Träfflista för sökning "AMNE:(MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences) ;lar1:(su);pers:(Scobie Martin)"

Search: AMNE:(MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences) > Stockholm University > Scobie Martin

Result 1-2 of 2

Sort/group result

Sort by: Hits per page:

Enumeration	Reference	Cover	Find
1.	Llona-Minguez, Sabin, et al. (author) Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1 2016 In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 59:3, s. 1140-1148 Journal article (peer-reviewed)abstract 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.
2.	Llona-Minguez, Sabin, et al. (author) Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1 2017 In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 60:5, s. 2148-2154 Journal article (peer-reviewed)abstract The dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression. Here we report on the discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. Compounds 16 and 18 display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit -to-lead development.

Skapa referenser, mejla, bekava och länka

Permalink

Result 1-2 of 2

Refine your search

Type of publication: journal article (2)

Type of content: peer-reviewed (2)

Author/Editor: Helleday, Thomas (2); Loseva, Olga (2); Artursson, Per (2); Jenmalm Jensen, Anni ... (2); Lundbäck, Thomas (2); Baranczewski, Pawel (2); show more...; Scobie, Martin (2); Höglund, Andreas (2); Wiita, Elisee (2); Jemth, Ann-Sofie (2); Llona-Minguez, Sabin (2); Warpman Berglund, Ul ... (2); Calderon-Montano, Jo ... (2); Almlöf, Ingrid (2); Svensson, Richard (1); Mateus, André (1); Jeppsson, Fredrik (1); Stenmark, Pål (1); Martens, Ulf (1); Häggblad, Maria (1); Lundgren, Bo (1); Sigmundsson, Kristmu ... (1); Homan, Evert (1); Burgos-Moron, Estefa ... (1); Meijer, Laurent (1); Valerie, Nicholas C. ... (1); Claesson, Magnus (1); Visnes, Torkild (1); Johanson, Lars (1); Jacques, Sylvain A. (1); Piedrafita, Javier (1); Maga, Giovanni (1); Crespan, Emmanuele (1); Hagbjörk, Ann-Louise (1); Cazares-Körner, Cind ... (1); show less...

University: Uppsala University (2); Stockholm University (2)Undo refine; Karolinska Institutet (2)

Language: English (2)

Research subject (UKÄ/SCB): Medical and Health Sciences (2); Natural sciences (1)

Year

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

LIBRIS.kb.se

Copy and save the link in order to return to this view