CDB15:0001516 TSHB — TSHR
Experimentally validated in Human; Orthology-inferred in Mouse, Rat, Frog, Zebrafish, Chicken, Macaque, Pig, Dog, Cow, Chimp, Marmoset, Sheep
Title
Journal:; Year Published:
Abstract
Recombinant human thyrotropins of the twenty-first century.
Expert opinion on pharmacotherapy, 2004; PubMed, Homo sapiens TSHB — Homo sapiens TSHR
ABSTRACT: In recent years, many new recombinant protein therapeutics have been developed and tested in clinical trials [1]. Current and future clinical uses of recombinant human thyroid-stimulating hormone (rhTSH; Thyrogen, Genzyme) in thyroid diseases are discussed in the review published in this issue of Expert Opinion on Pharmacotherapy [2]. As Thyrogen is a wild-type rhTSH produced in Chinese hamster ovary cells, it has relatively low affinity to the human TSH receptor. Such low affinity and weak intrinsic bioactivity of rhTSH, compared to the bovine or rodent TSH, may help to explain the results of several studies indicating limited clinical efficacy of Thyrogen. TSH analogues with largely increased receptor affinity, potency and efficacy, are expected to provide not only more effective than currently used diagnostic methods, but should also serve as indispensable second-generation thyrotropins for the diagnosis and treatment of thyroid carcinomas with a largely limited number of TSH receptors.
Molecular cloning, sequence and functional expression of the cDNA for the human thyrotropin receptor.
Biochemical and biophysical research communications, 1989; PubMed, Homo sapiens TSHB — Homo sapiens TSHR
ABSTRACT: We screened a human thyroid cDNA library with two synthetic oligonucleotides based on the reported amino acid sequence of the 3rd and 4th transmembrane domains of a putative human TSH receptor and related receptors. The nucleotide sequence of a 4 kb clone revealed an open reading frame of 764 amino acids (86,816 Daltons) with a putative signal peptide, seven transmembrane domains, five potential glycosylation sites, and a very short intracytoplasmic region. Homology with the extracellular domain of the pig LH/CG receptor was only 33%. Chinese hamster ovary cells stably transfected with this cDNA in an expression vector generated a functional receptor, able to activate adenylate cyclase, specifically in response to TSH stimulation.