Biological Activity of Synthetic Polypeptide Derivatives Related to the Structure of Hypothalamic TRF

Burgus, Roger; Dunn, Thomas F.; Desiderio, Dominic M.; Ward, Darrell N.; Vale, Wylie; Guillemin, Roger; Félix, Arthur; Gillessen, Dieter; Studer, R. O.

doi:10.1210/endo-86-3-573

Cited by 67 publications

(31 citation statements)

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“…The synthesis of the tripeptide pyroglutamylhistidyl-prolineamide (TRF), the thyreotropin releasing factor [ 1,2], and its labelling [3] have promoted studies of its mode of action at the molecular level [4]. One important step towards this aim is to define the shape of the molecule and the relationships between biological activity and conformations.…”

Section: Introductionmentioning

confidence: 99%

Proton NMR studies on thyrotropin releasing factor

et al. 1972

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Section: Introductionmentioning

confidence: 99%

Proton NMR studies on thyrotropin releasing factor

et al. 1972

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“…Burgus and associates (7)(8)(9) have reported that 'Also known as thyrotropin-releasing hormone (TRH).…”

Section: Introductionmentioning

confidence: 99%

“…Synthetic TRF and its analogues have been prepared, and structure-activity relationships studied by both of the above groups (9,(12)(13)(14) and by other workers (15)(16)(17). Natural and synthetic TRF is active in the mouse (14,16,18,19), rat (20), and man (16,17,(21)(22)(23)(24) (25); mean age 13 yr 7 months; group III, 9 patients (8 males, 1 female) with multiple anterior pituitary hormone deficiencies, including deficient TSH, and no demonstrable intracranial mass; mean age 15 yr 8 months.…”

Section: Introductionmentioning

confidence: 99%

Effect of thyrotropin-releasing factor on serum thyroid-stimulating hormone

Costom¹,

Grumbach²,

Kaplan³

1971

J. Clin. Invest.

125

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“…In 1969, two groups lead by Guillemin [5] and Schally [2] discovered that the hypothalamic substance responsible for the release of thyrotropin was the tripeptide pGlu-His-Pro-NH 2 or thyrotropin-releasing hormone (TRH). TRH has dual role; it acts as a hormone and it is also a neuropeptide.…”

Section: Introductionmentioning

confidence: 99%

Exploratory neuropharmacological evaluation of a conformationally constrained thyrotropin-releasing hormone analogue

Teixidó¹,

Prókai-Tátrai²,

Wang³

et al. 2007

Brain Research Bulletin

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A conformationally constrained peptidomimetic derived from the endocrine and neuroactive tripeptide thyrotropin-releasing hormone (pGlu-His-Pro-NH 2 ) was synthesized by convenient solidphase organic chemistry and evaluated as a potential central nervous system agent. While this ethylene-bridged peptide analogue has been reported to lack the hormonal effect of the native peptide, we have shown in animal models that it possesses central nervous system activity characteristic of thyrotropin-releasing hormone. Compared to control, the peptidomimetic showed significant analeptic and antidepressant-like potencies. Moreover, an enhanced selectivity in antidepressant-like effect was measured when compared to that of the native peptide. Immobilized artificial membrane chromatography and in vitro metabolic stability studies also revealed that this constrained peptidomimetic has higher affinity to the blood-brain barrier than the native peptide and is metabolically stable. Consequently, this structure may be used as a template to design centrally selective and metabolically stable thyrotropin-releasing hormone analogues as potential neuropharmaceutical agents.

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Biological Activity of Synthetic Polypeptide Derivatives Related to the Structure of Hypothalamic TRF

Cited by 67 publications

References 0 publications

Proton NMR studies on thyrotropin releasing factor

Proton NMR studies on thyrotropin releasing factor

Effect of thyrotropin-releasing factor on serum thyroid-stimulating hormone

Exploratory neuropharmacological evaluation of a conformationally constrained thyrotropin-releasing hormone analogue

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