摘要
肽脱甲酰基酶是一类负责在翻译的过程中从N端-蛋氨酸中去除N-甲酰基团催化作用的金属酶。PDF抑制剂正进入药物开发中新的阶段。最初,PDF被认为是一个可用于抗菌药物开发的重要靶标;但是基因组数据检索在寄生虫(恶性疟疾原虫)和人类中发现了PDF-类序列,从而将这个靶标从抗菌扩展到抗疟疾和抗癌的药物开发中的应用。使用结构的和机制信息与高通量的筛选一起,几类化学类的,有着更强的药效和更好的专一性的PDF抑制剂被确定了。许多的药物如,GSK-1322322 (II期),BB-83698 (I期), 和LBM-415 (I期)都已经进入到临床开发阶段。这个领域的发展促使我们综述了PDF的不同方面,尤其是他们的结构,不同的PDF抑制剂分类,以及分子模型研究。简而言之,这篇综述重点介绍了PDF作为一个通用的靶标和它的抑制剂,以及不同的PDF抑制剂未来的前景。
关键词: 抗菌,抗癌,抗疟疾,临床开发,肽脱甲酰基酶。
Current Medicinal Chemistry
Title:Peptide Deformylase: A New Target in Antibacterial, Antimalarial and Anticancer Drug Discovery
Volume: 22 Issue: 2
Author(s): Jaiprakash N. Sangshetti, Firoz A. Kalam Khan and Devanand B. Shinde
Affiliation:
关键词: 抗菌,抗癌,抗疟疾,临床开发,肽脱甲酰基酶。
摘要: Peptide deformylase (PDF) is a class of metalloenzyme responsible for catalyzing the removal of the N-formyl group from N-terminal methionine following translation. PDF inhibitors are moving into new phase of drug development. Initially, PDF was considered as an important target in antibacterial drug discovery; however genome database searches have revealed PDF-like sequences in parasites (P. falciparum) and human, widening the utility of this target in antimalarial and anticancer drug discovery along with antibacterial. Using structural and mechanistic information together with high throughput screening, several types of chemical classes of PDF inhibitors with improved efficacy and specificity have been identified. Various drugs like, GSK-1322322 (Phase II), BB-83698 (Phase I), and LBM-415 (Phase I) have entered into clinical developments. Developments in the field have prompted us to review the current aspects of PDFs, especially their structures, different classes of PDF inhibitors, and molecular modeling studies. In nut shell, this review enlightens PDF as a versatile target along with its inhibitors and future perspectives of different PDF inhibitors.
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Cite this article as:
Jaiprakash N. Sangshetti, Firoz A. Kalam Khan and Devanand B. Shinde , Peptide Deformylase: A New Target in Antibacterial, Antimalarial and Anticancer Drug Discovery, Current Medicinal Chemistry 2015; 22 (2) . https://dx.doi.org/10.2174/0929867321666140826115734
DOI https://dx.doi.org/10.2174/0929867321666140826115734 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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