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Results found for "positive allosteric modulators"
- Trevena Announces Advancement of TRV045 Into Clinical Development for Diabetic Neuropathic Pain
TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival.
- Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation
- When Pain Becomes a Catalyst: How Personal Experience Redefined One Scientist’s Mission
His interest in model development, in capturing the lived human experience through preclinical systems on RGS proteins , pain comorbidities like addiction and depression, and pushing for more accurate model
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
Moreover, Frizzleds and Celsrs have been demonstrated to play core roles in the modulation of cochlear
- 📰 GPCR Weekly News, May 6 to 12, 2024
CCR6 for Autoimmune Diseases MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model and Clinical Management of the TADopathy, X-Linked Acrogigantism Thrombosis With Thrombocytopenia and Post-COVID-Vaccination inhibition with the porcupine inhibitor LGK974 decreases trabecular bone but not fibrosis in a murine model Chemistry July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs Post Doctoral Fellow Postdoc Position Principal Scientist, In vitro Pharmacology Senior Associate Scientist
- Using Live-cell High-Content Screening to Characterize CB2 Ligands: Insights From 16 Synthetic Cannabinoids
The cannabinoid receptor type 2 (CB2R) has emerged as a compelling target across inflammation, immune modulation For teams optimizing CB2 modulators —or exploring biased agonism, polypharmacology, or downstream signaling—live-cell
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
; whether they regulate intracellular cyclic AMP (cAMP) and calcium concentrations ([Ca2+]i), which modulate These findings suggest that the melatonin MT2 receptor is expressed in ASM, and modulates airway smooth
- Immunomodulatory Role of Neuropeptides in the Cornea
However, progress in this area has led to an increase in studies that have begun modulating neuropeptide
- Fentanyl and Xylazine: Why Breathing Fails in Overdose
Catherine’s work lays the foundation for designing better interventions, from preclinical models to clinical From Street Samples to Lab Models What makes Catherine’s research particularly powerful is how it stays collaborating with harm-reduction groups such as the Red Project in Grand Rapids , she ensures her models For Catherine, those numbers aren’t just statistics—they’re signals guiding how to build better models
- VAMP2: a crucial player in the delivery of MOR to the synapse
synthesis in the endoplasmic reticulum, GPCRs are transported to the Golgi apparatus to undergo additional post-translational SNARE protein complex in neurotransmitter release has been well characterized, the mechanisms that modulate , which can interact with different fusion proteins and also this different molecular codes will be modulated
- GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP
Our results revealed that GB83 is a bona fide agonist of PAR2 that uniquely modulates PAR2-mediated cellular
- Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage...
neuromodulators, acting through G-protein-coupled receptors (GPCRs), fine-tune motoneuron (MN) IME by modulating However, intracellular partners linking GPCRs to TASK1 modulation are not yet well-known.
- Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism, microbiota..
roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R activation in gut IELs to modulation
- AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
Recently, AlphaFold2 has been developed to predict structure models of many functionally important proteins Herein we evaluated the accuracy of GPCR structure models predicted by AlphaFold2. However, the predicted models and experimental structures were different in many aspects including the These differences impeded the use of predicted structure models in the functional study and structure-based
- Why Dose-Response Curves Are Pharmacology’s Secret Weapon
lecture walks you through: What dose-response curves are and why they’re indispensable How curve-fitting models
- Serotonin Receptor 5-HT2A Regulates TrkB Receptor Function in Heteroreceptor Complexes
the regulated expression of 5-HT2A and TrkB is a molecular mechanism for the brain-region-specific modulation
- What If the Most Important Part of Your Drug Isn’t What It Binds—But What It Does?
through real-world experiments, decades of receptor pharmacology wisdom, and the cutting-edge operational model
- Rhodopsin as a Molecular Target to Mitigate Retinitis Pigmentosa
update on the current knowledge regarding small molecule compounds that have been evaluated as rhodopsin modulators
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
If you’ve read our previous post, you probably know what CELT-335 is and its high affinity for the cannabinoid CB2R are located primarily in the immune system and peripheral tissues, where they modulate inflammation
- Decoding β-Arrestins: from Structure to function
signaling: conformational dynamics and intracellular responses GPCR signaling is a complex process modulated Apart from G proteins, GPCRs engage other effectors for signaling modulation. tissue-specific expression, have played a pivotal role in identifying essential effector proteins that modulate
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
Polygalaxanthone III and Pachymic acid, could interact with multiple targets (5-HTR, DR, ADRA, AR, ESR, NR3C1) and modulate
- Endosomal parathyroid hormone receptor signaling
October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation In this model, GPCR signaling is turned-off by receptor phosphorylation via GPCR kinases (GRKs) and subsequent However, over the last decade, this model has been extended by discovering that some internalized GPCRs
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
axis of PTK2, integrin αIIbβ3, and CIB1 in collagen- and GPVI-dependent thrombus formation, which is modulated
- GPR15 expressed in T lymphocytes from RA patients is involved in leukocyte chemotaxis to the...
Recent evidence indicates that GPR15 may be associated with modulation of the chronic inflammatory response
- A central alarm system that gates multi-sensory innate threat cues to the amygdala
findings suggest that parallel pathways independently relay innate threat signals from different sensory modalities about whether and how multi-sensory innate threat cues are integrated and conveyed from each sensory modality lateral parabrachial nucleus in the brainstem respond to multi-sensory threat cues from various sensory modalities
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating
- HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural ...
studies of class IB phosphoinositide 3-kinases There is considerable interest in developing antibodies as modulators
- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
The current study has attempted to close the gap by generating highly refined model structures of C5aR2 inactive), complexed to C-terminal peptide of C5a (meta-active) and the C5a (active), embedded to a model The computational modeling and the 1.5-μs molecular dynamics data presented in the current study are






