Barbara Preti
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View article: Targeting Ion Channel TRPM4
Targeting Ion Channel TRPM4 Open
The transient receptor potential melastatin 4 (TRPM4) ion channel is ubiquitously expressed. Dysregulation and/or functional mutations of TRPM4 lead to several diseases. Within our studies, we screened for TRPM4 inhibitors and identified s…
View article: Discovery and Structure–Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists
Discovery and Structure–Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists Open
A series of benzyloxy and phenoxy derivatives of the adenosine receptor agonists N6-cyclopentyl adenosine (CPA) and N6-cyclopentyl 5'-N-ethylcarboxamidoadenosine (CP-NECA) were synthesized, and their potency and selectivity were assessed. …
View article: Species-Specific Effects of Cation Channel TRPM4 Small-Molecule Inhibitors
Species-Specific Effects of Cation Channel TRPM4 Small-Molecule Inhibitors Open
Background: The Transient Receptor Potential Melastatin member 4 ( TRPM4 ) gene encodes a calcium-activated non-selective cation channel expressed in several tissues. Mutations in TRPM4 have been reported in patients with different types o…
View article: Species-specific effects of cation channel TRPM4 small-molecule inhibitors
Species-specific effects of cation channel TRPM4 small-molecule inhibitors Open
Background The Transient Receptor Potential Melastatin member 4 ( TRPM4 ) gene encodes a calcium-activated non-selective cation channel expressed in several tissues. Mutations in TRPM4 have been reported in patients with different types of…
View article: Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor
Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor Open
Despite being among the most characterized G protein-coupled receptors (GPCRs), adenosine receptors (ARs) have always been a difficult target in drug design. To date, no agonist other than the natural effector and the diagnostic regadenoso…
View article: Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor
Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor Open
Despite being amongst the most characterized G protein-coupled receptors (GPCRs), adenosine receptors (ARs) have always been a difficult target in drug design. To date, no agonist other than the natural effector and the diagnostic regadeno…
View article: Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression
Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression Open
Summary The development of therapeutic agonists for G protein-coupled receptors (GPCRs) is hampered by the propensity of GPCRs to couple to multiple intracellular signalling pathways. This promiscuous coupling leads to numerous downstream …