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Small Molecule Antagonists Of The Urokinase (Upa): Urokinase Receptor (Upar) Interaction With High Reported Potencies Show Only Weak Effects In Cell-Based Competition Assays Employing The Native Upar Ligand, Melissa De Souza, Hayden Matthews, Jodi A. Lee, Marie Ranson, Michael J. Kelso
Small Molecule Antagonists Of The Urokinase (Upa): Urokinase Receptor (Upar) Interaction With High Reported Potencies Show Only Weak Effects In Cell-Based Competition Assays Employing The Native Upar Ligand, Melissa De Souza, Hayden Matthews, Jodi A. Lee, Marie Ranson, Michael J. Kelso
Illawarra Health and Medical Research Institute
Binding of the urokinase-type plasminogen activator (uPA) to its cell-surface-bound receptor uPAR and upregulation of the plasminogen activation system (PAS) correlates with increased metastasis and poor prognosis in several tumour types. Disruptors of the uPA:uPAR interaction represent promising anti-tumour/metastasis agents and several approaches have been explored for this purpose, including the use of small molecule antagonists. Two highly potent non-peptidic antagonists 1 and 2 (IC50 1 = 0.8 nM, IC50 2 = 33 nM) from the patent literature were reportedly identified using competition assays employing radiolabelled uPAR-binding uPA fragments and appeared as useful pharmacological tools for studying the PAS. Before …
Muscarinic Receptor Antagonists, The Overactive Bladder And Efficacy Against Urinary Urgency, Kylie J. Mansfield
Muscarinic Receptor Antagonists, The Overactive Bladder And Efficacy Against Urinary Urgency, Kylie J. Mansfield
Graduate School of Medicine - Papers (Archive)
The overactive bladder (OAB) is a debilitating condition in which patients suffer from urinary urgency, frequency and nocturiawith or without urge urinary incontinence. The mainstay of pharmacotherapy for OAB is muscarinic receptor antagonists, which havebeen shown to be effective treatments for the symptoms of OAB. The mechanism underlying the efficacy of antimuscarinic agentsagainst the symptoms of OAB is not completely understood. This review explores the role of bladder mucosal muscarinic receptors in the signaling pathways that are activated in response to bladder filling. The cholinergic system is seen to be involved in bladder afferent signaling at many levels and as …