基于胺和氨基酸的化合物作为碳酸酐酶激活剂。
Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators.
机构信息
NEUROFARBA Department, Pharmaceutical and Nutraceutical Section, University of Florence, via Ugo Schiff 6, 50019 Sesto Fiorentino, FI, Italy.
Department of Food and Drug, University of Parma, Parco Area delle Scienze, 27/A, 43124 Parma, Italy.
出版信息
Molecules. 2021 Dec 2;26(23):7331. doi: 10.3390/molecules26237331.
After being rather neglected as a research field in the past, carbonic anhydrase activators (CAAs) were undoubtedly demonstrated to be useful in diverse pharmaceutical and industrial applications. They also improved the knowledge of the requirements to selectively interact with a CA isoform over the others and confirmed the catalytic mechanism of this class of compounds. Amino acid and amine derivatives were the most explored in in vitro, in vivo and crystallographic studies as CAAs. Most of them were able to activate human or non-human CA isoforms in the nanomolar range, being proposed as therapeutic and industrial tools. Some isoforms are better activated by amino acids than amines derivatives and the stereochemistry may exert a role. Finally, non-human CAs have been very recently tested for activation studies, paving the way to innovative industrial and environmental applications.
在过去，碳酸酐酶激活剂（CAAs）作为一个研究领域被忽视了，但它们无疑在各种药物和工业应用中具有重要作用。它们还增进了人们对于选择性与一种碳酸酐酶同工型相互作用而非其他同工型的要求的认识，并证实了这类化合物的催化机制。在体外、体内和晶体学研究中，氨基酸和胺类衍生物是最受关注的碳酸酐酶激活剂。其中大多数能够在纳摩尔范围内激活人源或非人类源碳酸酐酶同工型，被提议作为治疗和工业工具。一些同工型被氨基酸激活的效果优于胺类衍生物，立体化学可能发挥作用。最后，最近还对非人类源碳酸酐酶进行了激活研究，为创新性的工业和环境应用铺平了道路。
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