Kyle A. Emmitte
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View article: Developing inhibitors of the guanosine triphosphate hydrolysis accelerating activity of Regulator of G protein Signaling-14
Developing inhibitors of the guanosine triphosphate hydrolysis accelerating activity of Regulator of G protein Signaling-14 Open
View article: I-GAT: Interpretable Graph Attention Networks for Ligand Optimization
I-GAT: Interpretable Graph Attention Networks for Ligand Optimization Open
Designing selective and potent ligands for target receptors remains a significant challenge in drug discovery. Computational approaches, particularly advancements in machine learning (ML), offer transformative potential in addressing this …
View article: Developing inhibitors of the guanosine triphosphate hydrolysis accelerating activity of Regulator of G protein Signaling-14
Developing inhibitors of the guanosine triphosphate hydrolysis accelerating activity of Regulator of G protein Signaling-14 Open
Regulator of G protein Signaling-14 (RGS14), an intracellular inactivator of G protein-coupled receptor (GPCR) signaling, is considered an undruggable protein given its shallow and relatively featureless protein-protein interaction interfa…
View article: Efficient Regioselective Synthesis of Benzimidazoles and Azabenzimidazoles to Enable the Rapid Development of Structure–Activity Relationships for Activation of SLACK Potassium Channels
Efficient Regioselective Synthesis of Benzimidazoles and Azabenzimidazoles to Enable the Rapid Development of Structure–Activity Relationships for Activation of SLACK Potassium Channels Open
The sodium-activated potassium channel known as SLACK (KNa1.1 or Slo2.2) is widely expressed in the central nervous system and represents a potential target for the treatment of several neurological disorders. While much recent progress ha…
View article: Phenethylaminylation: Preliminary <i>In Vitro</i> Evidence for the Covalent Transamidation of Psychedelic Phenethylamines to Glial Proteins using 3,5-Dimethoxy-4-(2-Propynyloxy)-Phenethylamine as a Model Compound
Phenethylaminylation: Preliminary <i>In Vitro</i> Evidence for the Covalent Transamidation of Psychedelic Phenethylamines to Glial Proteins using 3,5-Dimethoxy-4-(2-Propynyloxy)-Phenethylamine as a Model Compound Open
Psychedelics are well known for their ability to produce profoundly altered states of consciousness. But, more importantly, the effects of psychedelics can influence neurobehavioral changes that last well after these acute subjective effec…
View article: Structure–Activity Relationship Studies in a Series of 2-Aryloxy-N-(pyrimidin-5-yl)acetamide Inhibitors of SLACK Potassium Channels
Structure–Activity Relationship Studies in a Series of 2-Aryloxy-N-(pyrimidin-5-yl)acetamide Inhibitors of SLACK Potassium Channels Open
Epilepsy of infancy with migrating focal seizures (EIMFS) is a rare, serious, and pharmacoresistant epileptic disorder often linked to gain-of-function mutations in the KCNT1 gene. KCNT1 encodes the sodium-activated potassium channel known…
View article: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons
Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons Open
More than 20 recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (K Na ) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which a…
View article: Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons
Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons Open
View article: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (KNa) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which…
View article: Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (KNa) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which…
View article: Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Author response: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (KNa) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which…
View article: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (KNa) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which…
View article: Structure–Activity Relationship Studies in a Series of Xanthine Inhibitors of SLACK Potassium Channels
Structure–Activity Relationship Studies in a Series of Xanthine Inhibitors of SLACK Potassium Channels Open
Gain-of-function mutations in the KCNT1 gene, which encodes the sodium-activated potassium channel known as SLACK, are associated with the rare but devastating developmental and epileptic encephalopathy known as epilepsy of infancy with mi…
View article: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons
Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on somatostatin- and parvalbumin-expressing cortical GABAergic neurons Open
More than 20 recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (K Na ) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which a…
