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Increasing evidence suggests that intratumor microbiota are an intrinsic component in the tumor microenvironment across multiple cancer types, and that there is a close relationship between microbiota and tumor progression. Therefore, how to address the interaction between bacteria and malignances has become a growing concern. Tachyplesin I (TPI), a peptide with dual antimicrobial and antitumor effects, holds great promise as a therapeutic alternative for the aforementioned diseases, with the advantage of broad-spectrum activities, quick killing efficacy, and a low tendency to induce resistance. This review comprehensively summarizes the pharmacological mechanisms of TPI with an emphasis on its antimicrobial and antitumor potential. Furthermore, it presents advances in TPI derivatives and gives a perspective on their future development. The article is based on literature searches using PubMed and SciFinder to retrieve the most up-to-date information of TPI. Bacterial infections and cancer both pose a serious threat to health due to their symbiotic interactions and drug resistance. TPI is anticipated to be a novel agent to control pathogenic bacteria and various tumors through multiple mechanisms of action. Indeed, the continuous advancements in chemical modification and innovative applications of TPI give hope for future improvements in therapeutic efficacy.

Tachyplesin I and its derivatives: A pharmaco-chemical perspective on their antimicrobial and antitumor potential