Results 41 to 50 of about 377,374 (415)

The cyclin dependent kinase inhibitor Roscovitine prevents diet-induced metabolic disruption in obese mice

open access: yesScientific Reports, 2021
Most strategies to treat obesity-related disorders have involved prevention of diet-induced weight gain in lean mice. Treatment of obese individuals will require therapies that reverse the detrimental effects of excess body weight.
Nabil Rabhi   +6 more
doaj   +1 more source

Regulation of signal duration and the statistical dynamics of kinase activation by scaffold proteins [PDF]

open access: yesPLoS Comput Biol. 2008 Jun 27;4(6):e1000099, 2008
Scaffolding proteins that direct the assembly of multiple kinases into a spatially localized signaling complex are often essential for the maintenance of an appropriate biological response. Although scaffolds are widely believed to have dramatic effects on the dynamics of signal propagation, the mechanisms that underlie these consequences are not well ...
arxiv   +1 more source

Discovery and development of Seliciclib. How systems biology approaches can lead to better drug performance [PDF]

open access: yes, 2015
Seliciclib (R-Roscovitine) was identified as an inhibitor of CDKs and has undergone drug development and clinical testing as an anticancer agent. In this review, the authors describe the discovery of Seliciclib and give a brief summary of the biology of ...
Cavicchi, Laura   +4 more
core   +4 more sources

Physicochemical Properties of analogs α-Aminophosphonates Drugs Determined via Molecular Dynamics Simulation

open access: yesAsian Pacific Journal of Cancer Biology, 2019
Objective: Cyclin-dependent kinases (CDKs, play important roles in cell cycle regulation. Since deregulation of cyclins and/or alteration or absence of inhibitors has been associated with many cancers, there is strong interest in CDKs inhibitors that ...
Reihaneh Sabbaghzadeh
doaj   +1 more source

Prediction of kinase inhibitor response using activity profiling, in-vitro screening, and elastic net regression [PDF]

open access: yesBMC Systems Biology 2014, 8:74, 2013
Many kinase inhibitors have been approved as cancer therapies. Recently, libraries of kinase inhibitors have been extensively profiled, thus providing a map of the strength of action of each compound on a large number of its targets. These profiled libraries define drug-kinase networks that can predict the effectiveness of new untested drugs and ...
arxiv   +1 more source

The emerging roles and therapeutic potential of cyclin-dependent kinase 11 (CDK11) in human cancer. [PDF]

open access: yes, 2016
Overexpression and/or hyperactivation of cyclin-dependent kinases (CDKs) are common features of most cancer types. CDKs have been shown to play important roles in tumor cell proliferation and growth by controlling cell cycle, transcription, and RNA ...
Duan, Zhenfeng   +4 more
core   +1 more source

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.

open access: yesAngewandte Chemie, 2019
Cyclin-dependent kinases 4 and 6 (CDK4/6) are key regulators of the cell cycle, and there are FDA-approved CDK4/6 inhibitors for treating patients with metastatic breast cancer.
Baishan Jiang   +6 more
semanticscholar   +1 more source

Signalling, cell cycle and pluripotency in embryonic stem cells [PDF]

open access: yes, 2002
International ...
Burdon, Tom   +2 more
core   +1 more source

Are all cyclin-dependent kinases 4/6 inhibitors created equal?

open access: yesnpj Breast Cancer, 2019
The harnessing in clinical practice of cyclin-dependent kinases 4/6 inhibitors, namely palbociclib, ribociclib, and abemaciclib, has substantially changed the therapeutic approach for hormone receptor-positive metastatic breast cancer (BC).
A. Marra, G. Curigliano
semanticscholar   +1 more source

Identification and characterization of an irreversible inhibitor of CDK2 [PDF]

open access: yes, 2015
Irreversible inhibitors that modify cysteine or lysine residues within a protein kinase ATP binding site offer, through their distinctive mode of action, an alternative to ATP-competitive agents.
Anscombe, Elizabeth   +16 more
core   +1 more source

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