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抑制剂

抑制剂简介

抑制剂是一类能够降低或阻止生物体内的酶活性、受体的活性或是细胞内特定反应过程的小分子化合物。它们在有机化学、化学化工和生物医药领域中有着广泛的应用,尤其是在药物研发方面。

分类与作用机制

  1. 竞争性抑制剂:这类抑制剂通过与其目标蛋白质(如酶)结合,占据其底物结合位点,从而阻止真正的底物与蛋白质的正常结合。这种类型的抑制通常可以通过增加底物浓度来缓解。
  2. 非竞争性抑制剂:非竞争性抑制剂通过改变蛋白质的功能状态或结构,而不直接与其活性部位相结合。它们可能会影响蛋白质的构象变化或者与其他位点相互作用。
  3. 不可逆抑制剂:这类抑制剂与酶或其他生物分子形成共价键,导致其永久失去功能。由于这种特性,此类抑制剂通常用于实验室研究中。

应用领域

  1. 药物开发:在生物医药领域,抑制剂被广泛用作潜在的治疗药物,用于对抗各种疾病如癌症、病毒感染等。
  2. 酶学研究:有机化学和生物化学研究经常使用特定类型的抑制剂来探究酶的功能和作用机理。
  3. 合成与催化:化学化工中,通过调节反应条件或引入适当的抑制剂可以提高某些目标产物的选择性。

总结

抑制剂的研究和发展对于理解生命过程至关重要,并在药物开发、基础科学研究等多个领域发挥着重要作用。随着技术的进步,新的抑制剂不断被发现和开发出来,为医学治疗提供了更多的可能性。

