Characterising the Biochemical Mechanism of Action of PolQ Inhibitors

Programme : Back to Ms Holly Cooper

Poster

Characterising the Biochemical Mechanism of Action of PolQ Inhibitors

Authors

H Cooper¹; C McWhirter¹; L Edwardes¹; O Alkhatib¹; A Ferdinand²; W Krajewski²;
¹ Artios, UK; ² Cancer Research Horizons, UK

Discussion

Authors

H Cooper¹; C McWhirter¹; L Edwardes¹; O Alkhatib¹; A Ferdinand²; W Krajewski²;
¹ Artios, UK; ² Cancer Research Horizons, UK

Discussion

DNA polymerase Q (PolQ) is essential
for microhomology mediated end-joining (MMEJ) repair of double-strand breaks [1]
and has been proposed as an attractive target for the treatment of BRCA
deficient and other DNA repair pathway defective cancers. [2]

This poster describes the development of an automated
stopped kinetic assay using the Formulatrix Tempest Smart Batch function and its
subsequent use, along with biophysical and structural characterisation to
elucidate the biochemical mechanism of small molecule PolQ polymerase domain
inhibitors. [3]

[1] https://academic.oup.com/nar/article/31/21/6117/1042372

[2]https://www.nature.com/articles/s41580-021-00405-2

[3] https://www.nature.com/articles/s41467-021-23463-8