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Venoms as a platform for human drugs: translating toxins into therapeutics.

机译:毒液作为人类药物的平台:将毒素转化为治疗剂。

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INTRODUCTION: An extraordinarily diverse range of animals have evolved venoms for predation, defence, or competitor deterrence. The major components of most venoms are peptides and proteins that are often protease-resistant due to their disulfide-rich architectures. Some of these toxins have become valuable as pharmacological tools and/or therapeutics due to their extremely high specificity and potency for particular molecular targets. There are currently six FDA-approved drugs derived from venom peptides or proteins. AREAS COVERED: This article surveys the current pipeline of venom-derived therapeutics and critically examines the potential of peptide and protein drugs derived from venoms. Emerging trends are identified, including an increasing industry focus on disulfide-rich venom peptides and the use of a broader array of molecular targets in order to develop venom-based therapeutics for treating a wider range of clinical conditions. EXPERT OPINION: Key technical advances in combination with a renewed industry-wide focus on biologics have converged to provide a larger than ever pipeline of venom-derived therapeutics. Disulfide-rich venom peptides obviate some of the traditional disadvantages of therapeutic peptides and some may be suitable for oral administration. Moreover, some venom peptides can breach the blood brain barrier and translocate across cell membranes, which opens up the possibility of exploiting molecular targets not previously accessible to peptide drugs.
机译:简介:种类繁多的动物已经进化出毒液来捕食,防御或威慑对手。大多数毒液的主要成分是肽和蛋白质,由于它们富含二硫键的结构而经常具有蛋白酶抗性。这些毒素中的一些由于其对特定分子靶标的极高的特异性和效力,已成为有价值的药理工具和/或治疗剂。目前有六种FDA批准的毒液肽或蛋白质衍生药物。涵盖的领域:本文调查了毒液衍生治疗剂的当前开发流程,并严格审查了毒液衍生的肽和蛋白质药物的潜力。确定了新兴趋势,包括业界日益关注富含二硫键的毒液肽,以及使用更广泛的分子靶标来开发基于毒液的疗法,以治疗更广泛的临床疾病。专家意见:关键技术进步与全行业对生物制剂的重新关注相结合,已提供了比以往任何时候都更多的毒液治疗药物。富含二硫键的毒液肽消除了治疗性肽的一些传统缺点,有些可能适合口服。此外,某些毒肽可以突破血脑屏障并在细胞膜上移位,这为开发利用肽类药物以前无法获得的分子靶标提供了可能性。

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