cGAMP-activated cGAS–STING signaling: its bacterial origins and evolutionary adaptation by metazoans

DJ Patel, Y Yu, W Xie - Nature Structural & Molecular Biology, 2023 - nature.com
The metazoan cGAMP-activated cGAS–STING innate immunity pathway is triggered in
response to genomic instability and DNA damage, thereby providing host defense against …

AlphaFill: enriching AlphaFold models with ligands and cofactors

ML Hekkelman, I de Vries, RP Joosten, A Perrakis - Nature Methods, 2023 - nature.com
Artificial intelligence-based protein structure prediction approaches have had a
transformative effect on biomolecular sciences. The predicted protein models in the …

Discovery of VH domains that allosterically inhibit ENPP1

PE Solomon, CJ Bracken, JA Carozza, H Wang… - Nature chemical …, 2024 - nature.com
Abstract Ectodomain phosphatase/phosphodiesterase-1 (ENPP1) is overexpressed on
cancer cells and functions as an innate immune checkpoint by hydrolyzing extracellular …

Targeting ENPP1 for cancer immunotherapy: Killing two birds with one stone

R Huang, Q Ning, J Zhao, X Zhao, L Zeng, Y Yi… - Biochemical …, 2024 - Elsevier
Cancer immunotherapy, particularly with immune checkpoint inhibitors, has revolutionized
the paradigm of cancer treatment. Nevertheless, the efficacy of cancer immunotherapy …

Discovery of Orally Bioavailable Phthalazinone Analogues as an ENPP1 Inhibitor for STING-Mediated Cancer Immunotherapy

Y Cho, M Kang, SH Ji, HJ Jeong, JE Jung… - Journal of Medicinal …, 2023 - ACS Publications
A lack of the T cell-inflamed tumor microenvironment limits the efficacy of immune
checkpoint inhibitors (ICIs). Activation of stimulator of interferon genes (STING)-mediated …

Naturally occurring quercetin and myricetin as potent inhibitors for human ectonucleotide pyrophosphatase/phosphodiesterase 1

P Duangiad, B Nutho, T Chaijarasphong, NP Morales… - Scientific reports, 2024 - nature.com
Abstract Ecto-nucleotide pyrophosphatases/phosphodiesterases 1 (ENPP1) is a key
enzyme in purinergic signaling pathways responsible for cell-to-cell communications and …

Development of novel ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitors for tumor immunotherapy

X Wang, X Lu, D Yan, Y Zhou, X Tan - International Journal of Molecular …, 2022 - mdpi.com
The cyclic guanosine monophosphate–adenosine monophosphate synthase–stimulator of
interferon genes–TANK-binding kinase 1–interferon regulating factor 3 (cGAS-STING-TBK1 …

Design and synthesis of new adamantyl derivatives as promising antiproliferative agents

AI Shahin, SO Zaraei, BO AlKubaisi, S Ullah… - European Journal of …, 2023 - Elsevier
A series of adamantyl carboxamide derivatives containing sulfonate or sulfonamide moiety
were designed as multitargeted inhibitors of ectonucleotide pyrophosphatases …

[HTML][HTML] A humanized monoclonal antibody targeting an ectonucleotidase rescues cardiac metabolism and heart function after myocardial infarction

S Li, B Tao, J Wan, E Montecino-Rodriguez… - Cell Reports …, 2024 - cell.com
Myocardial infarction (MI) results in aberrant cardiac metabolism, but no therapeutics have
been designed to target cardiac metabolism to enhance heart repair. We engineer a …

Studies on the Inhibition of Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) by 2-(3, 4-Dihydroxyphenyl)-7, 8-dihydroxy-3-methoxychromen-4-one, a …

A Rauf, Z Akram, M Naveed, N AlMasoud, TS Alomar… - Chemistry, 2023 - mdpi.com
Ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) regulates skeletal and soft
tissue mineralization by hydrolyzing nucleotide triphosphates and cyclic nucleotides, and is …