Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01359
Abstract: The polo-box domain (PBD) of Plk1 is a promising target for cancer therapeutics. We designed and synthesized novel phosphorylated macrocyclic peptidomimetics targeting PBD based on acyclic phosphopeptide PMQSpTPL. The inhibitory activities of 16e on Plk1-PBD… read more here.
Keywords: plk1; box domain; pbd; plk1 pbd ... See more keywords
Identification of novel potent peptide inhibitors targeting the polo-box domain of PLK1: structure-based pharmacophore modelling, virtual screening, molecular docking, molecular dynamics study and biological evaluation
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2025.2563601
Abstract: Abstract Multiple myeloma, a hematological malignancy, shows PLK1 overexpression in cells correlates with poor prognosis, suggesting PLK1 as a potential therapeutic target. In this study, we discovered five peptides (PLs 1–5) targeting the polo box… read more here.
Keywords: virtual screening; box domain; targeting polo; polo box ... See more keywords
Inhibitors of the PLK1 polo-box domain: drug design strategies and therapeutic opportunities in cancer
Sign Up to like & getrecommendations! Published in 2022 at "Expert Opinion on Drug Discovery"
DOI: 10.1080/17460441.2023.2159942
Abstract: ABSTRACT Introduction Polo Like Kinase 1 (PLK1) is a key regulator of mitosis and its overexpression is frequently observed in a wide variety of human cancers, while often being associated with poor survival rates. Therefore,… read more here.
Keywords: pbd; polo box; inhibitors plk1; plk1 polo ... See more keywords