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The κ opioid receptor (κ receptor, KOR) is a G protein‐coupled receptor with well established roles in analgesia and immune modulation. Although historically studied primarily in the central nervous system (CNS), growing evidence indicates that κ signalling in peripheral tissues plays an important role in regulating pain, inflammation and immune ...
Rumsha Khan +3 more
wiley +1 more source
Xanomeline and Trospium Chloride: Mechanism of Action, Clinical, and Translational Science
ABSTRACT Xanomeline‐trospium chloride (Cobenfy, formerly KarXT) is a first‐in‐class, oral central M1/M4 muscarinic receptor agonist approved for the treatment of schizophrenia in adults. Cobenfy represents a paradigm shift by avoiding direct dopamine D2 receptor blockade and thus significantly reduces the burden of metabolic, extrapyramidal, and ...
Samantha Avila, Ingrid L. Chen
wiley +1 more source
Four series of 20 (het)aryl substituted 7‐deazapurine nucleobases were synthesized. Several potent antagonists of all four subtypes of adenosine receptors were identified by functional assay. High‐throughput screening of the IMTM compound library for modulatory activity on adenosine receptors (ARs) identified two deazapurine hits based on 2,6‐diaryl‐7 ...
Ugnė Šinkevičiūtė +9 more
wiley +1 more source
An adenylyl cyclase that functions during late development of Dictyostelium
A variety of extracellular signals lead to the accumulation of cAMP which can act as a second message within cells by activating protein kinase A (PKA).
Fuller, D +4 more
core
Editorial: Adenylyl cyclase isoforms as potential drug targets
Tarsis F. Brust +3 more
doaj +1 more source
\(\bf Aims\) In contrast to the membrane bound adenylyl cyclases, the soluble adenylyl cyclase (sAC) is activated by bicarbonate and divalent ions including calcium. sAC is located in the cytosol, nuclei and mitochondria of several tissues including cardiac muscle. However, its role in cardiac pathology is poorly understood. Here we investigate whether
Schirmer, Ilona +11 more
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The adenylyl and guanylyl cyclase superfamily
Current Opinion in Structural Biology, 1998New structures solved in 1997 revealed that the adenylyl cyclase core consists of a pair of catalytic domains arranged in a wreath. Homologous catalytic domains are arranged in diverse adenylyl and guanylyl cyclases as symmetric homodimers or pseudosymmetric heterodimers.
James Hurley
exaly +3 more sources
Inhibition of human thyroid adenylyl cyclase by 2-iodoaldehydes
2-Iodohexadecanal (IHDA), which can be formed upon addition of iodine to the vinyl ether group of plasmalogens, has been identified as a major thyroid iodolipid (Pereira et al. (1990) J. Biol. Chem. 265, 17018-17025).
Valerie Panneels +2 more
exaly +1 more source

