Deoxycytidine kinase inhibitor
WebA 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 ... WebGemcitabine is a broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate …
Deoxycytidine kinase inhibitor
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WebDeoxycytidine kinase (dCK) inhibition is synthetic lethal with BRCA2 deficiency. Drug Resist Updat. 2024 Jan 22;67:100932. doi: 10.1016/j.drup.2024.100932. Online ahead of print. 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 …
WebJun 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 … WebHerein we describe the development of potent dCK inhibitors and demonstrate their in vivo efficacy using 18F-L-FAC PET as a noninvasive and clinically applicable PD biomarker. …
Web7.Effect of 5-aza-2'-deoxycytidine and Paclitaxel on the poorly differentiated gastric cancer cells甲基化转移酶抑制剂和紫杉醇对低分化胃癌细胞株的作用 ... 1.The co-effect of extracellular-signal regulated kinase mitogen-activated protein kinase signaling pathway inhibitor and DNA methyltransferase inhibitor on human ... WebDeoxycytidine is a deoxyribonucleoside, a component of deoxyribonucleic acid. It is similar to the ribonucleoside cytidine , but with one hydroxyl group removed from the C2' …
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 …
WebRemarkably, 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 ... summer money imagesWebApr 13, 2024 · Pevonedistat (NEDD-8 inhibitor) and APR-246 (TP53 reactivator) both did not meet trial endpoints. However, early phase trials of BCL-2, TIM3, and CD47 inhibitors have shown exciting data and are currently under phase 3 investigation. ... and impaired phosphorylation of decitabine due to mutations in deoxycytidine kinase (dCK) causing … palatine fire eligibility listWebNov 26, 2014 · Recently, we have shown that small molecule dCK inhibitors in combination with pharmacological perturbations of de novo dNTP biosynthetic pathways could … summer monday morning imagesWebJul 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 … palatine fireworks 2021http://www.chem.ucla.edu/~jung/pdfs/303.pdf summer monitor 02000WebDeoxycytidine kinase, which catalyzes the phosphorylation of deoxycytidine (dCR) to form deoxycytidine monophosphate in the presence of specific nucleoside 5′-triphosphates and a cation, has been purified about 100-fold from extracts of calf thymus. ... The inhibition produced by dCTP appeared to be competitive with the phosphate donor (ATP ... palatine flag footballDeoxycytidine 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 palatine flights