TSH Receptor

Thyrotropin receptor; Thyroid-stimulating hormone Receptor

The TSH receptor (TSHR) is a member of the glycoprotein hormone receptors, a subfamily of family A G protein-coupled receptors. The TSH receptor (TSHR) undergoes complex post –translational modifications including intramolecular cleavage and receptor multimerization. TSHR and its endogenous ligand thyrotropin (TSH) are of essential importance for growth and function of the thyroid gland and proper function of the TSH/TSHR system is pivotal for production and release of thyroid hormones.

The TSHR activates different G-protein subtypes and signaling pathways, whereby Gs- and Gq-induced signaling are probably of highest importance. TSH and its receptor are required for thyroid hormone synthesis and release in the thyroid gland. Dysfunctions of the TSHR are the underlying cause of various gain- or loss-of-function phenotypes associated with thyroid malfunction. It has been suggested that the TSHR is involved in the development and mechanisms of ophthalmopathy. TSHR is also a major autoantigen for autoimmune diseases of the thyroid gland. In addition, TSHR has been proposed to be a potent target against thyroid cancer with several experimental compounds under development.

TSH Receptor 相关产品（9）

货号	产品名	Cas	产品描述
PL12486	D3-βArr	662164-09-2	D3-βArr 是一种促甲状腺激素受体正变构调节剂，通过促甲状腺激素受体直接激活启动 β-Arr 1 的易位，并增强促甲状腺激素介导的体外成骨细胞分化。
PL11824	ML-109	1186649-91-1	ML-109 是有效的、促甲状腺激素受体 (TSHR) 的全激动剂，其 EC50 值为 40 nM。
PC10786	ML224	1338824-21-7	选择性TSHR反向激动剂,ML224(NCGC00242364; ANTAG3)是促甲状腺激素受体TSHR反激动剂，IC50值为2.3uM。
PL12484	NCGC00229600	1338824-20-6	NCGC00229600 是 TSHR 的变构反向激动剂。NCGC00229600 抑制 TSH 和刺激在 Graves 病中内源表达的 TSHRs 的抗体激活。
PL12488	Org41841	301847-37-0	ORG41841 是促黄体激素/绒毛膜促性腺激素受体 (LHCGR) 和促甲状腺激素受体 (TSHR) 的部分激动剂，其 EC50 值分别为 0.2 和 7.7 μM。
PL12489	Teprotumumab	1036734-93-6	Teprotumumab 是一种阻断 IGF-1 受体 (IGF-1R) 的人单克隆抗体。Teprotumumab 与 IGF-1R 的细胞外 α-亚基结构域配体结合。Teprotumumab 抑制纤维细胞中的 TSH 和 IGF-1 作用。Teprotumumab 可降低 TSH 依赖性 IL-6 和 IL-8 的表达和 Akt 的磷酸化。Teprotumumab 可用于甲状腺相关眼病的研究。
PL12487	TSHR antagonist S37a	2143452-20-2	TSHR antagonist S37a 是一个高选择性的促甲状腺激素受体 TSHR 拮抗剂，具有研究格雷夫斯眼窝病的潜力。
PL12490	TSHR antagonist S37b	2143452-22-4	TSHR antagonist S37b 是 TSHR antagonist S37a (HY-129995A) 的低活性异构体，对促甲状腺激素受体 TSHR 有较小的抑制作用。TSHR antagonist S37b 可以用于甲状腺功能的研究。
PL12485	VA-K-14 hydrochloride	1171341-19-7	VA-K-14 hydrochloride 是一种特异性促甲状腺激素受体 (TSHR) 拮抗剂 (IC50= 12.3 μM)。