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Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening.

Bioorganic & medicinal chemistry - 1 Jan 2020

Mamontova E M, Zakharenko A L, Zakharova O D, Dyrkheeva N S, Volcho K P, Reynisson J, Arabshahi H J, Salakhutdinov N F, Lavrik O I

Abstract excerpt

Spinocerebellar ataxia syndrome with axonal neuropathy (SCAN1) is a debilitating neurological disease that is caused by the mutation the Tyrosyl-DNA phosphodiesterase 1 (TDP1) DNA repair enzyme. The crucial His493 in TDP1's binding site is replaced with an arginine amino acid residue rendering the enzyme dysfunctional. A virtual screen was performed against the homology model of SCAN1 and seventeen compounds were...

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PMID: 31831297
DOI: 10.1016/j.bmc.2019.115234

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