ChemDiv 化合物库包含有针对 Macl-GPIb alpha 相互作用的27,000种化合物。白细胞与血小板的相互作用在介导白细胞粘附到血栓和白细胞募集到血管损伤部位方面具有重要作用。这种相互作用是通过β2整合素Mac-1(也称为整合素αMβ2)及其在血小板上的配体糖蛋白Ibalpha(GPIb)介导的,后者是GP Ib-IX-V 复合物和血小板von Willebrand 因子(vWf)受体的组成部分。
研究表明,Mac-1-GPIb alpha 相互作用涉及Mac-1 I 结构域(与vWf A1结构域同源),以及GPIb 富含亮氨酸重复和羧基末端附近区域。由于白细胞-血小板相互作用双向诱导信号,增强促炎和促凝血细胞反应,因此它提供了一个分子靶点,用于破坏促进血栓形成、动脉粥样硬化和血管成形术相关再狭窄的白细胞-血小板复合物引起的血管炎症。
目前的抗血栓药物,包括抗血小板药物和抗凝药物,与显著的出血风险和增加的死亡率相关。研究表明,针对Mac-1-GPIb 相互作用的小分子靶向治疗成功地抑制了血栓形成。此外,确定了针对这种相互作用的靶向治疗具有降低出血风险的抗血栓治疗潜力。
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Vadadustat | TAK875 | TAK-779 | Tegobuvir | RN-1734 | BMS-687453 | AM211 | FT011 | BMS754807 | AAI101 | ||
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RPW-24 | SRT1720 hydrochloride | INH6 | SRT 2183 | AMG208 | Pentadecanoic acid | Apiopaeonoside | Pemirolast potassium | L-Anserine nitrate salt | Sodium Picosulfate | ||
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Lercanidipine | Cobicistat | 1-Ethyl-2-benzimidazolinone | ROSIRIDIN | PF-AKT400 | Benzyl alcohol | 1-Methylnicotinamide chloride | MX69 | CVT-10216 | LCL161 | ||
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Tirasemtiv | Roniacol | Rg3039 | Z433927330 | Desloratadine | CH5132799 | 5-Bromoindole | Smurf1-IN-A01 | Halosulfuron-methyl | Piceatannol | ||
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ML346 | SB 4 | Daclatasvir | Daclatasvir dihydrochloride | NADPH (tetracyclohexanamine) | AZD8055 | Vistusertib | PAβN dihydrochloride | HZ1157 | Rotundine | ||
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Thiamet G | B-AP15 | Silmitasertib | Levofloxacin | Pamicogrel | GSK369796 Dihydrochloride | 2-Chloronaphthoquinone | TFAP | Tenovin3 | Azvudine | ||
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Milnacipran hydrochloride | BW-A78U | Tenovin-6 | DL-Normetanephrine hydrochloride | Triclocarban | CUDC101 | Chlorpropham | Mestinon | Zacopride hydrochloride | PF04691502 | ||
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L-Hyoscyamine | Noreugenin | ML-030 | BC-1382 | Gadolinium chloride | Vorolanib | VTP-27999 TFA | GSK0660 | Lomerizine hydrochloride | 8-CHLOROQUINAZOLIN-4(1H)-ONE |