Deoxycytidine kinase inhibitor
WebNational Center for Biotechnology Information WebSep 12, 2013 · Abstract. Combined inhibition of ribonucleotide reductase and deoxycytidine kinase (dCK) in multiple cancer cell lines depletes deoxycytidine triphosphate pools …
Deoxycytidine kinase inhibitor
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WebWe demonstrate that while inhibition of deoxycytidine kinase will prevent the accumulation of dATP and induction of apoptosis to a large degree, inhibition of both … WebJun 25, 2024 · DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with antitumor activity. But, how does DI-82 protect against cancer cells via dCK? Let’s discuss it in …
WebMar 1, 2024 · Deoxycytidine kinase (dCK) inhibition triggers synthetic lethality in BRCA2-deficient contexts. Showing that dCK is a target of NorAdS was still insufficient to prove … WebNov 26, 2014 · Recently, we have shown that small molecule dCK inhibitors in combination with pharmacological perturbations of de novo dNTP biosynthetic pathways could …
Deoxycytidine kinase (dCK) phosphorylates several deoxyribonucleosides and their nucleoside analogues (a nucleoside with a sugar and a different nucleic acid base substitute or analogue that has unique properties when modified) using phosphate groups from ATP and UTP. More specifically, dCK adds the first … See more Deoxycytidine kinase (dCK) is an enzyme which is encoded by the DCK gene in humans. dCK predominantly phosphorylates deoxycytidine (dC) and converts dC into deoxycytidine monophosphate. … See more One method of to regulate both catalytic activity and substrate specificity is a post-translational modification on Serine 74, a residue in the insert region on each of the individual dCK subunits. Although serine 74 is far from dCK's active site, phosphorylation of … See more Deficiency of dCK is associated with resistance to antiviral and anticancer chemotherapeutic agents. Conversely, increased deoxycytidine kinase activity is associated with … See more dCK is a homodimer where each monomer subunit consists of multiple alpha helices surrounding a beta sheet core. Each subunit includes a nucleotide donor binding site, … See more dCK is a key enzyme in the nucleoside salvage pathway (NSP). More specifically, this pathway recycles preformed nucleosides from degrading DNA molecules to … See more • Nucleoside phosphorylase See more • Hazra S, Szewczak A, Ort S, Konrad M, Lavie A (April 2011). "Post-translational phosphorylation of serine 74 of human deoxycytidine kinase favors the enzyme adopting the open conformation making it competent for nucleoside binding and release" See more http://www.chem.ucla.edu/~jung/pdfs/303.pdf
WebDeoxycytidine kinase (dCK) is a rate-limiting enzyme in the deoxyribonucleoside salvage pathway and a critical determinant of therapeutic activity for several nucleoside analog prodrugs. We have previously reported the development of 1-(2′-deoxy-2′-18F-fluoro-β-d-arabinofuranosyl)cytosine (18F-FAC), a new probe for PET of dCK activity in immune …
WebAug 12, 2024 · TRE-515 is a potential first-in-class, orally administered, small molecule inhibitor of deoxycytidine kinase (dCK), the rate-limiting enzyme in the nucleoside salvage pathway. “Inflammation ... jcapzWebDecitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR) is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in … jcaraWebOct 10, 2014 · A series of deoxycytidine kinase inhibitors was simultaneously optimized for potency and PK properties. A co-crystal structure then allowed merging this series with a high throughput screening hit ... jcap ubsWebRemarkably, midostaurin is an oral multi-kinase inhibitor, with activity against not only FLT3 kinase but also KIT, VEGFR, PDGFR, and protein kinase C, and is well tolerated. 5,17 Preclinical studies have shown synergism between HMAs and midostaurin against FLT3-ITD AML . 5 Midostaurin in combination with azacytidine in a phase I/II study on ... jc aragonWebJul 1, 2024 · Deoxycytidine kinase (dCK) ... Reversine is a ATP-Competitive Aurora Kinase Inhibitor. dBET6, an Orally Active PROTAC Degrader of BET, Has Potential to Treat ALL. About The Author Louis Gilman. Email* Archives. March 2024 (16) February 2024 (18) January 2024 (14) December 2024 (21) kyaku japanese meaningWebClinical diagnosis of hepatocellular carcinoma (HCC) relies heavily on radiological imaging. However, information pertaining to liver cancer treatment such as the proliferation status is lacking. Imaging tumor proliferation can be valuable in patient management. This study investigated 18F-labeled clofarabine ([18F]CFA) targeting deoxycytidine kinase (dCK) … jcapxWebA series of deoxycytidine kinase inhibitors was simultaneously optimized for potency and PK properties. A co-crystal structure then allowed merging this series with a high throughput screening hit ... kyaku kyadaff biografia