Deoxycytidine kinase inhibitor
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 … WebDec 1, 2009 · 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 to afford a highly potent, selective and orally bioavailable inhibitor, compound 10.This compound showed dose dependent inhibition of …
Deoxycytidine kinase inhibitor
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WebJul 20, 2024 · The inhibition of RNR by gemcitabine has been reported to lead to depletion of dCTP, a potent feedback inhibitor of deoxycytidine kinase, leading to a more efficient phosphorylation of gemcitabine. Moreover, since gemcitabine competes with dCTP, a decrease in dCTP pools increases incorporation of gemcitabine into DNA, a mechanism … http://www.chem.ucla.edu/~jung/pdfs/303.pdf
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 WebNational Center for Biotechnology Information
WebPTHR10513:SF19 DEOXYCYTIDINE KINASE 1 hit; PTHR10513 DEOXYNUCLEOSIDE KINASE 1 hit; PIRSF. PIRSF000705 DNK 1 hit; Pfam. View protein in Pfam; PF01712 dNK 1 hit; SUPFAM. SSF52540 P-loop containing nucleoside triphosphate hydrolases 1 … WebApr 12, 2024 · Indeed, HMAs are prodrugs, whose activation requires phosphorylation by the uridine-cytidine kinase (UCK) and deoxycytidine kinase (DCK) . ... Emavusertib (EMA) is a small molecule kinase inhibitor that blocks a serine/threonine kinase belonging to the interleukin one receptor-associated kinase four (IRAK4) family. Spliceosome mutations ...
WebDI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK [1] . (S)-DI-87 …
WebOct 20, 2015 · Identifying enzymes that, once introduced in cancer cells, lead to an increased efficiency of treatment constitutes an important goal for biomedical applications. Using an original procedure whereby mutant genes are generated based on the use of conditional lentivector genome mobilisation, we recently described, for the first time, the … camo trim fit shirt for valentine\u0027s dayWebRemarkably, 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 ... first rule of kpopWebGemcitabine is a broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate … camo tropicl knee pad pantsWebDeoxycytidine is a deoxyribonucleoside, a component of deoxyribonucleic acid. It is similar to the ribonucleoside cytidine , but with one hydroxyl group removed from the C2' … camo tripod deer stand coversWebJan 31, 2001 · Deoxycytidine kinase (dCK) is the main enzyme in the salvage of deoxyribonucleosides as a consequence of its broad substrate specificity. dCK is the only enzyme that can supply cells with all four ... first rule of screenwritingWebJun 1, 2014 · A new analytical method for determining deoxycytidine kinase (dCK) activity in biological milieus using luminescence is reported here. This method, based on utilizing adenosine triphosphate (ATP) as the sole phosphate donor in the kinase reaction and monitoring ATP consumption via a luciferase-based chemiluminescence reaction, is … camo trooper helmetWebWe demonstrate that while inhibition of deoxycytidine kinase will prevent the accumulation of dATP and induction of apoptosis to a large degree, inhibition of both … camo trumpet hat