Results 211 to 220 of about 30,280 (221)
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Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)

ACS Medicinal Chemistry Letters, 2021
Soluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe successful efforts to design improved sAC inhibitors amenable for in vivo interrogation of sAC inhibition to assess its potential therapeutic applications. This work culminated in the identification
Makoto Fushimi   +19 more
openaire   +3 more sources

MANT-substituted guanine nucleotides: A novel class of potent adenylyl cyclase inhibitors

Life Sciences, 2003
Mammals express nine membranous adenylyl cyclase (AC) isoforms (AC1-AC9), but the precise functions of AC isoforms are still incompletely understood. This situation is at least partially due to the paucity of potent and isoenzyme-specific AC inhibitors.
Andreas, Gille, Roland, Seifert
openaire   +2 more sources

Chronic morphine-mediated adenylyl cyclase superactivation is attenuated by the Raf-1 inhibitor, GW5074

European Journal of Pharmacology, 2006
The utility of morphine for the treatment of chronic pain is limited by the development of analgesic tolerance. Adenylyl cyclase (AC) superactivation, induced by chronic opioid agonist administration, is regarded as one of the molecular mechanisms leading to tolerance.
Xu, Yue   +5 more
openaire   +2 more sources

Tissue levels, source, and regulation of 3'-AMP: an intracellular inhibitor of adenylyl cyclases.

Molecular Pharmacology, 1990
Tissue levels of 3'-AMP were measured in several rat tissues and the sensitivities of the respective adenylyl cyclases were compared with respect to "P" site-mediated inhibition by 3'-AMP2'-deoxy-3'AMP (2'd3'-AMP), and 2',5'-dideoxyadenosine. IC50 values for these P site inhibitors of adenylyl cyclases varied widely among tissues, e.g., with skeletal ...
M, Bushfield, I, Shoshani, R A, Johnson
openaire   +2 more sources

Synthetic heteroprostanoids of A- and E-types as novel non-comprehensive inhibitors of adenylyl cyclase in rat hepatocytes

Biochemical and Biophysical Research Communications, 2006
Treatment of rat hepatocyte plasma membranes with five novel synthetic heteroprostanoids of A- and E-types significantly decreased basal activity of adenylyl cyclase. Inhibition of forskolin-stimulated activity of the enzyme was seen as well. The maximal effective concentration for all substances tested was found at approximately 5x10(-6)-1x10(-5) M ...
A I, Hubich   +5 more
openaire   +2 more sources

Hydroxamate based inhibitors of adenylyl cyclase. Part 2: The effect of cyclic linkers on P-site binding

Bioorganic & Medicinal Chemistry Letters, 2002
AbstractFor Abstract see ChemInform Abstract in Full Text.
Daniel, Levy   +3 more
openaire   +2 more sources

Hydroxamate Based Inhibitors of Adenylyl Cyclase. Part 1. The Effect of Acyclic Linkers on P‐Site Binding.

ChemInform, 2002
AbstractFor Abstract see ChemInform Abstract in Full Text.
Daniel, Levy   +7 more
openaire   +2 more sources

Isoform Selectivity of Adenylyl Cyclase Inhibitors

The Journal of Pharmacology and Experimental Therapeutics, 2013
openaire   +1 more source

Faculty Opinions recommendation of Identification of an adenylyl cyclase inhibitor for treating neuropathic and inflammatory pain.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature, 2011
Joyce DeLeo, Alfonso Romero-Sandoval
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High-Throughput Screening Paradigm Identifying an Adenylyl Cyclase 2 Inhibitor

The Journal of Pharmacology and Experimental Therapeutics, 2013
openaire   +1 more source

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