Abstract
Venomous animals on the earth have been found to be valuable resources for the development of therapeutics. Enzymatic and non-enzymatic proteins and peptides are the major components of animal venoms, many of which can target various ion channels, receptors, and membrane transporters. Compared to traditional small molecule drugs, natural proteins and peptides exhibit higher specificity and potency to their targets. In this review, we summarize the varieties and characteristics of toxins from a few representative venomous animals, and describe the components and applications of animal toxins as potential drug candidates in the treatment of human diseases, including cancer, neurodegenerative diseases, cardiovascular diseases, neuropathic pain, as well as autoimmune diseases. In the meantime, there are many obstacles to translate new toxin discovery to their clinical applications. The challenges, strategies, and perspectives in the development of the protein toxin-based drugs are discussed as well.
Highlights
Animal venoms are composed of varieties of proteins and peptides fine-tuned by millions of years of evolution
The numbers of disulfide bonds vary in different venomous species, such as 10–40 cysteine residues have been found in cone snails, 40–80 residues in scorpions and snakes, with remarkable structural diversities resulted from long-term selective pressure and coevolution process
Protein toxins show multiple advantages compared to small molecule drugs for therapeutic applications, such as higher potency and selectivity, they still face many challenges, such as the short circulating half-life, the lack of membrane permeability, and poor oral bioavailability as well
Summary
Animal venoms are composed of varieties of proteins and peptides fine-tuned by millions of years of evolution. These toxins target multiple ion channels, receptors, and enzymes with high potency and sometimes exquisite selectivity, attracting much attention to further investigate their pharmacological and physiological properties. Toxins synthesized by venomous animals from both terrestrial animals and marine animals, such as scorpions, snakes, spiders, bees, cone snails, and sea anemones, are injected into the body for hunt or defense by animal wounding apparatus, such as fangs, barbs, spines, and stingers. Some venomous animals have been used to treat diseases for millennia in many parts of the world. As an example, has been used to treat spasms and endogenous wind in traditional Chinese medicine. Many important effects have been discovered when studying the functionality of
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