Deoxycytidine kinase inhibitor
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 … 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 ...
Deoxycytidine kinase inhibitor
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Web57 rows · Decitabine is a DNA methyltransferase inhibitor that targets DNA (cytosine-5)-methyltransferase 1 (DNMT1), interacts with deoxycytidine kinase, and displays …
WebDec 2, 2009 · Deoxycytidine kinase (dCK) is a rate-limiting enzyme in deoxyribonucleoside salvage, a metabolic pathway that recycles products of DNA degradation. dCK phosphorylates and therefore activates nucleoside analog prodrugs frequently used in cancer, autoimmunity, and viral infections. In contrast to its well established therapeutic … http://www.chem.ucla.edu/~jung/pdfs/303.pdf
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 … WebJul 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)
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
WebJul 1, 2024 · DI-87, an orally active and selective dCK inhibitor, has antitumor activity and is used in combination therapy against tumors expressing dCK. DI-87 is an Orally Active … primo professional water cooler reviewWebHerein 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. … primo professional water coolerWebJul 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 … play store app vidmateWebNov 10, 2024 · Murphy, J. M. et al. Development of new deoxycytidine kinase inhibitors and noninvasive in vivo evaluation using positron emission tomography. J. Med. Chem. … primo property management manchesterWebNational Center for Biotechnology Information primo professional water dispenser manualWebJan 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 ... primo property management nw limitedWebDeoxycytidine 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. primo pro series water cooler