<p>Lasso peptides, a significant group of ribosomally synthesized and post-translationally modified peptides (RiPPs), have emerged as potential therapeutic agents owing to their unique structural features and diverse biological activities. These peptides are characterized by an isopeptide-bonded macrolactam ring and a tail threaded through the ring, forming a distinctive lasso structure that provides remarkable stability and functionality, leading to significant therapeutic potential for antimicrobial, antiviral, anticancer, and anti-inflammatory applications. This review highlights the structural diversity and therapeutic applications of lasso peptides, emphasizing their potential as next-generation therapeutics. Additionally, while their mechanisms of action and innovative therapeutic prospects are explored, the challenges and limitations associated with their use are also discussed.</p>