Results 171 to 180 of about 83,442 (296)
Progress on the development of Class A GPCR‐biased ligands
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales+20 more
wiley +1 more source
A PDE4 shortform degrader: a first in isoform‐specific PDE4 inhibition
Clinically used phosphodiesterase 4 (PDE4) inhibitors lack selectivity for PDE4 enzyme isoforms, which leads to documented side effects. Building in enzyme selectivity has proved difficult because all PDE4 enzymes share highly conserved catalytic domains. The report by Sin et al.
Donald H. Maurice
wiley +1 more source
Cellular localization of the Mn2+‐dependent adenylyl cyclase (AC) in rat testis [PDF]
Jan O. Gordeladze+4 more
openalex +1 more source
The second messenger cyclic AMP (cAMP) dedifferentiates pathologic lung and skin myofibroblasts derived from patients with scleroderma by inhibiting the MAPK p38α. Though cAMP has anti‐fibrotic effects in fibroblasts from both organs, the cellular capacity to generate cAMP in response to the canonical stimulus prostaglandin E2 (PGE2) is substantially ...
Jared D. Baas+4 more
wiley +1 more source
Cholera Toxin Action on Rabbit Corpus Luteum Membranes: Effects on Adenylyl Cyclase Activity and Adenosine Diphospho-ribosylation of the Stimulatory Guanine Nucleotide-binding Regulatory Component1 [PDF]
Anne N. Hirshfield
openalex +1 more source
CAP Is a Bifunctional Component of the Saccharomyces cerevisiae Adenylyl Cyclase Complex [PDF]
Jeffrey E. Gerst+4 more
openalex +1 more source
Allosteric activation of the nitric oxide receptor soluble guanylate cyclase mapped by cryo-electron microscopy. [PDF]
Soluble guanylate cyclase (sGC) is the primary receptor for nitric oxide (NO) in mammalian nitric oxide signaling. We determined structures of full-length Manduca sexta sGC in both inactive and active states using cryo-electron microscopy. NO and the sGC-
Hammel, Michal+6 more
core
Exchange of substrate and inhibitor specificities between adenylyl and guanylyl cyclases [PDF]
The active sites of guanylyl and adenylyl cyclases are closely related. The crystal structure of adenylyl cyclase and modeling studies suggest that specificity for ATP or GTP is dictated in part by a few amino acid residues, invariant in each family ...
Beuve, A.+5 more
core +1 more source