• Thymidine kinase from herpesvirus is a sub-family of thymidine kinases that catalyses the transfer of phospho group of ATP to thymidine to generate thymidine monophosphate, which serves as a substrate during viral DNA replication. (wikipedia.org)
  • Such antivirals include: Purine analogues of guanine: Aciclovir, Famciclovir, Ganciclovir, Penciclovir, Valaciclovir, Valganciclovir Vidarabine Pyrimidine analogues of uridine: Idoxuridine, Trifluridine Brivudine Mutations in the gene coding thymidine kinase in herpes viruses can endow the virus with resistance to aciclovir. (wikipedia.org)
  • Foscarnet does not require activation (phosphorylation) by thymidine kinase or other kinases. (nih.gov)
  • B3 Ku binds to the C-terminal region of DNA-PK (amino acids 3002-3850) near the protein kinase domain (Jin et al. (nih.gov)
  • B10 HMG1 or 2 compete with Ku for binding to DNA-PK and stimulate DNA-dependent kinase activity in vitro in the absence of Ku (Yumoto et al. (nih.gov)
  • The cell line also contains a Renilla reporter driven by the thymidine kinase (TK) promoter to act as an internal control. (cancertools.org)
  • Glucocorticoids inhibit transcription of the murine cytoplasmic thymidine kinase gene (Tk-1). (elsevierpure.com)
  • A 140-bp fragment, extending from -143 to -3 bp with respect to the thymidine kinase translational start site, was capable of both basal and glucocorticoid-regulated transcription of reporter genes. (elsevierpure.com)
  • This element, when fused to upstream activation sequences from the herpes simplex virus thymidine kinase promoter, conveys glucocorticoid sensitivity in cis. (elsevierpure.com)
  • Rhee, K & Thompson, EA 1996, ' Glucocorticoid regulation of a transcription factor that binds an initiator-like element in the murine thymidine kinase (Tk-1) promoter ', Molecular Endocrinology , vol. 10, no. 12, pp. 1536-1548. (elsevierpure.com)
  • Brigatinib binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. (blogspot.com)
  • It has affinity for viral thymidine kinase and, once phosphorylated, causes DNA chain termination when acted on by DNA polymerase. (medscape.com)
  • The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. (drugs.com)
  • Transcriptional repressor of MYC and thymidine kinase promoters. (nih.gov)
  • Additionally E47 represses PU.1-dependent transactivation of the MCSFR promoter through antagonizing PU.1's ability to bind to DNA. (hindawi.com)
  • IL-6 induction paralleled increased DNA binding activity to the nuclear factor-kappa B (NF-kappa B)- and NF-IL-6-recognized sites in the IL-6 promoter. (cdc.gov)
  • Stimulation of DNA binding activity to the NF- kappa B and NF-IL-6 binding sites of the IL-6 promoter by asbestos or H2O2 were inhibited by tetramethylthiourea, a hydroxyl radical scavenger. (cdc.gov)
  • A mutation in the nuclear factor (NF)κB binding site of the IL-8 promoter suppressed promoter activity in KB/TP cells that overexpress TP. (elsevierpure.com)
  • Primary-structure analysis of the mouse Thymidine Adevice promoter revealed marked differences with its human homolog. (aspetjournals.org)
  • First, the mouse promoter lacks the highly polymorphic thymidine/adenine repeat occurring in the human promoter, which has been associated with some forms of hyperbilirubinemia. (aspetjournals.org)
  • Second, an L1 transposon element, which is absent in the human promoter, is found 480 bp upstream of the transcription start site in mouse. (aspetjournals.org)
  • Using the electromobility shift and DNase I footprinting experiments, we have identified a hepatocyte nuclear factor 1-binding site in the mouse UGT1A1 promoter that confers responsiveness to both factors HNF1α and HNF1β in HEK293 cells. (aspetjournals.org)
  • The cell line stably expresses CAGA12-Luc, a Smad3/Smad4-dependent reporter containing 12 copies of the CAGAC sites (AGAC motif underlined) from the PAI-1 promoter. (cancertools.org)
  • The 140-bp Tk-1 core promoter fragment binds to transcription factors in extracts from P1798 cells. (elsevierpure.com)
