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TRPA1 as an Analgesic Target

机译：TRPA1作为止痛目标

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Humans have cultivated chili peppers for over 5,000 years. For more than 1,000 years extracts from theseplants have been used medicinally in the treatment of various forms of pain. As a result, pain researchers have had a longstandinginterest in the molecular identity of the receptor for capsaicin, the chemical that produces the sensation of heatfrom “hot” peppers. When the Julius lab published that TRPV1 is the protein that confers capsaicin responsiveness [1],there was already significant investigation of this target in the pharmaceutical community. The future of TRPV1 as ananalgesic target is currently uncertain because inhibiting TRPV1 attenuates patients' ability to sense damaging heat [2,3] and because concerns have arisen that TRPV1 antagonists cause a transient hyperthermia. However, this interest inTRPV1 has spurred interest in a variety of other TRP channels in the pain area. As the receptor for mustard oil and othernoxious compounds that cause pain, TRPA1 in particular has emerged as a promising target. Recent data suggest thatTRPA1 is a broad chemosensor, activated by reactive chemicals that are encountered exogenously and by compoundssuch as hydrogen peroxide that are endogenously produced during inflammation or tissue damage. In this review, weexplore the rationale surrounding the use of TRPA1 as an analgesic target and discuss the unique challenges that facethose developing antagonists.
机译：人类已经栽培了5,000多年的辣椒。这些植物的提取物已在医学中用于治疗各种形式的疼痛已有1000多年的历史了。结果，疼痛研究人员对辣椒素受体的分子身份有着长期的兴趣，辣椒素是一种通过“辣椒”产生热量的化学物质。当朱利叶斯实验室发表TRPV1是赋予辣椒素反应性的蛋白质时[1]，在制药界已经对该目标进行了重大研究。 TRPV1作为镇痛药的目标目前尚不确定，因为抑制TRPV1会减弱患者感觉到破坏性热量的能力[2,3]，并且由于人们担心TRPV1拮抗剂会导致短暂的体温过高。但是，对TRPV1的这种兴趣激发了对疼痛区域中各种其他TRP渠道的兴趣。作为芥子油和其他引起疼痛的有毒化合物的受体，TRPA1尤其已成为有希望的目标。最近的数据表明，TRPA1是一种广泛的化学传感器，可被外源遇到的反应性化学物质以及炎症或组织损伤过程中内生的化合物（例如过氧化氢）激活。在这篇综述中，我们探讨了将TRPA1用作镇痛目标的基本原理，并讨论了那些正在发展的拮抗剂所面临的独特挑战。

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