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The ability to modulate cellular responses with light is the essence of photopharmacology. Photocontrollable peptides, capable of reversibly adopting either an active conformation or an inactive one, have been proven to successfully regulate disease-related processes. These bioactive compounds require suitable wavelengths, high photoconversions and physiological compatibility for their in vivo function. In this regard, novel photoswitches and their synthetic implementation into peptides open up new therapeutic opportunities for unexplored cellular targets. Altogether, these examples provide us with a collective comprehension of structure-related functional designs. Thus, in this book chapter, we summarize and discuss the most recent accomplishments in photoswitchable peptides focused on biology, which complements our review in Chemical Communications from 2019. Finally, we also suggest new possibilities to inspire chemical biologists in this field.

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