996;Richards et al, 2002). Both gonadotropins, as well as placental chorionic gonadotropin (CG) and thyroid-stimulating hormone (TSH) produced by pituitary thyrotropes, belong to the family of glycoprotein hormones (GPH) (Pierce and Parsons, 1981; Ulloa-Aguirre and Szkudlinski, 2015).…”
Section: Introductionmentioning
confidence: 99%
“…1A). Mutation of all four residues to lysines results in the increase of binding affinity of hTSH to the hTSHR (Szkudlinski et al 1996, Szkudlinski 2015. Jiang et al (2012) proposed, based on the crystal structure of the FSH-FSHR ECD complex, that the TSHα mutations Q13K, E14K, P16K and Q20K are concentrated at the top side of the sulphated-Tyr binding pocket of the hormone, generating additional positive charges for a stronger interaction with the sulphated-Tyr of the receptor.…”
Section: Discussionmentioning
confidence: 99%
“…The essential biological properties of a compound that define its interaction with a putative target are: selectivity, potency, phenotypic efficacy (agonist, antagonist, allosteric modulator), target engagement, and bioavailability (Nunez, Venhorst, & Kruse, ; Kenakin, ; Szkudlinski, ). The first three properties reflect the pharmacodynamic (PD) properties of a compound, its effect on the target, cellular transduction cascade, tissue/system function, and whole animal phenotypic read out, while the latter two properties reflect its pharmacokinetic (PK) properties.…”
Section: Compound Validationmentioning
confidence: 99%
“…The essential biological properties of a compound that define its interaction with a putative target are: selectivity, potency, phenotypic efficacy (agonist, antagonist, allosteric modulator), target engagement, and bioavailability (Nunez, Venhorst, & Kruse, 2011;Kenakin, 2014;Szkudlinski, 2015). The first three properties reflect the pharmacodynamic (PD) properties of a compound, its effect…”
Section: Compound Biologymentioning
confidence: 99%