  • Control cell extracts contain factors that bind to and protect (from deoxyribonuclease I) a distal promoter element from -106 to -87 bp, relative to the translational start site. (elsevierpure.com)
  • Glucocorticoids inhibit the amount or activity of the transcription factor that binds to this initiator-like element within the Tk-1 promoter. (elsevierpure.com)
  • The methylation of these CpG sites, over-represented in CpG islands in the promoter regulatory regions of many genes, disrupts the binding of transcription factors and attracts methyl-binding proteins that are associated with gene silencing and chromatin compaction. (biomedcentral.com)
  • Binds to 5'-d(GCC)(n)-3' trinucleotide repeats in promoter regions and acts as a repressor of the FMR1 gene. (nih.gov)
  • The researchers validates MTHFD2 as an anti cancer target and presents optimized potent MTHFD2 inhibitors (MTHFD2i) that can suppress acute myeloid leukemia by slowing down replication speed and inducing thymidine depletion, leading to apoptosis. (scilifelab.se)
  • Mechanistically, MTHFD2 inhibitors prevented thymidine production leading to misincorporation of uracil into DNA and replication stress. (lih.lu)
  • For example, in pyrimidine nucleoside phosphorylase (PYNP, ) there is an added three-stranded anti-parallel beta sheet as compared to other members of the family, such as E. coli thymidine phosphorylase (TP, ) ( PUBMED:9817849 ). (embl-heidelberg.de)
  • Three-dimensional structure of thymidine phosphorylase from Escherichiacoli at 2.8 A resolution. (embl-heidelberg.de)
  • The three-dimensional structure of thymidine phosphorylase fromEscherichia coli has been determined at 2.8 A resolution usingmultiple-isomorphous-replacement techniques. (embl-heidelberg.de)
  • Thymidine phosphorylase (TP) promotes angiogenesis and metastasis, and confers resistance to anticancer agents in some cancer cell types. (elsevierpure.com)
  • Fig. 1: DarT is a PARP-like protein that catalyses ADP-ribosylation of DNA at the thymidine base nitrogen. (nature.com)
  • Binds to protein and other compounds containing SH group. (medscape.com)
  • The platinum complex also can bind to nucleus and cytoplasmic protein. (medscape.com)
  • These phosphorylations stimulate the binding of the protein phosphatase PP2A-B56 to BRCA2 through a conserved binding motif. (nature.com)
  • We previously identified a putative binding motif for the serine/threonine protein phosphatase PP2A-B56 in BRCA2, which is of unknown significance 20 . (nature.com)
  • The E2A protein E47, but not EBF, was observed to bind to PU.1 and block PU.1's association with DNA. (hindawi.com)
  • protein cocrystal structures demonstrated binding to the active site of MTHFD2 and target engagement. (lih.lu)
  • Upon rinsing with the brilacidin oral rinse, brilacidin imitates defensin as a human host defense protein (HDP), and binds to and disrupts the bacterial cell membrane. (blogspot.com)
  • During spring 1999, Beijing/262/95-like variants, containing a The HA1 subunit of the H1N1 hemagglutinin protein consists characteristic deletion mutation at amino acid 134 of the HA of the globular head and contains five major antibody binding gene, were isolated from 13 persons at a DOD-GEIS influenza sites: Sa, Sb, Ca1, Ca2, and Cb (2-5). (cdc.gov)
  • RNA polymerase II is responsible for transcribing protein-coding genes, producing messenger RNAs (mRNAs) that carry the genetic information to the site of protein synthesis . (microbiologynote.com)
  • To understand how mammalian cells sense the presence and regulate the repair of these lesions, we employed a quantitative proteomic method to discover regioisomeric O2- and O4-n-butylthymidine (O2- and O4-nBudT)-binding proteins. (nih.gov)
  • Among these proteins, DDB1 and DDB2 selectively bind to O2-nBudT-containing DNA, whereas three high-mobility group (HMG) proteins (i.e. (nih.gov)
  • The NF-kappa B and NF-IL-6 DNA binding proteins were immunochemically characterized as a heterodimer p65/p50 and a homodimer C/EBP beta, respectively. (cdc.gov)
