Articles with "macrocyclic inhibitors" as a keyword



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Discovery of Macrocyclic Inhibitors of Apurinic/Apyrimidinic Endonuclease 1.

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Published in 2019 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.8b01529

Abstract: Apurinic/apyrimidinic endonuclease 1 (APE1) is an essential base excision repair enzyme that is upregulated in a number of cancers, contributes to resistance of tumors treated with DNA-alkylating or -oxidizing agents, and has recently been identified… read more here.

Keywords: endonuclease; inhibition ape1; apurinic apyrimidinic; macrocyclic inhibitors ... See more keywords
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Selective Macrocyclic Inhibitors of DYRK1A/B.

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Published in 2022 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.1c00630

Abstract: Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) is a therapeutic target of interest due to the roles it plays in both neurological diseases and cancer. We present the development of the first macrocyclic inhibitors of DYRK1A.… read more here.

Keywords: cell; inhibitors dyrk1a; chemistry; selective macrocyclic ... See more keywords