The fascination and fear of snakes dates back to time immemorial, with the first scientific treatise on snakebite envenoming, the Brooklyn Medical Papyrus, dating from ancient Egypt. Owing to their lethality, snakes have often been associated with images of perfidy, treachery and death. However, snakes did not always have such negative connotations. The curative capacity of venom has been known since antiquity, also making the snake a symbol of pharmacy and medicine. Today, there is renewed interest in pursuing snake-venom-based therapies. This Review focuses on the chemistry of snake venom and the potential for venom to be exploited for medicinal purposes in the development of drugs. The mixture of toxins that constitute snake venom is examined, focusing on the molecular structure, chemical reactivity and target recognition of the most bioactive toxins, from which bioactive drugs might be developed. The design and working mechanisms of snake-venom-derived drugs are illustrated, and the strategies by which toxins are transformed into therapeutics are analysed. Finally, the challenges in realizing the immense curative potential of snake venom are discussed, and chemical strategies by which a plethora of new drugs could be derived from snake venom are proposed.

对蛇的迷恋和恐惧可以追溯到远古时代，第一部关于蛇咬伤的科学论文是古埃及的布鲁克林医学纸莎草纸。由于其致命性，蛇常常与背信弃义、背叛和死亡的形象联系在一起。然而，蛇并不总是有这样的负面含义。蛇毒的治疗能力自古以来就为人所知，这也使蛇成为药剂和医学的象征。如今，人们对基于蛇毒的疗法重新产生了兴趣。本综述重点关注蛇毒的化学性质以及蛇毒在药物开发中用于医疗目的的潜力。对构成蛇毒的毒素混合物进行了检查，重点关注最具生物活性的毒素的分子结构、化学反应性和目标识别，从中可以开发出生物活性药物。阐述了蛇毒药物的设计和作用机制，并分析了将毒素转化为治疗药物的策略。最后，讨论了实现蛇毒巨大治疗潜力所面临的挑战，并提出了从蛇毒中提取大量新药的化学策略。