  • These K65R-mediated effects on RT structure and function help us to visualize the complex interaction with other key nucleotide RT drug resistance mutations, such as M184V, L74V, and thymidine analog resistance mutations. (rcsb.org)
  • Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. (nih.gov)
  • It inhibits viral replication at pyrophosphate-binding sites on virus-specific DNA polymerases. (medscape.com)
  • Binding of c-Abl to p53 inhibits the Mdm2-mediated degradation of p53 (Sionov et al. (nih.gov)
  • Similar to GATA1, Pax5 binds to PU.1 and inhibits its ability to activate transcription [ 20 ]. (hindawi.com)
  • MMAE binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. (blogspot.com)
  • Initiation marks the beginning of transcription, where RNA polymerase, the enzyme responsible for transcription, recognizes specific DNA sequences known as promoters and binds to them. (microbiologynote.com)
  • Autoradiography with [ 3 H]nicotine revealed no detectable abnormalities of high-affinity nicotine binding sites, but there was an absence of high-affinity [ 125 I]α-BGT sites. (jneurosci.org)
  • In the vertebrate brain, two categories of nicotinic receptors are distinguishable based on high-affinity binding of the agonist nicotine or high-affinity binding of the antagonist α-bungarotoxin (α-BGT). (jneurosci.org)
  • Because α7 is the only subunit of these three that is widely expressed in mammalian brain, it has been suspected that α7 contributes to the high-affinity α-BGT binding site, the structure and functional significance of which have been a long-standing source of controversy ( Sargent, 1993 ). (jneurosci.org)
  • From a pool of random DNA sequences, a library of 10 hairpin DNAs was selected, based on their strong binding affinity for bleomycin A5. (sciencedaily.com)
  • Their ability to selectively and with high affinity bind a given molecular structure is an essential key feature also for in vitro and in vivo diagnostics, for basic research and for many biotechnological applications. (wiley.com)
  • High affinity and binding specificity are however not the only requirements. (wiley.com)
  • FIG. 2 is a graph depicting the inhibition of .sup.125 I-IL-8 binding to neutrophils by unlabeled IL-8. (justia.com)
  • FIG. 4 is a graph depicting the inhibition of binding of .sup.125 I-IL-8 to human neutrophils by chimeric 5.12.14 Fab with an average IC.sub.50 of 1.6 nM. (justia.com)
  • 1998) . Ku can also bind to hairpin-ended DNA without activating DNA-PK (Smider et al. (nih.gov)
  • It is thought that TPundergoes a major conformational change upon substrate binding thatconsequently produces an active conformation. (embl-heidelberg.de)
  • RESULTS: The crystalstructure of PYNP from B. stearothermophilus with the substrate analogpseudouridine in its active site has been solved to 2.1 A resolution. (embl-heidelberg.de)
  • Active-site residues areconfirmed and a possible mechanism for substrate binding and subsequentdomain movement is suggested. (embl-heidelberg.de)
  • Role of glutamine 151 of human immunodeficiency virus type-1 reverse transcriptase in substrate selection as assessed by site-directed mutagenesis. (neb.com)
  • Glutamine 151 participates in the substrate dNTP binding function of HIV-1 reverse transcriptase. (neb.com)
  • The folate metabolism enzyme (MTHFD2) has recently gained a lot of attention due to its overexpression in a large variety of cancers combined with its role in thymidine synthesis, and is considered an emerging anticancer target. (scilifelab.se)
  • By binding to the active MTHFD2 site, the MTHFD2i was capable of reducing the replication speed and induce replication stress by preventing thymidine production, leading to mis-incorporation of uracil into DNA and replication stress. (scilifelab.se)
  • SN-38 binds to and stabilizes the topoisomerase I-DNA complex and prevents the relegation of DNA after it has been cleaved by topoisomerase I, inhibiting DNA replication. (medscape.com)
