Publications by authors named "Kyle Z Rajkowski"
Article Synopsis
- Catecholamine-stimulated β-adrenergic receptor (βAR) signaling controls various physiological functions and impacts airway disease treatments, primarily through a well-known pathway involving G-adenylyl cyclase, cAMP, and PKA.
- Regulation of βAR signaling is influenced by GRKs and β-arrestins, which can lead to desensitization and alternative signaling that counteracts the primary pathway, presenting a challenge for maximizing βAR therapy effectiveness.
- A small molecule screen identified DFPQ, which selectively inhibits β-arrestin recruitment to βAR without disrupting its coupling to G proteins, offering a potential therapeutic advantage by preventing receptor desensitization and maintaining the efficacy of β
Following insights from recent crystal structures of the muscarinic acetylcholine receptor, binding modes of Positive Allosteric Modulators (PAMs) were predicted under the assumption that PAMs should bind to the extracellular surface of the active state. A series of well-characterized PAMs for adenosine (A R, A R, A R) and muscarinic acetylcholine (M R, M R) receptors were modeled using both rigid and flexible receptor CHARMM-based molecular docking. Studies of adenosine receptors investigated the molecular basis of the probe-dependence of PAM activity by modeling in complex with specific agonist radioligands.
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