Nitrosonisoldipine is a selective inhibitor of inflammatory caspases and protects against pyroptosis and related septic shock
Sign Up to like & getrecommendations! Published in 2021 at "European Journal of Immunology"
DOI: 10.1002/eji.202048937
Abstract: Pyroptosis is a type of acute cell death that mainly occurs in immune cells. It is characterized with robust release of inflammatory cytokines and has emerged to play a critical role in the pathogenesis of… read more here.
Keywords: pyroptosis; selective inhibitor; inflammatory caspases; inhibitor inflammatory ... See more keywords
Discovery of rubiarbonone C as a selective inhibitor of cytochrome P450 4F enzymes
Sign Up to like & getrecommendations! Published in 2018 at "Archives of Toxicology"
DOI: 10.1007/s00204-018-2315-8
Abstract: Cytochrome P450 (CYP) enzymes, particularly CYP4A/4F, are the major ω-hydroxylases of arachidonic acid (AA) that can produce 20-hydroxyeicosatetraenoic acid (20-HETE). Although there are dissimilarities in substrate specificity, tissue distribution, and gene regulation between CYP4A and… read more here.
Keywords: cytochrome p450; selective inhibitor; inhibitor; rubiarbonone selective ... See more keywords
Selinexor, selective inhibitor of nuclear export: Unselective bullet for blood cancers.
Sign Up to like & getrecommendations! Published in 2020 at "Blood reviews"
DOI: 10.1016/j.blre.2020.100758
Abstract: Exportin 1 (XPO1), also known as chromosome maintenance 1 protein (CRM1), is the main transporter for hundreds of proteins like tumor suppressors, growth regulatory factors, oncoprotein mRNAs and others. Its upregulation leads to the inactivation… read more here.
Keywords: export; selective inhibitor; nuclear export; selinexor selective ... See more keywords
CARDIOPROTECTIVE AND ANTI INFLAMMATORY EFFECTS OF A SELECTIVE INHIBITOR OF THE SODIUM GLUCOSE COTRANSPORTER 2 (EMPAGLIFOZIN) IN DOXORUBICIN INDUCED CARDIOTOXICITY
Sign Up to like & getrecommendations! Published in 2019 at "Journal of the American College of Cardiology"
DOI: 10.1016/s0735-1097(19)31266-5
Abstract: Empagliflozin (EMPA), a selective inhibitor of the sodium glucose co-transporter 2 (SGLT2), reduced the risk of hospitalization for heart failure or cardiovascular death in type 2 diabetic patients. The mechanism by which EMPA induces cardiovascular… read more here.
Keywords: inhibitor sodium; selective inhibitor; cardioprotective anti; sodium glucose ... See more keywords
Selective Inhibitor Design for Kinase Homologs Using Multiobjective Monte Carlo Tree Search
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.2c00787
Abstract: Designing highly selective molecules for a drug target protein is a challenging task in drug discovery. This task can be regarded as a multiobjective problem that simultaneously satisfies criteria for various objectives, such as selectivity… read more here.
Keywords: structure; selective inhibitors; structure generator; target protein ... See more keywords
Development of a Selective Inhibitor of Protein Arginine Deiminase 2.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00274
Abstract: Protein arginine deiminase 2 (PAD2) plays a key role in the onset and progression of multiple sclerosis, rheumatoid arthritis, and breast cancer. To date, no PAD2-selective inhibitor has been developed. Such a compound will be… read more here.
Keywords: protein arginine; selective inhibitor; arginine deiminase;
Dissecting the Contribution of OATP1B1 to Hepatic Uptake of Statins Using the OATP1B1 Selective Inhibitor Estropipate.
Sign Up to like & getrecommendations! Published in 2019 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.8b01226
Abstract: Identification of a selective inhibitor of organic anion transporting polypeptide (OATP) 1B1 is critical in order to determine the contribution of OATP1B1-mediated uptake of investigational drugs into human hepatocytes for successful in vitro-to-in vivo extrapolation… read more here.
Keywords: hepatic uptake; selective inhibitor; contribution oatp1b1; oatp1b1 hepatic ... See more keywords
Identification of the first highly selective inhibitor of human lactate dehydrogenase B
Sign Up to like & getrecommendations! Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-00820-7
Abstract: Lactate dehydrogenase (LDH) catalyses the conversion of pyruvate to lactate and NADH to NAD+; it has two isoforms, LDHA and LDHB. LDHA is a promising target for cancer therapy, whereas LDHB is necessary for basal… read more here.
Keywords: cancer; selective inhibitor; lactate dehydrogenase;
Metabolic Disposition of Lurbinectedin, a Potent Selective Inhibitor of Active Transcription of Protein-Coding Genes, in Nonclinical Species and Patients
Sign Up to like & getrecommendations! Published in 2022 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.121.000668
Abstract: Lurbinectedin is a novel and potent selective inhibitor of active transcription of protein-coding genes, triggering apoptosis of cancerous cells. It has been approved for the treatment of patients with metastatic small-cell lung cancer with disease… read more here.
Keywords: inhibitor active; transcription protein; active transcription; selective inhibitor ... See more keywords
Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor
Sign Up to like & getrecommendations! Published in 2019 at "Science Advances"
DOI: 10.1126/sciadv.aav3660
Abstract: A next generation cancer drug candidate, a CDC7 inhibitor, TAK-931, was developed, which is being evaluated in clinical trials. Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments… read more here.
Keywords: potential target; selective inhibitor; inhibitor; tak 931 ... See more keywords
QStatin, a Selective Inhibitor of Quorum Sensing in Vibrio Species
Sign Up to like & getrecommendations! Published in 2018 at "mBio"
DOI: 10.1128/mbio.02262-17
Abstract: ABSTRACT Pathogenic Vibrio species cause diseases in diverse marine animals reared in aquaculture. Since their pathogenesis, persistence, and survival in marine environments are regulated by quorum sensing (QS), QS interference has attracted attention as a… read more here.
Keywords: selective inhibitor; vibrio; quorum sensing; vibrio species ... See more keywords