1. Signaling Pathways
  2. GPCR/G Protein
  3. ICMT

ICMT (异戊酰半胱氨酸羧甲基转移酶)

Isoprenylcysteine carboxyl methyltransferase

ICMT(异戊二烯基半胱氨酸羧基甲基转移酶)是一种参与复杂的翻译后修饰过程的酶,在异戊二烯化蛋白质的翻译后调控中起关键作用。ICMT主要催化翻译后异戊二烯甲基化的C端半胱氨酸残基的甲基化,并将这些蛋白质定位到细胞膜上。这种修饰给底物蛋白提供了疏水性不带电的C端,从而增强与生物膜的相互作用和/或改变与蛋白质伴侣相互作用的能力。ICMT催化的蛋白质异戊二烯化可能在癌症中发挥作用,例子包括ICMT修饰的RHO GTPases或Ras家族成员。当ICMT基因被敲除时,可以抑制KRAS诱导的胚胎成纤维细胞转化,抑制RAS驱动的肿瘤发生;或ICMT抑制可阻碍RHO GTPase相关的癌细胞侵袭和转移[1][2]

ICMT (Isoprenylcysteine carboxyl methyltransferase) is an enzyme involved in complex post-translational modification processes and plays a key role in the post-translational regulation of prenylated proteins. ICMT primarily catalyzes the methylation of post-translationally isoprene-methylated C-terminal cysteine residues and targets these proteins to the cell membrane. This modification provides the substrate protein with a hydrophobic uncharged C terminus, thereby enhancing interaction with biological membranes and/or altering the ability to interact with protein partners. ICMT-catalyzed protein prenylation may play a role in cancer. Examples include ICMT-modified RHO GTPases or Ras family members. When the ICMT gene is knocked out, it can inhibit KRAS-induced embryonic fibroblast transformation and inhibit RAS-driven tumorigenesis; or ICMT inhibition can hinder RHO GTPase-related cancer cell invasiveness and metastasis[1][2].

ICMT 相关产品 (66):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149712
    Spermatinamine Inhibitor
    Spermatinamine 是具有溴酪氨酰-精胺-溴酪氨酰序列的新型生物碱,和天然 ICMT 抑制剂。Spermatinamine 能够从澳大利亚海绵 Pseudoceratina 中分离得到。
    Spermatinamine
  • HY-149715
    R1-11 Inhibitor
    R1-11 是吲哚类 ICMT 抑制剂,IC50 为 0.6 μM,具有抗癌活性。R1-11 抑制 MDA-MB231 和 PC3 细胞的 IC50s 分别为 2.2 μM 和 2.0 μM。
    R1-11
  • HY-149714
    J6-3 Inhibitor
    J6-3 是 ICMT 的抑制剂,IC50 为 0.6 μM,具有抗癌活性。J6-3 抑制 MDA-MB231 细胞的 IC50 为 3.4 μM。
    J6-3
  • HY-149710
    POP-3MB Inhibitor
    POP-3MB (compound 1b) 是 ICMT 抑制剂 (IC50: 2.5 μM)。POP-3MB 可改变 K-Ras 的亚细胞定位,抑制 Ras 活化。POP-3MB 还抑制 Erk 磷酸化。
    POP-3MB
  • HY-117776
    CAY10677 Inhibitor
    CAY10677 (compound 15) 是强效的 ICMT 抑制剂,可抑制癌细胞增殖。CAY10677 具有良好 PAMPA 渗透性。
    CAY10677
  • HY-149711
    Farnesylcysteine Inhibitor
    Farnesylcysteine (FC) 是 ICMT 的竞争性抑制剂。fcly 突变体中法呢基半胱氨酸(FC)裂解酶活性定量低,对 ABA 的反应增强。Farnesylcysteine 可诱导拟南芥的 ABA 超敏表型。
    Farnesylcysteine