Various Carbonic Anhydrases in Physiopathological Events, Carbonic Anhydrase Inhibitors, and Hybrid Compounds

IF 1.2 4区 医学 Q4 CHEMISTRY, MEDICINAL
Ayse ER
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引用次数: 0

Abstract

Abstract: Enzymes are highly specific catalysts that accelerate reactions in biological systems. Carbonic anhydrase (CA) is an enzyme found in plants, microorganisms, and vertebrates. CA catalyses CO2 hydration/ dehydration. There are different families and isoenzymes of CAs. Fifteen α-CA isoenzymes have been reported in humans. The status of CO2 hydration and dehydration is important for a variety of biological processes. CAs play an important role in many physiological and pathological events in several tissue types. Their levels are increased in some diseases; therefore, CA inhibition has been applied as a therapeutic option. However, the high diversity of these isoenzymes is an important consideration. Isoenzyme- specific CA inhibitors can reduce the side effects of treatment. Some agents containing additional sulfonamides approved for other therapeutic applications, such as topiramate, celecoxib/valdecoxib, sulpiride, and famotidine, have inhibitory effects on CA isoenzymes. These bind to the zinc ion in the CA active site. Recently, research has been conducted on the use of a hybrid form of active ingredient and a CA inhibitor. CA inhibitor-NSAID hybrid compounds demonstrated more efficacy than NSAIDs in arthritis, which has attracted further attention of researchers in conducting research on CA-hybrid drugs.
生理病理事件中的各种碳酸酐酶,碳酸酐酶抑制剂和杂化化合物
摘要:酶是促进生物系统反应的高度特异性催化剂。碳酸酐酶(CA)是一种存在于植物、微生物和脊椎动物中的酶。CA催化CO2水合/脱水。CAs有不同的家族和同工酶。在人类中已经报道了15种α-CA同工酶。二氧化碳的水合和脱水状态对各种生物过程都很重要。CAs在多种组织类型的许多生理和病理事件中发挥重要作用。它们的水平在某些疾病中升高;因此,CA抑制已被作为一种治疗选择。然而,这些同工酶的高度多样性是一个重要的考虑因素。同工酶特异性CA抑制剂可以减少治疗的副作用。一些含有额外磺胺的药物被批准用于其他治疗应用,如托吡酯、塞来昔布/伐地昔布、舒必利和法莫替丁,对CA同功酶有抑制作用。它们与CA活性位点的锌离子结合。最近,研究已经进行了混合形式的有效成分和CA抑制剂的使用。CA抑制剂-非甾体抗炎药杂合物在关节炎中的疗效优于非甾体抗炎药,这也引起了研究人员对CA杂合药物研究的进一步关注。
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来源期刊
CiteScore
1.80
自引率
10.00%
发文量
245
审稿时长
3 months
期刊介绍: Aims & Scope Letters in Drug Design & Discovery publishes letters, mini-reviews, highlights and guest edited thematic issues in all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis is on publishing quality papers very rapidly by taking full advantage of latest Internet technology for both submission and review of manuscripts. The online journal is an essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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