  • We show that overexpression of KDM4A-C, but not KDM4D, disrupts MSH6 foci formation during S phase by demethylating its binding site, H3K36me3. (biologists.com)
  • In addition to a constitutively occupied E2F1-Sp1 site immediately upstream of the cyclin E transcription start region, there is downstream a cell cycle-regulated site (termed CERM) that may function as a cyclin E-repressor module. (nih.gov)
  • Roy is particularly interested in the subtle biochemistry of bleomycin, including the specificity of its binding regions along the DNA strand and the drug's detailed mechanisms of DNA cleavage. (sciencedaily.com)
  • The thymidine synthesis pathways are often upregulated in cancer and have, since the 1940s, been targeted therapeutically to induce thymineless cell death. (scilifelab.se)
  • Cisplatin is a platinum-containing compound that exerts an antineoplastic effect by covalently binding to DNA, with preferential binding to N-7 position of guanine and adenosine. (medscape.com)
  • We further demonstrated that TFAM binds directly and selectively with O4-alkyldT-harboring DNA, and the binding capacity depends mainly on the HMG box-A domain of TFAM. (nih.gov)
  • The results indicated that glycyrrhizin exhibited a greater binding energy score for HSV-1 polymerase (− 22.45 kcal/mol) and VSV nucleocapsid (− 19.77 kcal/mol) in comparison to the cocrystallized ligand (− 13.31 and − 11.44 kcal/mol, respectively). (biomedcentral.com)
  • Once bound, RNA polymerase begins to unwind the DNA double helix and initiate the synthesis of a complementary RNA strand. (microbiologynote.com)
  • FIG. 3 demonstrates a negative isotype matched Fab does not inhibit the binding of .sup.125 I-IL-8 to human neutrophils. (justia.com)
  • The active-site cleft, where thepyrimidine and phosphate substrates bind, is between the two domains. (embl-heidelberg.de)
  • Furthermore, the guanidinium planes of K65R and Arg(72) were stacked in two different rotameric conformations in TFV-DP- and dATP-bound structures that may help explain how K65R RT discriminates the drug from substrates. (rcsb.org)
  • This is a Smad3/Smad4-dependent reporter, although it also binds complexes of Smad2 exon 3 with Smad4. (cancertools.org)
  • To this end, Scott Blanchard (Cornell University New York, USA) presented a study by single-molecule techniques that revealed a dynamic exchange between three metastable configurations of tRNA bound to E. coli ribosome, one of which is a previously unidentified hybrid state in which only deacylated tRNA adopts its hybrid (P/E) configuration. (biomedcentral.com)
  • Functional analysis of amino acid residues constituting the dNTP binding pocket of HIV-1 reverse transcriptase. (neb.com)
  • We have investigated histidine residues near the active site of the mitogenic Pasteurella multocida toxin. (openbiochemistryjournal.com)
  • In this report we hypothesized that factors required for early B cell commitment would bind to PU.1 and antagonize its ability to induce myeloid differentiation. (hindawi.com)
  • One aspect of the invention is an anti-IL-8 monoclonal antibody having the following characteristics: ability to bind human IL-8 with a K.sub.d between about 1.times.10.sup. (justia.com)
  • wherein the monoclonal antibody does not bind to C5a, .beta. (justia.com)
  • Monoclonal antibodies, which competitively bind to extracellular receptors or their natural ligands, and targeted drugs, which target a component of the intracellular signal transduction pathway, are available for several cancers. (basicmedicalkey.com)
  • B7 The SH3 domain of c-Abl binds to the C-terminal region of DNA-PK (amino acids 3414-3850) and may compete with Ku for binding to the same region (Jin et al. (nih.gov)
  • Previous research has shown that bleomycin can cause death in aberrant cells by migrating to the cell nucleus, binding with DNA and subsequently causing breaks in the DNA sequence. (sciencedaily.com)
  • HMGB1, HMGB2, and mitochondrial transcription factor A (TFAM)) exhibit preferential binding to O4-nBudT-bearing DNA. (nih.gov)
