Ethan Swartz
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View article: Adherence to Recent Evidence-Based Guidelines for Statin Therapy in Primary Prevention for Type 2 Diabetes Patients
Adherence to Recent Evidence-Based Guidelines for Statin Therapy in Primary Prevention for Type 2 Diabetes Patients Open
Guideline adherence alone is insufficient; therapy optimization and follow-up are critical for achieving LDL-C targets.
View article: Structure–Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation
Structure–Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation Open
Recently, we have shown that harmine induces β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. We explore structure–activity relationships of the 7-position of harmine for both DYRK1A kinase inhibition a…
View article: GLP-1 receptor agonists synergize with DYRK1A inhibitors to potentiate functional human β cell regeneration
GLP-1 receptor agonists synergize with DYRK1A inhibitors to potentiate functional human β cell regeneration Open
GLP-1 receptor agonists, widely used to treat diabetes, are converted to human β cell regenerative drugs by adding a DYRK1A inhibitor.
View article: Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor Open
Recently, our group identified that harmine is able to induce β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. Since, harmine suffers from a lack of selectivity, both against other kinases and CNS off-t…
View article: Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors
Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors Open
Small molecule inhibitors of dual specificity, tyrosine phosphorylation-regulated kinase 1A (DYRK1A), including harmine and others, are able to drive human β cell regeneration. While DYRK1A is certainly a target of this class, whether it i…
View article: Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation
Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation Open
DYRK1A has been implicated as an important drug target in various therapeutic areas, including neurological disorders and oncology. DYRK1A has more recently been shown to be involved in pathways regulating human β-cell proliferation, thus …