Abstract:
:MTH1 is a member of the nudix phosphohydrolase superfamily of enzymes, and it is involved in nucleotide pool homeostasis. The protein exerts its scavenging action by hydrolyzing oxidized nucleotides, thus avoiding their misincorporation into replicating DNA. Recent reports have validated its inhibition as a potential broad-spectrum target in oncology and have described small molecules able to engage this target with antiproliferative effect. In the accompanying paper (DOI: 10.1021/acs.jmedchem.5b01760 ), a team at AstraZeneca led by Jason G. Kettle elegantly demonstrated the complete lack of antiproliferative activity of cancer cells to highly potent MTH1 inhibitors.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Papeo Gdoi
10.1021/acs.jmedchem.6b00283subject
Has Abstractpub_date
2016-03-24 00:00:00pages
2343-5issue
6eissn
0022-2623issn
1520-4804journal_volume
59pub_type
评论,杂志文章abstract::Hydroxy-2-phenylindoles carrying substituted benzyl groups and similar substituents at the nitrogen were synthesized and tested for their ability to displace estradiol from its receptor. All of the derivatives tested exhibited high binding affinities for the calf uterine estrogen receptor, with RBA values ranging from...
journal_title:Journal of medicinal chemistry
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abstract::Analogues of angiotensin II and III (ANG II and ANG III) in which the tyrosine and/or phenylalanine residues were substituted have been synthesized by the solid-phase method and purified by (carboxymethyl)cellulose chromatography and reversed-phase HPLC. The antagonist and agonist potencies of these peptides were dete...
journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
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更新日期:2014-04-10 00:00:00
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journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
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更新日期:2009-12-10 00:00:00