Search Results - "Sprague, Daniel J"
-
1
Mu-opioid receptor selective superagonists produce prolonged respiratory depression
Published in iScience (21-07-2023)“…Synthetic opioids are increasingly challenging to combat the opioid epidemic and act primarily at opioid receptors, chiefly the G protein-coupled receptor…”
Get full text
Journal Article -
2
Fluorinated triphenylphosphonium analogs improve cell selectivity and in vivo detection of mito-metformin
Published in iScience (22-12-2022)“…Triphenylphosphonium (TPP+) conjugated compounds selectively target cancer cells by exploiting their hyperpolarized mitochondrial membrane potential. To date,…”
Get full text
Journal Article -
3
Enantio- and periselective nitroalkene Diels-Alder reaction
Published in Organic & biomolecular chemistry (14-12-2012)“…The periselective Diels-Alder reaction of 5-substituted pentamethylcyclopentadienes and nitroethylene has been realized by helical-chiral hydrogen bond donor…”
Get more information
Journal Article -
4
Adaptation of a Small-Molecule Hydrogen-Bond Donor Catalyst to an Enantioselective Hetero-Diels–Alder Reaction Hypothesized for Brevianamide Biosynthesis
Published in Organic letters (20-02-2015)“…Chiral diamine-derived hydrogen-bond donors were evaluated for their ability to effect stereocontrol in an intramolecular hetero-Diels–Alder (HDA) reaction…”
Get full text
Journal Article -
5
-
6
Identification of a dihydropyridine scaffold that blocks ryanodine receptors
Published in iScience (21-01-2022)“…Ryanodine receptors (RyRs) are large, intracellular ion channels that control Ca2+ release from the sarco/endoplasmic reticulum. Dysregulation of RyRs in…”
Get full text
Journal Article -
7
Substituted Imidazoline Synthesis: A Diastereo- and Enantioselective aza-Henry Route to a Human Proteasome Modulator
Published in Organic letters (06-11-2020)“…The first enantio- and diastereoselective synthesis of Tepe’s human proteasome modulator is described. Routes to this and other highly substituted chiral…”
Get full text
Journal Article -
8
Diastereo- and enantioselective additions of α-nitro esters to imines for anti -α,β-diamino acid synthesis with α-alkyl-substitution
Published in Chemical science (Cambridge) (28-02-2018)“…The discovery that a -symmetric bis(AMidine) [BAM] catalyst promotes an -selective addition of α-substituted α-nitro esters to imines is described, providing…”
Get full text
Journal Article -
9
Natural variation in the binding pocket of a parasitic flatworm TRPM channel resolves the basis for praziquantel sensitivity
Published in Proceedings of the National Academy of Sciences - PNAS (03-01-2023)“…The drug praziquantel (PZQ) is the key clinical therapy for treating schistosomiasis and other infections caused by parasitic flatworms. A schistosome target…”
Get full text
Journal Article -
10
The anthelmintic meclonazepam activates a schistosome transient receptor potential channel
Published in The Journal of biological chemistry (01-01-2024)“…Parasitic flatworms cause various clinical and veterinary infections that impart a huge burden worldwide. The most clinically impactful infection is…”
Get full text
Journal Article -
11
Molecular and cellular basis of praziquantel action in the cardiovascular system
Published in American Journal of Physiology: Cell Physiology (01-02-2023)“…The anthelmintic drug praziquantel (PZQ) causes contraction of parasitic schistosomes as well as constriction of blood vessels within the mesenteric…”
Get more information
Journal Article -
12
Target-based discovery of a broad-spectrum flukicide
Published in Nature structural & molecular biology (01-09-2024)“…Diseases caused by parasitic flatworms impart a considerable healthcare burden worldwide. Many of these diseases—for example, the parasitic blood fluke…”
Get full text
Journal Article -
13
Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites
Published in ACS chemical biology (17-04-2020)“…BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All…”
Get full text
Journal Article -
14
The TRIM33 Bromodomain Recognizes Histone Lysine Lactylation
Published in ACS chemical biology (18-11-2024)“…Histone lysine lactylation (Kla) regulates inflammatory gene expression in activated macrophages and mediates the polarization of inflammatory (M1) to…”
Get full text
Journal Article -
15
Development of activity-based probes for the protein deacylase Sirt1
Published in Bioorganic chemistry (01-11-2020)“…[Display omitted] •Development of a Sirt1-selective activity-based probe (ABP).•Activity-based labeling measured Sirt1 activity in vitro and in HEK293T…”
Get full text
Journal Article -
16
Zinc‐Chelating BET Bromodomain Inhibitors Selectively Accumulate and Affect Gene Expression in Pancreatic β‐Cells
Published in The FASEB journal (01-05-2022)“…The islets of Langerhans are a heterogeneous mixture of endocrine (hormone‐secreting) cells in the mammalian pancreas. Of particular interest are the β‐cells…”
Get full text
Journal Article -
17
TRP drop, TRP drop: a steady patter of anti-schistosomal target illumination
Published in Frontiers in parasitology (13-02-2024)“…Infections caused by parasitic flatworms impart a significant disease burden. This is well exemplified by the neglected tropical disease schistosomiasis, which…”
Get full text
Journal Article -
18
The Anthelmintic Activity of Praziquantel Analogs Correlates with Structure-Activity Relationships at TRPM PZQ Orthologs
Published in ACS medicinal chemistry letters (09-11-2023)“…The anthelmintic drug praziquantel remains a key clinical therapy for treating various diseases caused by parasitic flatworms. The parasite target of…”
Get full text
Journal Article -
19
The Anthelmintic Activity of Praziquantel Analogs Correlates with Structure-Activity Relationships at TRPMPZQ Orthologs
Published in ACS medicinal chemistry letters (09-11-2023)“…The anthelmintic drug praziquantel remains a key clinical therapy for treating various diseases caused by parasitic flatworms. The parasite target of…”
Get full text
Journal Article -
20
Trisubstituted 1,3,5-Triazines: The First Ligands of the sY12-Binding Pocket on Chemokine CXCL12
Published in ACS medicinal chemistry letters (11-11-2021)“…CXCL12, a CXC-type chemokine, binds its receptor CXCR4, and the resulting signaling cascade is essential during development and subsequently in immune…”
Get full text
Journal Article