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494 items found for "Bcl-2"
- Ode to GPCRs
different functional entities: (1) a discriminator or receptor, which binds the primary messenger, (2) Nobel Prize in Physiology or Medicine 1947. https://www.nobelprize.org/prizes/medicine/1947/summary/. 2. /2000/summary/. 55. ACS Pharmacol Transl Sci 3, 203–220 (2020). https://pubs.acs.org/doi/10.1021/acsptsci.0c00004/. 72. ACS Pharmacol Transl Sci 3, 221–236 (2020). https://pubs.acs.org/doi/full/10.1021/acsptsci.0c00006/.
- Do You Believe AI Could Accelerate Drug Discovery?
The AlphaFold database encompasses over 200 million proteins, aiding structural biology, protein design Of 161 molecules tested, 42 substituted more than 50% of [³H]-LSD at 10 μM, achieving a 26% hit rate. The highest affinity compounds (15 to 24 nM) were identified from AF2 docking. Science https://doi.org/10.1126/science.adn6354 (2024) Abramson, J., Adler, J., Dunger, J. et al. Nature 630, 493–500 (2024). https://doi.org/10.1038/s41586-024-07487-w
- Navigating the Signaling Network: RTK and GPCR Crosstalk Uncovered
., & Ghosh, P. (2024).
- Canonical chemokine receptors as scavenging “decoys”
E, 2002). J., 2013). E., et al. 2008). T., et al., 2013). E., et al. 2008).
- From DNA day to GPCR genomics
In the United States, DNA Day was officially celebrated on April 25th, 2003. Eventually, April 25th was declared and recognized as International DNA Day1. S. (2002) National Human Genome Research Institute. W., & Skiniotis, G. (2023). . https://doi.org/10.1101/2023.03.20.533387
- Chemokine receptor-targeted drug discovery: progress and challenges
system is implicated in a wide range of inflammatory, autoimmune and infectious diseases (Proudfoot 2002 immunosuppressive tumor microenvironment, and facilitate metastatic spread (Nagarsheth, Wicha, and Zou 2017 ; Poeta et al. 2019). ongoing, completed or recruiting) (Isberg et al. 2016). ; Wang and Norcross 2008).
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Nibbs et al. 2013). Volpe et al. 2012). Gurevich, et al. 2018; Y. A. Berchiche et al. 2011). Volpe et al. 2012; B. N. Zhao et al. 2019). Sapmaz et al. 2019, M. N. J. Seaman 2012).
- Odorant receptors – a bit of smell for drug discovery
initiate a neuronal response that drives odorant discrimination and perception (Young J. and Trask B. 2002 highly variable from more than 60 ORs in the testis and only a few ORs in the liver (Flegel C. et al. 2013 ; Maßberg D. and Hatt H. 2018). there are highly increased in prostate tissue, especially in prostate cancer (Maßberg D. and Hatt H. 2018 Al 2017) and its activation promotes migration and angiogenesis (Kim S. et. al 2015).
- TM5-TM6: structural switches that modulate the coupling of serotonin receptors to Gs or Gi
., 2022 to investigate the molecular basis involved in G protein-receptor interactions, particularly Additionally, structural analysis of the TM5 and TM6 regions of 27 class A GPCRs coupled to Gs or Gi/ o yielded similar results, TM5 was 5.6 ± 1.5 residues longer while TM6 was 2.6 ± 1.6 residues shorter pubmed.ncbi.nlm.nih.gov/35714614/ *Above information was taken from the original article published by Huang et al., 2022
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
September 2022 "Over 100 mutations in the rhodopsin gene have been linked to a spectrum of retinopathies We identify 69 retinopathy variants, including 20 previously uncharacterized variants, that exhibit diminished
- The Gluopsins: Opsins without the Retinal Binding Lysine
September 2022 "Opsins allow us to see.
- Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling
October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
October 2022 GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed
- Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies
- Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures The method has found druggable sites overlapping with the cocrystallized allosteric ligands in 21 GPCR We then mapped the 394 GPCR X-ray structures available at the time of the analysis (September 2020). Results show that for each of the 21 structures with bound ligands there exist many other GPCRs that
- Emerging approaches for decoding neuropeptide transmission
November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
September 2022 "Sound is converted by hair cells in the cochlea into electrical signals, which are transmitted
- GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin...
August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous cryo-electron microscopy structures of CX3CR1-Gi1 complexes in ligand-free and CX3CL1-bound states at 2.8
- Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells
September 2022 "Pregnant and lactating women have been discouraged from using cannabis by Health Canada Our results demonstrated that THC and CBD reduced cellular viability at concentrations above 30μM and 20μM
- Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...
October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and
- Co-activation of GPCRs facilitate GIRK-dependent current
October 2022 "The activity of dopamine neurons is dependent on both intrinsic properties and afferent
- G protein-coupled receptor signaling: transducers and effectors
October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance
- Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking: ...
October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking