Inhibitors of the PLK1 polo-box domain: drug design strategies and therapeutic opportunities in cancer
JM Stafford, MD Wyatt, C McInnes - Expert Opinion on Drug …, 2023 - Taylor & Francis
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 …
overexpression is frequently observed in a wide variety of human cancers, while often being …
Plk1-targeted small molecule inhibitors: molecular basis for their potency and specificity
Members of polo-like kinases (collectively, Plks) have been identified in various eukaryotic
organisms and play pivotal roles in cell proliferation. They are characterized by the presence …
organisms and play pivotal roles in cell proliferation. They are characterized by the presence …
Inhibitors of the Polo‐Box Domain of Polo‐Like Kinase 1
A Berg, T Berg - ChemBioChem, 2016 - Wiley Online Library
Abstract Polo‐like kinase 1 (Plk1), a key player in mitosis, is overexpressed in a wide range
of tumor types and has been validated as a target for tumor therapy. In addition to its N …
of tumor types and has been validated as a target for tumor therapy. In addition to its N …
Identification of a new heterocyclic scaffold for inhibitors of the polo-box domain of polo-like kinase 1
As a mitotic-specific target widely deregulated in various human cancers, polo-like kinase 1
(Plk1) has been extensively explored for anticancer activity and drug discovery. Although …
(Plk1) has been extensively explored for anticancer activity and drug discovery. Although …
Structure-activity and mechanistic studies of non-peptidic inhibitors of the PLK1 polo box domain identified through REPLACE
SN Craig, M Baxter, D Chapagai, JM Stafford… - European journal of …, 2022 - Elsevier
Abstract Polo-like kinase 1 (PLK1) is a serine/threonine-protein kinase involved in cell cycle
regulation and mitotic progression. Studies have shown that PLK1 is upregulated in many …
regulation and mitotic progression. Studies have shown that PLK1 is upregulated in many …
Development of bifunctional inhibitors of polo‐like kinase 1 with low‐nanomolar activities against the polo‐box domain
A Scharow, D Knappe, W Reindl, R Hoffmann… - …, 2016 - Wiley Online Library
Abstract Polo‐like kinase 1 (Plk1), a validated cancer target, harbors a protein–protein
interaction domain referred to as the polo‐box domain (PBD), in addition to its enzymatic …
interaction domain referred to as the polo‐box domain (PBD), in addition to its enzymatic …
Novel macrocyclic peptidomimetics targeting the polo-box domain of polo-like kinase 1
The polo-box domain (PBD) of Plk1 is a promising target for cancer therapeutics. We
designed and synthesized novel phosphorylated macrocyclic peptidomimetics targeting …
designed and synthesized novel phosphorylated macrocyclic peptidomimetics targeting …
Polo-like kinases inhibitors
L Garuti, M Roberti, G Bottegoni - Current medicinal chemistry, 2012 - ingentaconnect.com
Polo-like kinases (PLKs) are a family of serine/threonine kinases that play crucial roles in
multiple stages of mitosis. PLK1 is the most studied member of the family. It is overexpressed …
multiple stages of mitosis. PLK1 is the most studied member of the family. It is overexpressed …
Targeting subcellular localization through the polo-box domain: non-ATP competitive inhibitors recapitulate a PLK1 phenotype
C McInnes, K Estes, M Baxter, Z Yang, DB Farag… - Molecular cancer …, 2012 - AACR
The polo-box domain (PBD) has critical roles in the mitotic functions of polo-like kinase 1
(PLK1). The replacement with partial ligand alternative through computational enrichment …
(PLK1). The replacement with partial ligand alternative through computational enrichment …
Optimized Plk1 PBD inhibitors based on poloxin induce mitotic arrest and apoptosis in tumor cells
A Scharow, M Raab, K Saxena… - ACS chemical …, 2015 - ACS Publications
Polo-like kinase 1 (Plk1) is a central regulator of mitosis and has been validated as a target
for antitumor therapy. The polo-box domain (PBD) of Plk1 regulates its kinase activity and …
for antitumor therapy. The polo-box domain (PBD) of Plk1 regulates its kinase activity and …