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  • Llona-Minguez, SabinKarolinska Institutet (author)

Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1

  • Article/chapterEnglish2016

Publisher, publication year, extent ...

  • 2016-01-27
  • American Chemical Society (ACS),2016
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:su-128185
  • https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-128185URI
  • https://doi.org/10.1021/acs.jmedchem.5b01741DOI
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-280245URI
  • http://kipublications.ki.se/Default.aspx?queryparsed=id:132958180URI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell sternness. Here we report on the development of the first potent and selective dCTPase inhibitors that enhance the cytotoxic effect of cytidine analogues in leukemia cells. Boronate 30 displays a promising in vitro ADME profile, including plasma and mouse microsomal half-lives, aqueous solubility, cell permeability and CYP inhibition, deeming it a suitable compound for in vivo studies.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Höglund, AndreasKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Sprint BioSci AB, Huddinge, Sweden. (author)
  • Jacques, Sylvain A.Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Univ Strasbourg, Fac Pharm, MEDALIS Drug Discovery Ctr, LFCS,CAMB,UMR7199,CNRS,LIT,UMR7200, F-67401 Illkirch Graffenstaden, France. (author)
  • Johanson, LarsKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Karolinska Inst, Dept Med Biochem & Biophys, Div Translat Med & Chem Biol, Chem Biol Consortium Sweden, Stockholm, Sweden. (author)
  • Calderon-Montano, Jose ManuelKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden. (author)
  • Claesson, MagnusStockholms universitet,Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Svante Arrhenius Vag 16C, SE-10691 Stockholm, Sweden.(Swepub:su)macl7147 (author)
  • Loseva, OlgaKarolinska Institutet (author)
  • Valerie, Nicholas C. K.Karolinska Institutet (author)
  • Lundbäck, ThomasKarolinska Institutet (author)
  • Piedrafita, JavierTorrey Pines Inst Mol Studies, 3550 Gen Atom Court, San Diego, CA 92121 USA. (author)
  • Maga, GiovanniCNR, IGM, Via Abbiategrasso 207, I-27100 Pavia, Italy. (author)
  • Crespan, EmmanueleCNR, IGM, Via Abbiategrasso 207, I-27100 Pavia, Italy. (author)
  • Meijer, LaurentManRos Therapeut, Perharidy Res Ctr, F-29680 Roscoff, Bretagne, France. (author)
  • Burgos Moron, EstefaniaKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden. (author)
  • Baranczewski, PawelUppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab,Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.(Swepub:uu)pawba132 (author)
  • Hagbjörk, Ann-LouiseUppsala universitet,Science for Life Laboratory, SciLifeLab,Institutionen för farmaci (author)
  • Svensson, RichardUppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab(Swepub:uu)ricsv977 (author)
  • Wiita, EliseeKarolinska Institutet (author)
  • Almlöf, IngridKarolinska Institutet (author)
  • Visnes, TorkildKarolinska Institutet (author)
  • Jeppsson, FredrikKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden. (author)
  • Sigmundsson, KristmundurKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Karolinska Inst, Dept Med Biochem & Biophys, Div Translat Med & Chem Biol, Chem Biol Consortium Sweden, Stockholm, Sweden.;Duke NUS Grad Med Sch, Singapore, Singapore. (author)
  • Jenmalm Jensen, AnnikaKarolinska Institutet (author)
  • Artursson, PerUppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab(Swepub:uu)perartur (author)
  • Jemth, Ann-SofieKarolinska Institutet (author)
  • Stenmark, PålStockholms universitet,Institutionen för biokemi och biofysik,Stockholm Univ, Dept Biochem & Biophys, Svante Arrhenius Vag 16C, SE-10691 Stockholm, Sweden.(Swepub:su)stenm (author)
  • Warpman Berglund, UlrikaKarolinska Institutet (author)
  • Scobie, MartinKarolinska Institutet (author)
  • Helleday, ThomasKarolinska Institutet (author)
  • Karolinska InstitutetKarolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Sprint BioSci AB, Huddinge, Sweden. (creator_code:org_t)

Related titles

  • In:Journal of Medicinal Chemistry: American Chemical Society (ACS)59:3, s. 1140-11480022-26231520-4804

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