Results 261 to 270 of about 152,744 (302)

Dissecting the Determinants of Cyclin-Dependent Kinase 2 and Cyclin-Dependent Kinase 4 Inhibitor Selectivity

Journal of Medicinal Chemistry, 2006
Cyclin dependent kinases are a key family of kinases involved in cell cycle regulation and are an attractive target for cancer chemotherapy. The roles of four residues of the cyclin-dependent kinase active site in inhibitor selectivity were investigated by producing cyclin-dependent kinase 2 mutants bearing equivalent cyclin-dependent kinase 4 residues,
Pratt DJ, Bentley J, Jewsbury P, Boyle FT, Endicott JA, Noble MEM   +5 more
openaire   +4 more sources

Inhibitors of Cyclin-Dependent Kinase 1/2 for Anticancer Treatment

Medicinal Chemistry, 2020
Background: The cell cycle is regulated by cyclin-dependent kinases (CDKs) and their cognate cyclins, along with their endogenous inhibitors (CDKIs). CDKs act as central regulators in this process. Different CDKs play relevant roles in different phases.
Jiajia Mou, Yanru Deng, Danghui Chen
openaire   +3 more sources

Cyclin-dependent kinase 2 (cdk2) in the murine cdc2 kinaseTS mutant [PDF]

Somatic Cell and Molecular Genetics, 1992
Kinases of the mammalian cdc2 family including cdk2 (cyclin-dependent kinase 2) are thought to be involved in both the G2/M transition and DNA replication. To investigate the role of cdc2 kinase and cdk2 in cell cycle progression, murine tsFT210 cells bearing a temperature-sensitive cdc2 mutation were used.
Reiko Honda, Masakane Yamashita, Yoshitaka Nagahama, Yoshiki Ohba, Hideyo Yasuda, Masayuki Kamijo, Taisuke Nakata, Jun Ninomiya-Tsuji, Mayumi Nakamura   +8 more
openaire   +2 more sources

Purification and Crystallization of Human Cyclin-dependent Kinase 2

Journal of Molecular Biology, 1993
The major transitions of the eukaryotic cell cycle are triggered by cyclin-dependent protein kinases. We report the purification and crystallization of the catalytic subunit of human cyclin-dependent kinase 2 (CDK2), which has been implicated in the control of the G1/S transition.
Sung-Hou Kim, Jarmila Jancarik, Hendrik De Bondt, Jody Rosenblatt, David O. Morgan   +4 more
openaire   +3 more sources

Regulation of Cyclin-Dependent Kinase 2 Activity by Ceramide

Experimental Cell Research, 2000
Cyclin-dependent kinases have been implicated in the inactivation of retinoblastoma (Rb) protein and cell cycle progression. Recent studies have demonstrated that the lipid molecule ceramide is able to induce Rb hypophosphorylation leading to growth arrest and cellular senescence.
J.Y. Lee, Alicja Bielawska, Lina M. Obeid   +2 more
openaire   +3 more sources

Structural and binding studies of cyclin‐dependent kinase 2 with NU6140 inhibitor

Chemical Biology & Drug Design, 2021
AbstractCyclin‐dependent kinase 2 (CDK2) is an established target protein for therapeutic intervention in various diseases, including cancer. Reported inhibitors of CDK2 target the ATP‐binding pocket to inhibit the kinase activity. Many small molecule CDK2 inhibitors have been discovered, and their crystal structure with CDK2 or CDK2–cyclin A complex ...
Sumalatha Rani Talapati, Megha Goyal, Vijayashankar Nataraj, Manoj Pothuganti, Sreevidya M. R, Suraj Gore, Murali Ramachandra, Thomas Antony, Sunil S. More, Narasimha K. Rao   +9 more
openaire   +3 more sources

A flavonoid gossypin binds to cyclin-dependent kinase 2

Bioorganic & Medicinal Chemistry Letters, 2008
Flavonoids have low toxicity and mild activity. In order to find flavonoids showing cyclin-dependent kinase 2 (CDK2) binding effects, 347 flavonoid derivatives were docked into the crystal structure of the CDK2. The docking study showed that gossypin has a good conformational match with CDK2, which was confirmed by the binding affinity assay using NMR ...
Hojung Kim, Ji Hye Kim, Youhoon Chong, Yoongho Lim, Eun-Jung Lee, Bora Jung, Joong-Hoon Ahn   +6 more
openaire   +3 more sources

Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update

Journal of Medicinal Chemistry, 2018
Cyclin-dependent kinase 2 (CDK2) drives the progression of cells into the S- and M-phases of the cell cycle. CDK2 activity is largely dispensable for normal development, but it is critically associated with tumor growth in multiple cancer types. Although the role of CDK2 in tumorigenesis has been controversial, emerging evidence proposes that selective
Solomon Tadesse, Shudong Wang, Elizabeth C. Caldon, Elizabeth C. Caldon, Wayne D. Tilley   +4 more
openaire   +5 more sources

A comprehensive bioinformatic analysis of cyclin-dependent kinase 2 (CDK2) in glioma

Gene, 2022
Glioma is one of the most prevalent malignant brain tumors and its incidence is rising continuously in recent years. Studies suggested that the regulatory mechanism of CDK2 in glioma might different from most of the other cancer types METHODS: Data were accessed from TCGA, GTEx, CGGA, CancerSEA, and TISCH.
Hengrui Liu, Jieling Weng
openaire   +2 more sources

Cyclin-dependent kinase 2 regulates the interaction of Axin with β-catenin

Biochemical and Biophysical Research Communications, 2004
Axin, a negative regulator of Wnt, forms a complex with glycogen synthase kinase 3beta, beta-catenin, and adenomatous polyposis coli and promotes GSK3beta-dependent phosphorylation of beta-catenin, thereby stimulating degradation of the beta-catenin. An essential step in that process is the phosphorylation of Axin.
Sung Il Kim, Mi Su Lee, Chun Shik Park, Eek-hoon Jho, Woo Keun Song, Min Seong Kwon   +5 more
openaire   +3 more sources