A Selective Adenylyl Cyclase 1 Inhibitor Relieves Pain Without Causing Tolerance [PDF]
Frontiers in Pharmacology, 2022 Among the ten different adenylyl cyclase isoforms, studies with knockout animals indicate that inhibition of AC1 can relieve pain and reduce behaviors linked to opioid dependence. We previously identified ST034307 as a selective inhibitor of AC1.
Gianna Giacoletti +12 more
doaj +4 more sources
Carbonic Anhydrase Inhibitor Modulation of Intraocular Pressure Is Independent of Soluble Adenylyl Cyclase [PDF]
Journal of Ocular Pharmacology and Therapeutics, 2023 Purpose: We investigated whether a clinically used carbonic anhydrase inhibitor (CAIs) can modulate intraocular pressure (IOP) through soluble adenylyl cyclase (sAC) signaling. Methods: IOP was measured 1 h after topical treatment with brinzolamide, a topically applied and clinically used CAIs, using direct cannulation of the anterior chamber in sAC ...
Shakarr V. Wiggins +5 more
openalex +3 more sources
Protein Associated with Myc (PAM) Is a Potent Inhibitor of Adenylyl Cyclases [PDF]
Journal of Biological Chemistry, 2001 Using the yeast two-hybrid assay and the second of the two large cytosolic domains of type V adenylyl cyclase (ACV) as bait, we identified a small region (amino acids 1028-1231) in the protein associated with Myc (PAM) as an interaction site for ACV.
Klaus Scholich +2 more
openalex +4 more sources
Selective Adenylyl Cyclase Type 1 Inhibitors as Potential Opioid Alternatives For Chronic Pain [PDF]
Neuropsychopharmacology, 2017 Selective Adenylyl Cyclase Type 1 Inhibitors as Potential Opioid Alternatives For Chronic ...
Val J. Watts
openalex +3 more sources
Adenine Nucleoside 3′-Tetraphosphates Are Novel and Potent Inhibitors of Adenylyl Cyclases [PDF]
Journal of Biological Chemistry, 1998 2'-Deoxyadenosine 3'-tetraphosphate (2'-deoxy-3'-A4P) and 2', 5'-dideoxyadenosine 3'-tetraphosphate (2',5'-dideoxy-3'-A4P) were synthesized, and their effects were tested on crude and purified forms of native adenylyl cyclases isolated from brain. Syntheses combined the method of alkoxide activation with the use of tribromoethyl phosphoromorpholino ...
Laurent Désaubry, Roger A. Johnson
openalex +4 more sources
Isoform selectivity of adenylyl cyclase inhibitors: characterization of known and novel compounds. [PDF]
J Pharmacol Exp Ther, 2013 Nine membrane-bound adenylyl cyclase (AC) isoforms catalyze the production of the second messenger cyclic AMP (cAMP) in response to various stimuli. Reduction of AC activity has well documented benefits, including benefits for heart disease and pain.
Brand CS +4 more
europepmc +5 more sources
A selective adenylyl cyclase 1 inhibitor relieves pain without causing tolerance [PDF]
Archives of Oral Biology, 2021 This study aimed to investigate the antinociceptive effects of the selective adenylyl cyclase type 1 (AC1) inhibitor ST034307 on tooth movement nociception through orofacial nociceptive behavior tests and molecular examination.We placed fixed nickel-titanium alloy closed-coil springs around the incisors of male Sprague-Dawley rats to induce tooth ...
Gianna Giacoletti +10 more
openalex +3 more sources
Structure-based development of novel adenylyl cyclase inhibitors. [PDF]
J Med Chem, 2008 In mammals, the second messenger cAMP is synthesized by a family of transmembrane isoforms (tmACs) and one known cytoplasmic enzyme, "soluble" adenylyl cyclase (sAC). Understanding the individual contributions of these families to cAMP signaling requires tools which can distinguish them.
Schlicker C +6 more
europepmc +4 more sources
Pro-nucleotide Inhibitors of Adenylyl Cyclases in Intact Cells [PDF]
Journal of Biological Chemistry, 2004 9-substituted adenine derivatives with protected phosphoryl groups were synthesized and tested as inhibitors of adenylyl cyclase in isolated enzyme and intact cell systems. Protected 3'-phosphoryl derivatives of 2',5'-dideoxyadenosine (2',5'-dd-Ado) and beta-l-2',5'-dd-Ado, protected 5'-phosphoryl derivatives of beta-l-2',3'-dd-Ado, and protected ...
Wolfgang H.G. Laux +6 more
openalex +4 more sources
The Soluble Adenylyl Cyclase Inhibitor LRE1 Prevents Hepatic Ischemia/Reperfusion Damage Through Improvement of Mitochondrial Function [PDF]
International Journal of Molecular Sciences, 2020 Hepatic ischemia/reperfusion (I/R) injury is a leading cause of organ dysfunction and failure in numerous pathological and surgical settings. At the core of this issue lies mitochondrial dysfunction. Hence, strategies that prime mitochondria towards damage resilience might prove applicable in a clinical setting.
João S. Teodoro +7 more
openalex +5 more sources