Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that
transduce extracellular signals into cellular responses. They are major pharmacological …
transduce extracellular signals into cellular responses. They are major pharmacological …
[HTML][HTML] Role of calcium homeostasis in modulating EMT in cancer
CA Jones, LA Hazlehurst - Biomedicines, 2021 - mdpi.com
Calcium is essential for cells to perform numerous physiological processes. In cancer, the
augmentation of calcium signaling supports the more proliferative and migratory cells, which …
augmentation of calcium signaling supports the more proliferative and migratory cells, which …
Cryo-EM structure of the human adenosine A2B receptor–Gs signaling complex
The human adenosine A2B receptor (A2BR) is a class AG protein–coupled receptor that is
involved in several major physiological and pathological processes throughout the body …
involved in several major physiological and pathological processes throughout the body …
Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors
G Protein-coupled receptors (GPCRs) are the most frequently exploited drug target family,
moreover they are often found mutated in cancer. Here we used a dataset of mutations …
moreover they are often found mutated in cancer. Here we used a dataset of mutations …
N-Acyl-N-Alkyl Sulfonamide Probes for Ligand-Directed Covalent Labeling of GPCRs: The Adenosine A2B Receptor as Case Study
BLH Beerkens, V Andrianopoulou, X Wang… - ACS Chemical …, 2024 - ACS Publications
Small molecular tool compounds play an essential role in the study of G protein-coupled
receptors (GPCRs). However, tool compounds most often occupy the orthosteric binding …
receptors (GPCRs). However, tool compounds most often occupy the orthosteric binding …
A2B adenosine receptor signaling and regulation
ZG Gao, M Haddad, KA Jacobson - Purinergic Signalling, 2024 - Springer
The A2B adenosine receptor (A2BR) is one of the four adenosine-activated G protein-
coupled receptors. In addition to adenosine, protein kinase C (PKC) was recently found to …
coupled receptors. In addition to adenosine, protein kinase C (PKC) was recently found to …
[HTML][HTML] Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism
LS den Hollander, OJM Béquignon, X Wang… - Biochemical …, 2023 - Elsevier
Abstract CC chemokine receptor 2 (CCR2), a G protein-coupled receptor, plays a role in
many cancer-related processes such as metastasis formation and immunosuppression …
many cancer-related processes such as metastasis formation and immunosuppression …
[HTML][HTML] Stationed or relocating: The seesawing emt/met determinants from embryonic development to cancer metastasis
Epithelial and mesenchymal transition mechanisms continue to occur during the cell cycle
and throughout human development from the embryo stage to death. In embryo …
and throughout human development from the embryo stage to death. In embryo …
Cancer‐related somatic mutations alter adenosine A1 receptor pharmacology—A focus on mutations in the loops and C‐terminus
G protein‐coupled receptors (GPCRs) are known to be involved in tumor progression and
metastasis. The adenosine A1 receptor (A1AR) has been detected to be over‐expressed in …
metastasis. The adenosine A1 receptor (A1AR) has been detected to be over‐expressed in …
Current adenosinergic therapies: what do cancer cells stand to gain and lose?
A key objective in immuno-oncology is to reactivate the dormant immune system and
increase tumour immunogenicity. Adenosine is an omnipresent purine that is formed in …
increase tumour immunogenicity. Adenosine is an omnipresent purine that is formed in …