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80 items found for "Timm H Westhoff"
- A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...
August 2022 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology characterized this H3R biosensor on intact cells by monitoring the effect of consecutive ligand injections in time
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
Using time-resolved cryo-electron microscopy (cryo-EM) and variability analysis to monitor the transitions Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).
- Time is your enemy, GPCRs are your friend
Come attend this month's virtual café talk to see the awesome work of Dr. Stuart Maudsley on how an aging physiological context affects #GPCR signaling #drgpcr. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- Residency time of agonists does not affect the stability of GPCR-arrestin complexes
September 2022 " Background and purpose: The interaction of arrestins with G-protein coupled receptors (GPCRs) desensitizes agonist-dependent receptor responses and often leads to receptor internalization. GPCRs that internalize without arrestin have been classified as "class A" GPCRs whereas "class B" GPCRs co-internalize with arrestin into endosomes. The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation. Here, we ask the question whether agonists with very slow off-rates can cause the formation of particularly stable receptor-arrestin complexes." Read more at the source #DrGPCR #GPCR #IndustryNews
- Dr. Tim De Groof - Dr. GPCR Podcast
Tim De Groof! It’s not often when you get the best of both worlds - nano-bodies and #GPCRs.
- APEX2/AUR Biosensor: A Powerful Tool for Protein Interaction and Trafficking
peroxidase enzyme that catalyzes the oxidation of specific substrates in the presence of hydrogen peroxide (H When AUR is oxidized by APEX2 in the presence of H 2 O 2 , it produces a fluorescent product that can The development of molecular tools to study GPCR trafficking in real-time opens new avenues for understanding
- Addex Therapeutics CEO Tim Dyer: There is a $4-bil market opportunity in dyskinesia
January 2022 "Watch our CEO Tim Dyer on AlphaStreet. In his interview, Mr.
- Nanobodies: New Dimensions in GPCR Signaling Research
., Choi, H. J., Fung, J. J., Pardon, E., Casarosa, P., Chae, P. S., Devree, B. T., Rosenbaum, D. H., Pautsch, A., Steyaert, J., Weis, W. I., & Kobilka, B. K. (2011). M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hübner, H., Pardon, E., Valant, C., Sexton, P. O., Ploegh, H. L., & Garcia, K. C. (2015). Structural biology. D., Tworak, A., Watanabe, K., Pardon, E., Steyaert, J., Kandori, H., Katayama, K., Kiser, P.
- From DNA day to GPCR genomics
conformational changes that occur during G-protein activation by the β2-adrenergic receptor, using a time-resolved L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. G., & Schiöth, H. B. (2003). M., Pérez-Hernández, G., Batebi, H., Gao, Y., Eskici, G., Seven, A. Time-resolved cryo-EM of G protein activation by a GPCR. bioRxiv : the preprint server for biology, 2023.03.20.533387
- Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall ...
Unlike LGR2 in other insect species, HLGR2 was found to play a crucial role in the control of H. cunea Conclusion: HLGR2 is essential for the growth and development and wing expansion and maturation in H.
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
fluorescence, electrochemiluminescence, fluorescence emission, immunofluorescence staining, HTRF (homogeneous time-resolved fluorescence), and TR-FRET (time-resolved fluorescence resonance energy transfer). References Eishingdrelo, H., & Kongsamut, S. (2013). Wei, H., Ahn, S., Shenoy, S. K., Karnik, S. S., Hunyady, L., Luttrell, L. M., & Lefkowitz, R.
- Odorant receptors – a bit of smell for drug discovery
than 60 ORs in the testis and only a few ORs in the liver (Flegel C. et al. 2013; Maßberg D. and Hatt H. although there are highly increased in prostate tissue, especially in prostate cancer (Maßberg D. and Hatt H. olfactory-specific chaperones to be correctly targeted to the surface of heterologous cells (Maßberg D. and Hatt H.
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
will facilitate further development of therapeutic agents targeting the DOR.Communicated by Ramaswamy H.
- Decoding β-Arrestins: from Structure to function
F et al. 2021, Chen, H. et al. 2022). H., & Lee, J. H. 2020, Casiraghi, M. et al. 2019), double electron-electron resonance (DEER) spectroscopy for high-resolution M. et al. 2019), and hydrogen-deuterium exchange (HDX) mass spectrometry for time-dependent conformational
- Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors
expression, restoration to ≥57% of WT levels was achieved for 6 by treatment with 1 µM CAN1404 for 24 h,
- Do You Believe AI Could Accelerate Drug Discovery?
Of 161 molecules tested, 42 substituted more than 50% of [³H]-LSD at 10 μM, achieving a 26% hit rate.
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
Nature chemical biology, 5(10), 734–742. https://doi.org/10.1038/nchembio.206 Wei, H., Ahn, S., Shenoy Z., Wilderman, A., Katakia, T., McCann, T., Yokouchi, H., Zhang, L., Corriden, R., Liu, D., Feigin, M
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
The increase in active β-arrestin molecules and the time they spend diffusing on the plasma membrane H., Heydenreich, F. M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K.
- Overview of adhesion GPCRs self-activation
However, at that time the structural conformation of the transmembrane (TM) region was not yet known. Qian, Y., Ma, Z., Liu, C., Li, X., Zhu, X., Wang, N., Xu, Z., Xia, R., Liang, J., Duan, Y., Yin, H.,
- Ode to GPCRs
George H. Edmond H.
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
all of the other current GPCR discovery procedures, Orion’s approach does not require the onerous and time-consuming of a small protein GPCR ligand using new peptide chemistry technology and rational design Gaertner, H.
- Bell-Evans model and steered molecular dynamics in uncovering the dissociation kinetics of ligands..
kinetics-based drug development have become immensely interested in predicting the drug target residence time Screening drug candidates in terms of their computationally predicted residence times, which is a measure from steered molecular dynamics simulations and the Bell-Evans model to predict the absolute residence times We have predicted the absolute ligand residence times on the timescale of seconds.
- Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling
Bioluminescence Resonance Energy Transfer (BRET), has revolutionized the study of GPCRs by enabling real-time One of the significant advantages of FRET and BRET-based sensors is their ability to provide real-time discovery efforts by enabling the precise characterization of pharmacological interventions in real time Galés, C., et al., Real-time monitoring of receptor and G-protein interactions in living cells. Eidne, Bioluminescence resonance energy transfer (BRET) for the real-time detection of protein-protein
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling pathways over time weeks to allow biosensor expression, fiber photometry is used in order to record drug responses in real time
- 📰 GPCR Weekly News, April 29 to May 5, 2024
If you aren't joining us this time, stay tuned for more Dr. GPCR University content coming soon.
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
In this study, for the first time, we demonstrate the nuclear localization of H2R in lymphatic endothelial At the same time, H2R as a GPCR imparts many unresolved questions, such as the functional relevance of
- FSH and bone: Comparison between males with central versus primary hypogonadism
aims to investigate the possible role of FSH excess in male bone health, by comparing for the first time