{"entity": "publication", "iuid": "419774330de442a7b59aaa48bd3af0ae", "timestamp": "2026-08-11T07:46:51.945Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/419774330de442a7b59aaa48bd3af0ae.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/419774330de442a7b59aaa48bd3af0ae"}}, "title": "Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1.", "authors": [{"family": "Llona-Minguez", "given": "Sabin", "initials": "S"}, {"family": "H\u00f6glund", "given": "Andreas", "initials": "A"}, {"family": "Wiita", "given": "Elisee", "initials": "E"}, {"family": "Alml\u00f6f", "given": "Ingrid", "initials": "I"}, {"family": "Mateus", "given": "Andr\u00e9", "initials": "A"}, {"family": "Calder\u00f3n-Monta\u00f1o", "given": "Jos\u00e9 Manuel", "initials": "JM"}, {"family": "Cazares-K\u00f6rner", "given": "Cindy", "initials": "C"}, {"family": "Homan", "given": "Evert", "initials": "E"}, {"family": "Loseva", "given": "Olga", "initials": "O"}, {"family": "Baranczewski", "given": "Pawel", "initials": "P"}, {"family": "Jemth", "given": "Ann-Sofie", "initials": "AS"}, {"family": "H\u00e4ggblad", "given": "Maria", "initials": "M"}, {"family": "Martens", "given": "Ulf", "initials": "U"}, {"family": "Lundgren", "given": "Bo", "initials": "B"}, {"family": "Artursson", "given": "Per", "initials": "P"}, {"family": "Lundb\u00e4ck", "given": "Thomas", "initials": "T"}, {"family": "Jenmalm Jensen", "given": "Annika", "initials": "A"}, {"family": "Warpman Berglund", "given": "Ulrika", "initials": "U"}, {"family": "Scobie", "given": "Martin", "initials": "M"}, {"family": "Helleday", "given": "Thomas", "initials": "T"}], "type": "journal article", "published": "2017-03-09", "journal": {"title": "J. Med. Chem.", "issn": "0022-2623", "volume": "60", "issue": "5", "pages": "2148-2154", "issn-l": "0022-2623"}, "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.", "doi": "10.1021/acs.jmedchem.6b01786", "pmid": "28145708", "labels": {"Affiliated researcher": null}, "xrefs": [], "notes": [], "created": "2018-12-05T11:27:07.800Z", "modified": "2018-12-05T11:27:07.823Z"}