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Results found for "Elizabeth S. Dean"
- Fluorescence Polarization in GPCR Research
the other hand, when the polarized light hits the bound fluorescent ligand, the slower rotation speed means This means no washing steps are needed to reduce background signal. Figure 1. References Kumar V, Chunchagatta Lakshman PK, Prasad TK, Manjunath K, Bairy S, Vasu AS, Ganavi B, Jasti S, Kamariah N.
- Odorant receptors – a bit of smell for drug discovery
express multiple ORs, tumor cells associated with the nervous system express a single OR gene type (Kalra S. Al 2017) and its activation promotes migration and angiogenesis (Kim S. et. al 2015). OR2AT4 activation leads to reduced proliferation and enhanced apoptosis of acute myeloid leukemia cells (S cells proliferation via activation by β-ionone which initiates prostate cancer cell cycle arrest (Jones S.
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
the responsiveness of canonical G protein–coupled chemokine receptors that bind to the same ligand(s) an example of a dual-function receptor that directly regulates both cell migration and scavenging (S. Grundmann et al. 2018), did not affect chemokine scavenging, consistent with prior work (S. Scavenging may allow cells to continuously migrate by remaining responsive to chemokines (S.
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown.
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
Previously, we had identified a novel pyrazole-based agonist 1 ((S)-N-(1-(cyclobutylamino)-1-oxo-5-(piperidin
- New role of β-arrestins in MOR signaling
every day from an opioid overdose in the U.S., combatting the opioid overdose epidemic has become a mean Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391. Faouzi A, Varga BR, Majumdar S. Biased Opioid Ligands. Shiraki A, Shimizu S.
- Dr. GPCR University registration is now open! Secure your spot now!
includes congrats to: Clementine E Philibert and Mikel Garcia-Marcos for their work on Smooth operator(s) challenges Modulating Vertebrate Physiology by Genomic Fine-Tuning of GPCR Functions Smooth operator(s)
- Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets
November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s
- Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
Defensins and Mrgpra2 were critical for combating S. aureus infections and the formation of neutrophil
- Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools
Research Needs Built on more than two decade A GPCR Internalization Tool Designed for Real Research Needs s
- 📰 GPCR Weekly News, July 31 to August 6, 2023
Randy Hall's study: GPR37L1's role in shaping cortical astrocytes during development Dr. And Advance Novel Oral Small Molecule Medicines Targeting G Protein-Coupled Receptors Novo Nordisk A/S:
- Maria’s Travel Blogs: ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025
This joint effort by both associations is repeated every year, with 2026’s being in Dublin, Ireland.
- Understanding Enzyme Inhibition In GPCR Discovery Programs
sugar monophosphates; Pharmacology 2025; Nxera Pharma earns $10m milestone from AbbVie neurological deal This spotlight from Montana Molecular dives into how OPN3’s modulation of MCR4 in appetite circuits and
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
domain (WAP) is necessary for this modulatory activity, although data from GST pull-down (glutathione-S-transferase
- 📰 GPCR Buzz: August 5-11, 2024 | Top Highlights from DrGPCR University!
Dear GPCR Enthusiasts! Get ready to save the dates! Dr. s Check out the details of each course below: Open to the Public: Enrollment is Now Available!
- Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital ...
These data will be shared as an oral presentation by Ron S.
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
through cAMP/protein kinase A signaling, consistent with AVPR2 coupling to the G protein subunit alpha s.
- Using Live-cell High-Content Screening to Characterize CB2 Ligands: Insights From 16 Synthetic Cannabinoids
AV07, AV11, AV1 and AV18A showing specific displacement of CELT331 (80 nM) with fitted IC₅₀ values (mean What This Means for CB2 Drug Discovery Programs Taken together, the dataset offers several insights into References Brogi, S., Corelli, F., Di Marzo, V., Ligresti, A., Mugnaini, C., Pasquini, S., & Tafi, A.
- High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands
Source: Way GP, Sailem H, Shave S, Kasprowicz R, Carragher NO. Lin S, Schorpp K, Rothenaigner I, Hadian K. Image-based high-content screening in drug discovery.
- AlphaFold’s Breakthrough in GPCR Research: Revolutionizing Discovery, Yet Awaiting Experimental Proof
While AlphaFold2’s ability to predict static structures was groundbreaking, however, GPCRs are highly
- Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
The results provide rationale for considering a combination(s) of FDA-approved SFK (dasatinib) and MEK
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
Jang W, Senarath K, Feinberg G, Lu S, Lambert NA.
- Why Intracellular Drugs May Hold the Key to GPCR Therapeutics
Here ’s what members get: Weekly deep dives from Dr.
- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work in a developing Natural Products and Compounds: Potential Therapeutic Targets for the Treatment of Neurological Disease s
- The Impact of CB1 Receptor on Nuclear Receptors in Skeletal Muscle Cells
Further research is required to fully delineate their role(s)."
- 📰 GPCR Weekly News - January 2 to 8, 2023
s Director Stephen A.
- Unveiling GPCR Priming: The Hidden Synergy in Cellular Signalling
Proc Natl Acad Sci U S A, 2020. 117(35): p. 21723-21730. 2.
- Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling
Proc Natl Acad Sci U S A, 2012. 109 (45): p. 18607-12. 8.
- Decoding Schild Analysis: The Pharmacologist’s Lens on Competitive Antagonism
Here, the Schild plot becomes a diagnostic tool rather than a checkbox test: Slopes >1 often mean incomplete It ’s a screening tool, not a substitute for rigorous Schild validation.
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
This means that even if one of the ligands they are bound to is promiscuous, it will not compromise assay Data represent the mean ± SEM (n = 3 in triplicate). Degorce F, Card A, Soh S, Trinquet E, Knapik GP, Xie B.













