Novel allosteric PARP1 inhibitors for the treatment of BRCA-deficient leukemia.
Hewlett E, Toma M, Sullivan-Reed K, Gordo J, Sliwinski T, Tulin A, Childers WE, Skorski T.
Hewlett E, et al. Among authors: tulin a.
Med Chem Res. 2020 Jun;29(6):962-978. doi: 10.1007/s00044-020-02537-0. Epub 2020 Apr 19.
Med Chem Res. 2020.
PMID: 33071527
Free PMC article.
Unfortunately, all marketed PARP1 inhibitors act by competing with the cofactor NAD(+) and resistance is already developing to this anti-cancer mechanism. Allosteric PARP1 inhibitors could provide a means of overcoming this resistance. A high throughput screen perfo …
Unfortunately, all marketed PARP1 inhibitors act by competing with the cofactor NAD(+) and resistance is already developing to this anti-can …