1. Signaling Pathways
  2. GPCR/G Protein
  3. Adhesion G Protein-coupled Receptors (AGPCRs)

Adhesion G Protein-coupled Receptors (AGPCRs) (粘附类 G 蛋白偶联受体 (AGPCR) )

Adhesion G Protein-coupled Receptors (AGPCRs)

Adhesion G Protein-Coupled Receptors (AGPCRs) 是 G 蛋白偶联受体 (GPCR) 超家族的一个亚类,主要介导细胞黏附、细胞-细胞通讯和信号转导,在神经发育、免疫调节、血管生成及 癌症进展等过程中发挥重要作用。
AGPCR 家族包含 33 个成员,依据功能可分为免疫相关型 (如 ADGRE1-5)、发育与神经系统相关型 (如 ADGRG1, ADGRL3) 及心血管调控型 (如 ADGRA2),均以 "ADGR" 命名。其独特之处在于较长的细胞外 N 端结构及 GPS 蛋白水解位点,允许其在受到外部刺激后通过 “Stachel” 结构域自激活介导信号传导。
功能异常的 AGPCR 与脑发育缺陷、炎症性疾病、不育症及多种癌症相关。例如,ADGRG1 (GPR56) 突变可导致双侧额顶多小脑回畸形 (BFPP),ADGRE2 突变与振动性荨麻疹有关,而 ADGRG2 (GPR64) 缺陷可能导致先天性输精管双侧缺失 (CBAVD)。此外,GPR56 还在黑色素瘤转移和胶质瘤进展中发挥关键作用。随着对 AGPCRs 结构和功能研究的深入,该家族已成为神经系统疾病、免疫疾病及癌症的研究重点[1][2]

dhesion G Protein-Coupled Receptors (AGPCRs) are a subfamily of the G protein-coupled receptor (GPCR) superfamily, primarily mediating cell adhesion, cell-cell communication, and signal transduction, playing crucial roles in neural development, immune regulation, angiogenesis, and cancer progression.
The AGPCR family consists of 33 members, categorized based on function into immune-related types (e.g., ADGRE1-5), development and nervous system-related types (e.g., ADGRG1, ADGRL3), and cardiovascular regulatory types (e.g., ADGRA2), all designated with the "ADGR" prefix. A distinctive feature of AGPCRs is their long extracellular N-terminal domain and GPS (G protein-coupled receptor proteolytic site), which enables self-activation via the “Stachel” domain upon external stimulation, facilitating signal transduction.
Dysfunction of AGPCRs is associated with brain developmental disorders, inflammatory diseases, infertility, and various cancers. For instance, mutations in ADGRG1 (GPR56) can cause bilateral frontoparietal polymicrogyria (BFPP), mutations in ADGRE2 are linked to vibratory urticaria, and deficiency of ADGRG2 (GPR64) may result in congenital bilateral absence of the vas deferens (CBAVD). Additionally, GPR56 plays a key role in melanoma metastasis and glioma progression. With advancing research into AGPCR structure and function, this family has become a major focus in the study of neurological disorders, immune diseases, and cancer[1][2].

Adhesion G Protein-coupled Receptors (AGPCRs) 相关产品 (3):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16950A
    (E/Z)-4-Hydroxytamoxifen

    (E/Z)-4-羟基他莫昔芬

    Activator 99.62%
    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) 是 (Z)-4-Hydroxytamoxifen 和 (E)-4-Hydroxytamoxifen 的消旋体。(E/Z)-4-Hydroxytamoxifen 是选择性雌激素受体 (estrogen receptor) 调节剂,具有混合雌激素活性和抗雌激素活性,也是 Tamoxifen (HY-13757A) 的活性代谢物。(E/Z)-4-Hydroxytamoxifen 是 G 蛋白偶联雌激素受体 (GPER) 的一种低亲和力 (100-1000 nM) 激动剂。(E/Z)-4-Hydroxytamoxifen 有望用于周期性乳房痛的研究,如乳房疼痛、压痛、结节性的研究< /sup> [2]。
    (E/Z)-4-Hydroxytamoxifen
  • HY-P10365
    VPM-p15 Agonist 98.18%
    VPM-p15 是一种针对粘附 G 蛋白偶联受体 GPR64 (也称为 ADGRG2 或 HE6) 的优化肽激动剂。VPM-p15 与 GPR64 的亲和力相比原始的 p15 肽有显著提高。VPM-p15 诱导的 cAMP 水平显著增加,激活 GPR64,引发下游的 Gs,Gq,G12/13 信号传导。VPM-p15 可用于对粘附 GPCR 家族成员激活机制的研究。
    VPM-p15
  • HY-P3942
    SDP116 Inhibitor 98.65%
    SDP116 是 GPR116 Stachel 肽的合成 Stachel 衍生肽。SDP116 具有 ADGRF5 激动剂作用。
    SDP116