摘要
紊乱的kynurenine通路(KP)代谢与神经退行性疾病、精神疾病和癌症的进展有关。因此,通过这种途径调制的酶活性可以为这些条件提供潜在的新的治疗策略。考虑到其在KP中的显著位置,酶吲哚胺2,3-双加氧酶,犬尿氨酸3-单加氧酶和犬尿氨酸氨基转移酶,似乎是最有吸引力的目标。越来越多的人对这一途径产生了兴趣,这导致了一些有潜力的选择性的酶抑制剂的鉴定,有了有希望的临床前数据,以及几种酶晶体结构的说明,为使抑制剂活性的分子机制合理化提供了空间。该领域似乎即将产生一种或更多的抑制剂,应该能找到临床效用。
关键词: Kynurenine通路,神经变性,癌症,吲doleamine 2
Current Medicinal Chemistry
Title:Major Developments in the Design of Inhibitors along the Kynurenine Pathway
Volume: 24 Issue: 23
关键词: Kynurenine通路,神经变性,癌症,吲doleamine 2
摘要: Disrupted kynurenine pathway (KP) metabolism has been implicated in the progression of neurodegenerative disease, psychiatric disorders and cancer. Modulation of enzyme activity along this pathway may therefore offer potential new therapeutic strategies for these conditions. Considering their prominent positions in the KP, the enzymes indoleamine 2,3-dioxygenase, kynurenine 3-monooxygenase and kynurenine aminotransferase, appear the most attractive targets. Already, increasing interest in this pathway has led to the identification of a number of potent and selective enzyme inhibitors with promising pre-clinical data and the elucidation of several enzyme crystal structures provides scope to rationalize the molecular mechanisms of inhibitor activity. The field seems poised to yield one or more inhibitors that should find clinical utility.
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Major Developments in the Design of Inhibitors along the Kynurenine Pathway, Current Medicinal Chemistry 2017; 24 (23) . https://dx.doi.org/10.2174/0929867324666170502123114
DOI https://dx.doi.org/10.2174/0929867324666170502123114 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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