Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation
The onset of inflammation is associated with reactive oxygen species and oxidative damage
to macromolecules like 7,8-dihydro-8-oxoguanine (8-oxoG) in DNA. Because 8-oxoguanine …
to macromolecules like 7,8-dihydro-8-oxoguanine (8-oxoG) in DNA. Because 8-oxoguanine …
Targeting SAMHD1 with the Vpx protein to improve cytarabine therapy for hematological malignancies
…, L Ljungblad, K Sanjiv, IH Myrberg, CBJ Paulin… - Nature medicine, 2017 - nature.com
The cytostatic deoxycytidine analog cytarabine (ara-C) is the most active agent available
against acute myelogenous leukemia (AML). Together with anthracyclines, ara-C forms the …
against acute myelogenous leukemia (AML). Together with anthracyclines, ara-C forms the …
[HTML][HTML] Nucleobase and nucleoside analogues: resistance and re-sensitisation at the level of pharmacokinetics, pharmacodynamics and metabolism
Antimetabolites, in particular nucleobase and nucleoside analogues, are cytotoxic drugs that,
starting from the small field of paediatric oncology, in combination with other …
starting from the small field of paediatric oncology, in combination with other …
[HTML][HTML] Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress
…, Y Andersson, ER Scaletti, C Bengtsson, CBJ Paulin… - Nature cancer, 2022 - nature.com
The folate metabolism enzyme MTHFD2 (methylenetetrahydrofolate dehydrogenase/cyclohydrolase)
is consistently overexpressed in cancer but its roles are not fully characterized, and …
is consistently overexpressed in cancer but its roles are not fully characterized, and …
SAMHD1 protects cancer cells from various nucleoside-based antimetabolites
Recently, we demonstrated that sterile α motif and HD domain containing protein 1 (SAMHD1)
is a major barrier in acute myelogenous leukemia (AML) cells to the cytotoxicity of …
is a major barrier in acute myelogenous leukemia (AML) cells to the cytotoxicity of …
Ribonucleotide reductase inhibitors suppress SAMHD 1 ara‐CTP ase activity enhancing cytarabine efficacy
…, N Tsesmetzis, K Sanjiv, CBJ Paulin… - EMBO molecular …, 2020 - embopress.org
The deoxycytidine analogue cytarabine (ara‐C) remains the backbone treatment of acute
myeloid leukaemia ( AML ) as well as other haematological and lymphoid malignancies, but …
myeloid leukaemia ( AML ) as well as other haematological and lymphoid malignancies, but …
[HTML][HTML] With me or against me: Tumor suppressor and drug resistance activities of SAMHD1
…, K Sanjiv, J Kutzner, IH Myrberg, CBJ Paulin… - Experimental …, 2017 - Elsevier
Highlights • Sterile alpha motif and histidine/aspartic acid domain-containing protein 1 is a
deoxyribonucleoside triphosphate (dNTP) triphosphohydrolase that is involved in cellular …
deoxyribonucleoside triphosphate (dNTP) triphosphohydrolase that is involved in cellular …
[HTML][HTML] dUTPase inhibition augments replication defects of 5-Fluorouracil
A Hagenkort, CBJ Paulin, M Desroses, A Sarno… - Oncotarget, 2017 - ncbi.nlm.nih.gov
The antimetabolite 5-Fluorouracil (5-FU) is used in the treatment of various forms of cancer
and has a complex mode of action. Despite 6 decades in clinical application the contribution …
and has a complex mode of action. Despite 6 decades in clinical application the contribution …
Computational and experimental druggability assessment of human DNA glycosylases
…, M Hedenström, E Wiita, K Vallin, CBJ Paulin… - ACS …, 2019 - ACS Publications
Due to a polar or even charged binding interface, DNA-binding proteins are considered
extraordinarily difficult targets for development of small-molecule ligands and only a handful of …
extraordinarily difficult targets for development of small-molecule ligands and only a handful of …
[PDF][PDF] Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel
SM Zhang, CBJ Paulin, H Shu, M Yagüe-Capilla… - Iscience, 2024 - cell.com
SAMHD1 is a dNTP triphosphohydrolase governing nucleotide pool homeostasis and can
detoxify chemotherapy metabolites controlling their clinical responses. To understand …
detoxify chemotherapy metabolites controlling their clinical responses. To understand …