MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool
Cancers have dysfunctional redox regulation resulting in reactive oxygen species production,
damaging both DNA and free dNTPs. The MTH1 protein sanitizes oxidized dNTP pools to …
damaging both DNA and free dNTPs. The MTH1 protein sanitizes oxidized dNTP pools to …
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 …
CETSA: a target engagement assay with potential to transform drug discovery
AJ Jensen, DM Molina, T Lundbäck - Future medicinal chemistry, 2015 - Future Science
Extensive efforts have been made to analyze and understand the disappointing trend of
decreasing annual drug approval, particularly when it comes to first-in-class drugs, and this …
decreasing annual drug approval, particularly when it comes to first-in-class drugs, and this …
Microwave heated flow synthesis of spiro-oxindole dihydroquinazolinone based IRAP inhibitors
…, T Lundback, A Jenmalm-Jensen… - … Process Research & …, 2014 - ACS Publications
A fast and convenient synthetic route towards spiro-oxindole dihydroquinazolinones as
novel and drug-like insulin-regulated aminopeptidase (IRAP) inhibitors is reported. The …
novel and drug-like insulin-regulated aminopeptidase (IRAP) inhibitors is reported. The …
Binding to and inhibition of insulin-regulated aminopeptidase by macrocyclic disulfides enhances spine density
…, J Sävmarker, T Lundbäck, A Jenmalm-Jensen… - Molecular …, 2016 - ASPET
Angiotensin IV (Ang IV) and related peptide analogs, as well as nonpeptide inhibitors of
insulin-regulated aminopeptidase (IRAP), have previously been shown to enhance memory and …
insulin-regulated aminopeptidase (IRAP), have previously been shown to enhance memory and …
Discovery of the first potent and selective inhibitors of human dCTP pyrophosphatase 1
S Llona-Minguez, A Hoglund, SA Jacques… - Journal of medicinal …, 2016 - ACS Publications
The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool
through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs)…
through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs)…
Membrane-depolarizing channel blockers induce selective glioma cell death by impairing nutrient transport and unfolded protein/amino acid responses
…, LGJ Hammarström, A Jenmalm Jensen… - Cancer research, 2017 - AACR
Glioma-initiating cells (GIC) are considered the underlying cause of recurrences of
aggressive glioblastomas, replenishing the tumor population and undermining the efficacy of …
aggressive glioblastomas, replenishing the tumor population and undermining the efficacy of …
Aryl sulfonamide inhibitors of insulin-regulated aminopeptidase enhance spine density in primary hippocampal neuron cultures
…, V Pham, T Lundback, A Jenmalm-Jensen… - ACS chemical …, 2016 - ACS Publications
The zinc metallopeptidase insulin regulated aminopeptidase (IRAP), which is highly expressed
in the hippocampus and other brain regions associated with cognitive function, has been …
in the hippocampus and other brain regions associated with cognitive function, has been …
Computational and experimental druggability assessment of human DNA glycosylases
…, M Scobie, A Schmidt, A Jenmalm-Jensen… - 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 …
Inhibition of Insulin‐Regulated Aminopeptidase (IRAP) by Arylsulfonamides
…, J Sävmarker, T Lundbäck, A Jenmalm-Jensen… - …, 2014 - Wiley Online Library
The inhibition of insulin‐regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV
is known to improve memory and learning in rats. Screening 10 500 low‐molecular‐weight …
is known to improve memory and learning in rats. Screening 10 500 low‐molecular‐weight …