Endogenous intracellular allosteric modulators of GPCRs remain largely unexplored, with limited binding and phenotype data available. This gap arises from the lack of robust computational methods for ...

Evotec's insights into GPCRs and waveRAPID technology reveal new opportunities in drug discovery, focusing on orphan ...

and PKA (protein kinase A) in turn phosphorylates the receptor and turns off the G-protein signaling (heterologous desensitization, red line, and phosphate). GRK (GPCR kinase)-mediated GPCR ...

More importantly, using 2 label reversal datasets, GPCR and Kinase, CPGL showed superior performance compared to other existing deep learning models. The AUC were substantially improved by 20% on the ...

The canonical view of GPCRs is that they sit on the cell membrane where they activate a variety of reactions, including an enzyme called extracellular-signal-regulated kinase (ERK), which triggers a ...

The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of the ... This effect involves the sequential and additive action of protein kinase A, casein kinase I, and the ...

Septerna’s proprietary technology recapitulates GPCRs with their native structure, function and dynamics for unprecedented drug discovery for many diseases “GPCRs have proven to be the most prolific ...

Emerging evidence indicates that GRK2 can interact with a large number of GPCRs and non-GPCR substrates in both kinase-dependent and -independent modes. Some of these pathways are associated with ...

United States G protein-coupled receptor kinase 2 (GRK2) is an adapter protein that modulates G protein-coupled receptor (GPCR) signaling. It also regulates the functions and activity of other ...

GPCRs continue to be of intense interest as ... between GPRC5A and EPH receptor A2 (EphA2), a focal adhesion kinase (FAK)-regulating receptor tyrosine kinase. Overall, the data suggest GPRC5A ...

Smoothened, a G‐protein coupled receptor family member, interacts with the RNA‐ binding protein Smaug and promotes its phosphorylation by the kinase Fused. Phosphorylation of Smaug reduces its levels, ...