中文名称 英文名称 CAS号 化学式
—— 2-(2-Dihydroxyboryl-5-trifluoromethoxybenzylsulfanyl)pyrimidine-5-carboxylic acid (4-fluorophenyl)amide 1648843-04-2 C19H14BF4N3O4S
—— 4-((2S,4S)-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid 1644670-37-0 C25H30N2O4
—— inflachromene 908568-01-4 C21H19N3O4
—— 4-((2-(p-Chlorobenzoyl)-5-methoxy-2-methyl-3-indolyl)acetyl)morpholine 2854-32-2 C23H23ClN2O4
—— Hytrin 70024-40-7 C19H25N5O4*ClH*2H2O
—— (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-[1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 137071-32-0 C43H68ClNO11
—— 4-bromo-N-(tetrahydro-2-furanylmethyl)benzamide 326898-76-4 C12H14BrNO2
—— 5-O-[8-(cis-2,6-dimethylmorpholino)octylcarbamoyl]eseroline 154619-51-9 C28H46N4O3
—— (2R)-N-(2-aminoacetyl)-2-[[(2S)-4-[(3-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-[(3-fluorophenyl)methyl]amino]-3,3-dimethylbutanamide 284661-68-3 C35H48FN5O5S
—— Etripamil 1593673-23-4 C27H36N2O4
—— Meldonium; MET-88; Quaterin 86426-17-7 C6H16N2O3
—— [(2R,3S,4S,5S,6R)-6-[[(3Z,5Z,8S,9Z,11S,12R,13Z,15Z,18S)-12-[(2R,3S,4R,5S)-3,4-dihydroxy-6,6-dimethyl-5-(2-methylpropanoyloxy)oxan-2-yl]oxy-11-ethyl-8-hydroxy-18-[(1R)-1-hydroxyethyl]-9,13,15-trimethyl-2-oxo-1-oxacyclooctadeca-3,5,9,13,15-pentaen-3-yl]methoxy]-4-hydroxy-5-methoxy-2-methyloxan-3-yl] 3,5-dichloro-2-ethyl-4,6-dihydroxybenzoate 873857-62-6 C52H74Cl2O18
—— 1,2-Benzoxazol-3-yl 4-acetamidobenzene-1-sulfonate 77408-67-4 C15H12N2O5S
—— volasertib 755038-65-4 C34H50N8O3
—— (1S,4E,5'R,6R,6'R,7S,8R,10S,11R,12R,14R,15R,16S,18E,20E,22S,25R,27S,28R,29S)-22-ethyl-7,11,15-trihydroxy-6'-[(2S)-2-hydroxypropyl]-5',6,8,10,12,14,16,28,29-nonamethylspiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2'-oxane]-3,9,13-trione 11052-72-5 C45H74O10
—— trospium chloride 10405-02-4 C25H30NO3*Cl
—— (4S,5R)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole 548472-49-7 C25H24Cl2N2O2
—— Pyr-41 418805-02-4 C17H13N3O7
—— Quinupristin 120138-50-3 C53H67N9O10S
—— 30-ethyl-33-[(E,1S,2S)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone 59865-13-3 C62H111N11O12
—— (1S,4E,5'R,6R,6'R,7S,8R,10S,11R,12R,14R,15R,16S,18E,20E,22S,25R,27S,28R,29S)-22-ethyl-7,11,15-trihydroxy-6'-(2-hydroxypropyl)-5',6,8,10,12,14,16,28,29-nonamethylspiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2'-oxane]-3,9,13-trione 11052-72-5 C45H74O10
—— FK-506 (Tacrolimus) 104987-11-3 C44H69NO12
—— 4-amino-N-(3-methyl-1-((6-methylpyridin-2-yl)methyl)-1H-indazol-4-yl)thieno[3,2-d]pyrimidine-7-carboxamide 1527517-50-5 C22H19N7OS
—— N-[(2S)-1-[[(2R)-3-(1H-indol-3-yl)-2-[methyl(3-methylbutyl)amino]propanoyl]amino]-1-oxopropan-2-yl]-2-phenyl-1H-imidazole-5-carboxamide 150351-90-9 C30H36N6O3
—— HIV-1 Integrase Inhibitor 544467-07-4 C11H9N3O4
—— (E)-N-(4-Benzylpiperazin-1-Yl)-1-(3,5-Dimethyl-1-Phenyl-1h-Pyrazol-4-Yl)methanimine 304909-07-7 C23H27N5
—— S-Neoral 59865-13-3 C62H111N11O12
—— ((2-ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate 1842399-68-1 C19H26BNO7
—— 1-Azetidinethiocarboxylic acid, (1-(2-pyridyl)ethylidene)hydrazide 71555-25-4 C11H14N4S
—— roquefortine 58735-64-1 C22H23N5O2
—— [4-[2-[(16Z,24Z,26Z,28Z)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate 162635-04-3 C56H87NO16
—— KU0063794 938440-64-3 C25H31N5O4
—— (1R,9S,12S,13R,14S,17R,18Z,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 137071-32-0 C43H68ClNO11
—— GSK2795039 1415925-18-6 C23H26N6O2S
—— methyl 4-(N-2,5-dihydroxybenzylamino)benzoate 140674-76-6 C15H15NO4
—— tubacin 537049-40-4 C41H43N3O7S
—— Oxiranecarboxylic acid, [2S-[2alpha,3beta(R*)]]- 76684-89-4 C15H26N2O5
—— [(3S,5S,6S,8S)-8-[(3-amino-2,2-dimethyl-3-oxopropyl)carbamoyl]-6-hydroxy-3-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-2,9-dimethyldecan-5-yl]azanium;(E)-but-2-enedioate 173334-58-2 C64H110N6O16
—— Benzaldehyde, 3-ethyl-2,4-dihydroxy-6-((1E)-1-methyl-1-pentenyl)- 203051-01-8 C15H20O3
—— 3,5-Di-iso-propyl-4-hydroxybenzylidenmalonitril 71308-34-4 C16H18N2O
—— relacorilant 1496510-51-0 C27H22F4N6O3S
—— (4-benzylpiperazin-1-yl)-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethylene)amine 304909-07-7 C23H27N5
—— (1R,2R)-2-(pyridin-2-yl)cyclopropanecarboxylic acid ((2S,3S)-2-amino-3-methylpentyl)-(4′-propylbiphenyl-4-yl)amide 1287205-42-8 C30H37N3O
—— furmonertinib 1869057-83-9 C28H31F3N8O2
—— methyl (S)-2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholine-4-carboxylate 1621164-74-6 C23H24F2N4O4
—— (2-(1H-indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl)methanone 1332881-26-1 C21H19N3O4
—— (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one 1421919-75-6 C16H10F8N4O
—— N-{4-[4-(4-methoxyphenoxy)-2,6-dimethylphenyl]thiazol-2-yl}pyridine-4-carboxamide 1334921-03-7 C24H21N3O3S
—— Pixantrone dimaleate 144675-97-8 C25H27N5O10
—— (S)-4-Amino-6-((1-(2-isopropyl-8-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1-oxo-1,2-dihydroisoquinolin-3-yl)ethyl)amino)pyrimidine-5-carbonitrile 1425043-73-7 C25H25N7O2