Structure-guided inhibition of the cancer DNA-mutating enzyme APOBEC3A

S Harjes, HM Kurup, AE Rieffer, M Bayarjargal… - Nature …, 2023 - nature.com
The normally antiviral enzyme APOBEC3A is an endogenous mutagen in human cancer. Its
single-stranded DNA C-to-U editing activity results in multiple mutagenic outcomes including …

Seven-membered ring nucleobases as inhibitors of human cytidine deaminase and APOBEC3A

HM Kurup, MV Kvach, S Harjes, GB Jameson… - Organic & …, 2023 - pubs.rsc.org
The APOBEC3 (APOBEC3A-H) enzyme family as a part of the human innate immune system
deaminates cytosine to uracil in single-stranded DNA (ssDNA) and thereby prevents the …

Molecular mechanism for regulating APOBEC3G DNA editing function by the non-catalytic domain

H Yang, J Pacheco, K Kim, A Bokani, F Ito… - Nature …, 2024 - nature.com
APOBEC3G, part of the AID/APOBEC cytidine deaminase family, is crucial for antiviral
immunity. It has two zinc-coordinated cytidine-deaminase domains. The non-catalytic N …

Deciphering the role of Enterococcus faecium cytidine deaminase in gemcitabine resistance of gallbladder cancer

L Jiang, L Zhang, Y Shu, Y Zhang, L Gao, S Qiu… - Journal of Biological …, 2024 - ASBMB
Gemcitabine-based chemotherapy is a cornerstone of standard care for gallbladder cancer
(GBC) treatment. Still, drug resistance remains a significant challenge, influenced by factors …

Small-Angle X-ray Scattering (SAXS) Measurements of APOBEC3G Provide Structural Basis for Binding of Single-Stranded DNA and Processivity

FM Barzak, TM Ryan, N Mohammadzadeh, S Harjes… - Viruses, 2022 - mdpi.com
APOBEC3 enzymes are polynucleotide deaminases, converting cytosine to uracil on single-
stranded DNA (ssDNA) and RNA as part of the innate immune response against viruses and …

Efficient convergent synthesis of 1, 3-diazepinone nucleosides by ring-closing metathesis and direct glycosylation

AK Hedger, J Findell, DS Barak, CA Schiffer, JK Watts… - RSC …, 2024 - pubs.rsc.org
A new and highly efficient ring-closing metathesis-based strategy was developed for the
synthesis of the cyclic urea 1, 3-diazepinone, presenting significant improvement upon …

[HTML][HTML] Affinity Tag-Free Purification of SARS-CoV-2 N Protein and Its Crystal Structure in Complex with ssDNA

A Maiti, H Matsuo - Biomolecules, 2024 - pmc.ncbi.nlm.nih.gov
The nucleocapsid (N) protein is one of the four structural proteins in SARS-CoV-2, playing
key roles in viral assembly, immune evasion, and stability. One of its primary functions is to …

Next generation APOBEC3 inhibitors: Optimally designed for potency and nuclease stability

AK Hedger, W Myint, JM Lee… - …, 2024 - pmc.ncbi.nlm.nih.gov
APOBEC3 (or A3) enzymes have emerged as potential therapeutic targets due to their role
in introducing heterogeneity in viruses and cancer, often leading to drug resistance …

Synthesis of 1, 4-azaphosphinine nucleosides and evaluation as inhibitors of human cytidine deaminase and APOBEC3A

MV Kvach, S Harjes, HM Kurup… - Beilstein Journal of …, 2024 - beilstein-journals.org
Nucleoside and polynucleotide cytidine deaminases (CDAs), such as CDA and APOBEC3,
share a similar mechanism of cytosine to uracil conversion. In 1984, phosphapyrimidine …

Cross-linked DNA with carbazole pseudo-nucleoside enables potent inhibition of the cancer DNA-and RNA-mutating enzyme APOBEC3A

H Kurup, S Harjes, Y Su, T Hall, G Jameson, E Harjes… - 2023 - chemrxiv.org
The human antiviral enzyme APOBEC3A has mutagenic activity in many human cancers,
where it is used to fuel tumour evolution. Its single-stranded DNA and RNA C-to-U editing …