  • While the basic process of transcription is similar in prokaryotes and eukaryotes, there are notable differences due to the presence of a membrane-bound nucleus and organelles in eukaryotic cells . (microbiologynote.com)
  • 1993) and has helicase activity, but ssb-bound Ku does not activate DNA-PK (Smider et al. (nih.gov)
  • Further, the strength of this binding is closely associated with the degree of double-strand DNA cleavage. (sciencedaily.com)
  • Each of the 10 DNA samples underwent double-strand cleavage at more than one site. (sciencedaily.com)
  • Further, all of the observed cleavage sites were found within or in close proximity to an 8 base pair variable region, which had been randomized to create the original library. (sciencedaily.com)
  • Examination of the 10 DNA samples exposed to bleomycin revealed a total of 31 double-strand cleavage sites. (sciencedaily.com)
  • Two types of bleomycin binding and cleavage activity are detailed in the paper. (sciencedaily.com)
  • It frequently causes a mutation by interrupting the continuity of the bacterial OPERON at the site of insertion. (lookformedical.com)
  • An N-terminal PALB2 interaction domain recruits BRCA2 to sites of DNA damage as part of the BRCA1-PALB2-BRCA2 complex 12 . (nature.com)
  • Identification of the domain essential for polymerization and Arg-682 as the site of reactivity. (neb.com)
  • Thiamin pyrophosphokinase, thiamin-binding domain [Interproscan]. (ntu.edu.sg)
  • In our current study we examined whether E2A and/or EBF bind to PU.1 and antagonize its activity. (hindawi.com)
  • 19. Structural analyses of human thymidylate synthase reveal a site that may control conformational switching between active and inactive states. (nih.gov)
  • Mitochondrial Transcription Factor A Binds to and Promotes Mutagenic Transcriptional Bypass of O4-Alkylthymidine Lesions. (nih.gov)
  • Collectively, analyses of unique polyploidy markers and molecular signaling networks may be useful to further characterize functional aspects of decidual cell polyploidy at the site of implantation. (plos.org)
  • Fig. 2: DNA binding is highly coordinated by DarT for site-specific ADP-ribosylation of DNA. (nature.com)
  • Previous research has revealed that bleomycin binds with highly specific regions of the DNA strand, typically G-C sites, where a guanosine base pairs with a cytidine. (sciencedaily.com)
  • Comparison of data generated from the pooled DNA samples with results averaged across the individual samples comprising each pool revealed highly significant correlations for individual CpG sites across all nine regions, with an average overall correlation across all regions and pools of 0.95 (95% bootstrapped confidence intervals: 0.94 to 0.96). (biomedcentral.com)
  • We provide a set of high-resolution structures of this enzyme in ligand-free and pre- and post-reaction states, which reveals a specialized mechanism of catalysis that includes a key active-site arginine that extends the canonical ADP-ribosyltransferase toolkit. (nature.com)
  • Site-directed mutagenesis of arginine 72 of HIV-1 reverse transcriptase. (neb.com)
  • A comparative structure and sequence analysis suggests the existence of a universal stand-by site on the ribosome at the 30S platform dedicated for binding regulatory 5' mRNA elements. (biomedcentral.com)
  • Although less active than fibroblast growth factor, human rIL-6 also stimulated lung fibroblast growth, as evidenced by increased [3H]thymidine incorporation. (cdc.gov)
  • Models having this conformation were fitted, first manually and then by energy refinement, to the effector site of an atomic model of human deoxyhaemoglobin in which the side-chains in the NA, EF and H segments had been replaced by those of carp. (nih.gov)
  • 11. Probing the folate-binding site of human thymidylate synthase by site-directed mutagenesis. (nih.gov)
  • Find support for a specific problem in the support section of our website. (mdpi.com)