Structural insights into thyrotropin-releasing hormone receptor activation by an endogenous peptide agonist or its orally administered analogue
Dear Editor,
Thyrotropin-releasing hormone(TRH)is a tripeptide(L-pyroglu-tamyl-L-histidinyl-L-prolinamide)that is widely distributed in the brain and spinal cord,playing dual roles as both an endocrine hormone and a neuropeptide.TRH plays a central role in the hypothalamic-pituitary-thyroid(HPT)axis.1-3 TRH is mainly synthesized in the hypothalamus and stimulates the release of thyroid-stimulating hormone(TSH,also known as thyrotropin)and prolactin from the anterior lobe of the hypophysis.4,5TRH activates the class A G protein-coupled receptor(GPCR)thyrotropin-releasing hormone receptor(TRHR),leading to the coupling of Gαq/G11 and the subsequent production of inositol-1,4,5-tripho-sphate and the release of intracellular Ca2+ions.6 Outside of the hypothalamus,TRH functions as a neurotransmitter or a neuro-modulator2 and exhibits antidepressant activity,arousal,analeptic and neuroprotective effects,cardiovascular and gastrointestinal autonomic functions.2,7 TRH is considered a promising peptide template for the analogue development to treat brain and spinal injuries,or central nervous system(CNS)disorders including epilepsy,schizophrenia,spinal cord trauma,Alzheimer's disease(AD),Parkinson's disease(PD)and depression.
insights、receptor、activation、administered、agonist、analogue、endogenous、hormone、into、orally
32
G632.3;G423.3;R735.2
2022-10-21（万方平台首次上网日期，不代表论文的发表时间）
共4页
858-861
