Development of allosteric and selective CDK2 inhibitors for ...
2023年6月3日 · In this paper, we will showcase a series of anthranilic acid-derived inhibitors that bind an allosteric pocket of cyclin-dependent kinase 2 (CDK2) with nanomolar affinity. CDK2 is …
In this paper, we will showcase a series of anthranilic acid-derived inhibitors that bind an allosteric pocket of cyclin-dependent kinase 2 (CDK2) with nanomolar afnity. fi CDK2 is a member...
Identification and Characterization of an Irreversible Inhibitor of CDK2
2015年9月17日 · We describe the first example of an irreversible inhibitor that targets CDK2 by grafting a reactive vinyl sulfone moiety onto a potent reversible CDK2 inhibitor. The structure …
Inhibition of the CDK2 and Cyclin A complex leads to ... - Nature
2022年5月20日 · Cyclin-dependent kinase 2 (CDK2) complex is significantly over-activated in many cancers. While it makes CDK2 an attractive target for cancer therapy, most inhibitors …
Structural and binding studies of cyclin-dependent kinase 2
Our data show that NU6140 binds to CDK2 with a Kd of 800 nM as determined by SPR and stabilizes the protein against thermal denaturation (ΔT m-5°C). The cocrystal structure …
2022年6月30日 · showcase a series of anthranilic acid-derived inhibitors that bind an allosteric pocket of cyclin-dependent kinase 2 (CDK2) with nanomolar affinity. CDK2 is a member of the …
Cyclin-Dependent Kinase 2 - an overview | ScienceDirect Topics
Cyclin-dependent kinase 2 (CDK2) is a MITF target gene that is involved in regulating the cell cycle. CDK2 expression appears to be essential for melanoma clonogenic growth, and in a …
Differences in the Conformational Energy Landscape of CDK1 and CDK2 …
2019年1月17日 · We next employed surface plasmon resonance (SPR) as an orthogonal technique to measure inhibitor binding to cyclin-free CDK1 and CDK2 (Table 2). Glutathione-S …
Discriminative SKP2 Interactions with CDK-Cyclin Complexes …
2021年3月3日 · We describe reconstitution of stable complexes containing SKP1-SKP2 and CDK1-cyclin B or CDK2-cyclin A/E, mediated by the CDK regulatory subunit CKS1. We further …
SPR-derived binding affinities of CDK2 for four peptides with and ...
Most inhibitors of Cyclin-dependent kinase 2 (CDK2) target its ATP-binding pocket. It is difficult, however, to use this pocket to design very specific inhibitors because this catalytic pocket...