The tachykinergic system as avenues for drug intervention.

Pranela Rameshwar
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引用次数: 6

Abstract

This review discusses a family of receptors that interact with a family of small peptides that belong to the tachykinin family. The three subtypes of tachykinin receptors follow the following suggested nomenclature: NK1, NK2 and NK3. These receptors belong to the 7-transmembrane, G-protein coupled family. The NK receptor family has been implicated in a wide range of disorders, cancers, inflammation and neural-related diseases. The tachykinin NK receptors and their ligands have been implicated in solid and hematological tumors. Antagonists to NK receptors have been synthesized and some have been tested in preclinical and Phase II clinical studies. However, in order to be effective for treatment, it is imperative to understand the biology of NK receptor family as well as related molecules. One such molecule is HGFIN, also referred as nmb and osteoactivin. HGFIN is particularly relevant since it has been shown to interact with the high affinity ligand of NK1, substance P. This report discusses promising applications for targeting the NK receptors. The discussion proposes potential mechanisms that could occur when substance P interacts with HGFIN as well as the role of HGFIN when antagonists are used to block the NK receptors. This review is relevant for central and peripheral nervous system drug development and cancer targets and also discusses the indications for current patents.

快动系统作为药物干预的途径。
这篇综述讨论了一个受体家族,它与一个属于速激肽家族的小肽家族相互作用。速激素受体的三种亚型遵循以下建议的命名法:NK1、NK2和NK3。这些受体属于7-跨膜g蛋白偶联家族。NK受体家族与多种疾病、癌症、炎症和神经相关疾病有关。速动素NK受体及其配体与实体肿瘤和血液学肿瘤有关。NK受体拮抗剂已经合成,其中一些已经在临床前和II期临床研究中进行了测试。然而,为了有效地治疗,了解NK受体家族的生物学及其相关分子是必不可少的。其中一种分子是HGFIN,也被称为nmb和骨激活素。HGFIN特别重要,因为它已被证明与NK1的高亲和力配体p物质相互作用。本报告讨论了靶向NK受体的有希望的应用。讨论提出了当P物质与HGFIN相互作用时可能发生的潜在机制,以及当拮抗剂用于阻断NK受体时HGFIN的作用。本文综述了中枢和周围神经系统药物开发和肿瘤靶点,并讨论了当前专利的适应症。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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