View article: Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Heterozygous expression of a Kcnt1 gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (KNa) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of which…
View article: Heterozygous expression of a <i>Kcnt1</i> gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons
Heterozygous expression of a <i>Kcnt1</i> gain-of-function variant has differential effects on SST- and PV-expressing cortical GABAergic neurons Open
More than twenty recurrent missense gain-of-function (GOF) mutations have been identified in the sodium-activated potassium (K Na ) channel gene KCNT1 in patients with severe developmental and epileptic encephalopathies (DEEs), most of whi…
View article: Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685
Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685 Open
View article: Quercetin and Related Analogs as Therapeutics to Promote Tissue Repair
Quercetin and Related Analogs as Therapeutics to Promote Tissue Repair Open
Quercetin is a polyphenol of the flavonoid class of secondary metabolites that is widely distributed in the plant kingdom. Quercetin has been found to exhibit potent bioactivity in the areas of wound healing, neuroprotection, and anti-agin…
View article: Structure–Activity Relationship Study of the High-Affinity Neuropeptide Y <sub>4</sub> Receptor Positive Allosteric Modulator VU0506013
Structure–Activity Relationship Study of the High-Affinity Neuropeptide Y <sub>4</sub> Receptor Positive Allosteric Modulator VU0506013 Open
Positive allosteric modulators targeting the Y4 receptor (Y4R), a G protein-coupled receptor (GPCR) involved in the regulation of satiety, offer great potential in anti-obesity research. In this study, we selected 603…
View article: Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase Open
Purpose: Dysregulation of the insulin-like growth factor-I receptor (IGF-IR) signaling pathway has been implicated in the development of many types of tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcomas. Age…
View article: Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase Open
Purpose: Dysregulation of the insulin-like growth factor-I receptor (IGF-IR) signaling pathway has been implicated in the development of many types of tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcomas. Age…
View article: Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase Open
Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
View article: Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase Open
Supplementary Data from Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase
View article: Structure–activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels
Structure–activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels Open
View article: Small-Molecule Inhibitors of Slack Potassium Channels As Potential Therapeutics for Childhood Epilepsies
Small-Molecule Inhibitors of Slack Potassium Channels As Potential Therapeutics for Childhood Epilepsies Open
Slack channels are sodium-activated potassium channels that are encoded by the KCNT1 gene. Several KCNT1 gain of function mutations have been linked to malignant migrating partial seizures of infancy. Quinidine is an anti-arr…
View article: An Efficient Strategy for the Synthesis of α,α′-cis and trans-Disubstituted Medium Ring Ethers
An Efficient Strategy for the Synthesis of α,α′-cis and trans-Disubstituted Medium Ring Ethers Open
An asymmetric alkylation-ring-closing metathesis strat-egy was developed for the construction of a,a'-disubstituted medi-um ring ethers. The approach features an asymmetric alkylation of highly functionalized a-alkoxy acyl oxazolidinones f…
View article: Highly Selective Y<sub>4</sub> Receptor Antagonist Binds in an Allosteric Binding Pocket
Highly Selective Y<sub>4</sub> Receptor Antagonist Binds in an Allosteric Binding Pocket Open
Human neuropeptide Y receptors (Y1R, Y2R, Y4R, and Y5R) belong to the superfamily of G protein-coupled receptors and play an important role in the regulation of food intake and energy metabolism.…
View article: Total Synthesis of Brevetoxin A
Total Synthesis of Brevetoxin A Open
A total synthesis of brevetoxin A is reported. Two tetracyclic coupling partners, prepared from previously reported advanced fragments, were effectively united via a Horner—Wittig olefination. The resulting octacycle was progressed to subs…
View article: Enantioselective Total Synthesis of Brevetoxin A: Unified Strategy for the B, E, G, and J Subunits
Enantioselective Total Synthesis of Brevetoxin A: Unified Strategy for the B, E, G, and J Subunits Open
Brevetoxin A is a decacyclic ladder toxin that possesses five-,six-, seven-, eight-, and nine-membered oxacycles, as well as 22 tetrahedral stereocenters. Herein, we describe a unified approach to the B, E, G, and J rings predicated upon a…
View article: Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5
Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5 Open