Results 21 to 30 of about 215,802 (313)

Identification of abemaciclib derivatives targeting cyclin-dependent kinase 4 and 6 using molecular dynamics, binding free energy calculation, synthesis, and pharmacological evaluation

Frontiers in Pharmacology, 2023
CDK4/6 plays a crucial role in various cancers and is an effective anticancer drug target. However, the gap between clinical requirements and approved CDK4/6 drugs is unresolved.
Yanting Zhou, Xiandeng Li, Peifang Luo, Huiting Chen, Yan Zhou, Xueting Zheng, Yuan Yin, Haoche Wei, Hongji Liu, Wen Xia, Mingsong Shi, Xiaoan Li   +11 more
doaj   +1 more source

T-loop phosphorylation of Arabidopsis CDKA;1 is required for its function and can be partially substituted by an aspartate residue [PDF]

, 2007
As in other eukaryotes, progression through the cell cycle in plants is governed by cyclin-dependent kinases. Phosphorylation of a canonical Thr residue in the T-loop of the kinases is required for high enzyme activity in animals and yeast.
Dissmeyer, N., , Nowack, M., Pusch, S., Stals, H., Inzé, D., Grini, P., Schnittger, A.   +7 more
core   +2 more sources

A combination of STI571 and BCR-ABL1 siRNA with overexpressed p15INK4B induced enhanced proliferation inhibition and apoptosis in chronic myeloid leukemia

Brazilian Journal of Medical and Biological Research, 2014
p15INK4B, a cyclin-dependent kinase inhibitor, has been recognized as a tumor suppressor. Loss of or methylation of the p15INK4B gene in chronic myeloid leukemia (CML) cells enhances myeloid progenitor formation from common myeloid progenitors. Therefore,
D.Y. Xia, L. Liu, M.W. Hao, Q. Liu, R.A. Chen, Y.M. Liang   +5 more
doaj   +1 more source

The cyclin-dependent kinase inhibitor p57(Kip2) is epigenetically regulated in carboplatin resistance and results in collateral sensitivity to the CDK inhibitor seliciclib in ovarian cancer [PDF]

, 2012
Carboplatin remains a first-line agent in the management of epithelial ovarian cancer (EOC). Unfortunately, platinum-resistant disease ultimately occurs in most patients.
A Bali, C Beretta, D P Lovell, E Papacharalbous, E Rosenberg, G D’Andrilli, H M Coley, HM Coley, I-S Song, K Madhuri, MA Levesque, N A M Safuwan, N Syed, N Syed, P Chivers, P Vlachos, P Zhang, PS Larson, RM Glasspool, S Butler-Manuel, SH Wei, ST Kim, T Crook, T Giannopoulos, T Kobatake, V Masciullo, W Roeb, Y Ma   +27 more
core   +1 more source

The Renaissance of Cyclin Dependent Kinase Inhibitors [PDF]

Cancers, 2022
Cyclin-dependent kinases (CDK) regulate cell cycle progression. During tumor development, altered expression and availability of CDKs strongly contribute to impaired cell proliferation, a hallmark of cancer. In recent years, targeted inhibition of CDKs has shown considerable therapeutic benefit in a variety of tumor entities. Their success is reflected
Ettl, Tobias, Schulz, Daniela, Bauer, Richard J.   +2 more
openaire   +3 more sources

Trisubstituted pyrazolopyrimidines as novel angiogenesis inhibitors. [PDF]

, 2013
Current inhibitors of angiogenesis comprise either therapeutic antibodies (e.g. bevacicumab binding to VEGF-A) or small molecular inhibitors of receptor tyrosin kinases like e.g. sunitinib, which inhibits PDGFR and VEGFR.
Fürst, Robert, Gucký, Tomáš, Havlíček, Libor, Krystof, Vladimir, Liebl, Johanna, Strnad, Miroslav, Vollmar, Angelika M., Weitensteiner, Sabine B., Zahler, Stefan   +8 more
core   +5 more sources

Cyclin-dependent kinase 7 inhibitor THZ1 in cancer therapy

Chronic Diseases and Translational Medicine, 2019
Current cancer therapies have encountered adverse response due to poor therapeutic efficiency, severe side effects and acquired resistance to multiple drugs. Thus, there are urgent needs for finding new cancer-targeted pharmacological strategies. In this
Bin-Bin Li, Bo Wang, Cheng-Ming Zhu, Di Tang, Jun Pang, Jing Zhao, Chun-Hui Sun, Miao-Juan Qiu, Zhi-Rong Qian   +8 more
doaj   +1 more source

The novel mTOR inhibitor RAD001 (Everolimus) induces antiproliferative effects in human pancreatic neuroendocrine tumor cells [PDF]

, 2007
Background/Aim: Tumors exhibiting constitutively activated PI(3) K/Akt/mTOR signaling are hypersensitive to mTOR inhibitors such as RAD001 (everolimus) which is presently being investigated in clinical phase II trials in various tumor entities, including
Albert JM, Auernhammer CJ, Boulay A, Boulay A, Bousquet C, Burkhard Göke, Cao C, Christoph J. Auernhammer, Enrico N. De Toni, Faivre S, Gerald Spöttl, Grewe M, Heinrich H.D. Meyer, Hosoi H, Jeng YJ, Jennifer Meinecke, Kathrin Zitzmann, Kawamata S, Kirchner GI, Luo J, O?Reilly KE, Oberg K, Ramage JK, Sawyers CL, Shah T, Shaw RJ, Stephan Brand, Sun SY, Vignot S, von Wichert G, Wang L, Wanner K, Wendel HG, Wullschleger S, Yao JC, Yee KW   +35 more
core   +1 more source

Upregulation of cyclin-dependent kinase inhibitors CDKN1B and CDKN1C in hepatocellular carcinoma-derived cells via goniothalamin-mediated protein stabilization and epigenetic modifications

Toxicology Reports, 2015
Cell cycle deregulation is common in human hepatocellular carcinoma (HCC). To ensure proper cell cycle controlling, cyclin/cyclin-dependent kinases (CDK) complexes are tightly regulated by CDK inhibitors (CKIs) in normal cells.
Yu-Ting Peng, Wen-Ren Wu, Lih-Ren Chen, Kung-Kai Kuo, Cheng-Hui Tsai, Yu-Ting Huang, Yu-Hsuan Lan, Fang-Rong Chang, Yang-Chang Wu, Yow-Ling Shiue   +9 more
doaj   +1 more source

Dbf4-Cdc7 (DDK) Inhibitor PHA-767491 Displays Potent Anti-Proliferative Effects via Crosstalk with the CDK2-RB-E2F Pathway

Biomedicines, 2022
Precise regulation of DNA replication complex assembly requires cyclin-dependent kinase (CDK) and Dbf4-dependent kinase (DDK) activities to activate the replicative helicase complex and initiate DNA replication. Chemical probes have been essential in the
Tekle Pauzaite, James Tollitt, Betul Sopaci, Louise Caprani, Olivia Iwanowytsch, Urvi Thacker, John G. Hardy, Sarah L. Allinson, Nikki A. Copeland   +8 more
doaj   +1 more source