Establishment of high-throughput screening HTRF assay for identification small molecule inhibitors of Skp2-Cks1.
S-phase kinase associated protein 2 (Skp2), a member of the F-box family that constitute the largest known class of ubiquitin E3 specificity components, is responsible for recognizing and recruiting cyclin-dependent kinase inhibitor p27 for its ubiquitination in the presence of the small accessory protein cyclin-dependent kinase regulatory subunit 1(Cks1). Skp2 ... is overexpressed in esophageal carcinoma tissues and closely related with tumor poor prognosis, and perturbation of the Skp2-Cks1 interaction by inhibitors or RNAi could inhibit the proliferation and metastasis of tumor cells. Therefore, inhibition of Skp2 function by small-molecule compounds targeting Skp2-Cks1 interaction is emerging as a promising and novel anti-cancer strategy. In this study, we establish an improved high-throughput screening platform to screen Skp2 inhibitors targeting Skp2-Cks1interaction, which may provide a new therapeutic approach for the clinic.
Mesh Terms:
Antineoplastic Agents, CDC2-CDC28 Kinases, Drug Screening Assays, Antitumor, Esophageal Neoplasms, Humans, Protein Kinase Inhibitors, S-Phase Kinase-Associated Proteins
Antineoplastic Agents, CDC2-CDC28 Kinases, Drug Screening Assays, Antitumor, Esophageal Neoplasms, Humans, Protein Kinase Inhibitors, S-Phase Kinase-Associated Proteins
Sci Rep
Date: Dec. 26, 2020
PubMed ID: 34702937
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