Tabriz University of Medical Sciences Pharmaceutical Sciences 1735-403X 27 4 2021 12 01 Recent Progress in Development of Polo-Like Kinase 1 Inhibitors: Efforts So Far 453 471 10.34172/PS.2021.19 EN Ramesh L. Sawant https://orcid.org/0000-0003-0064-7122 Jyoti B. Wadekar Rushikesh D. Ukirde Ganesh D. Barkade https://orcid.org/0000-0003-3836-3125 Journal Article 10.34172/PS.2021.19 2020 09 23 2021 04 15 Polo-like kinase 1(Plk1) plays an important role in the inhibition of cell proliferation and which is come under the family of serine/threonine-protein kinase. Which is a highly specific target for cancer therapy. In some clinical studies, Plk1 has been identified as a target for cancer. Currently, so many scientists are working on the development of the Plk1 inhibitors and so many scientists and researchers thinking about working on it. Recent strategy for Plk1 inhibition is the development of small molecule inhibitors which will inhibit the Plk1 through the ATP-binding site of the Plk. Now new generation Plk1 inhibitors being tested clinically which are targeting polo box domain. This review highlights the recent progress made in the development of Plk1 inhibitors as anticancer agents.