XPHuang
380 posts
XPHuang
@ahuangxp
@xphuang.bsky.social Biased for GPCRs, NIMH Psychoactive Drug Screening Program (PDSP), Roth Lab, UNC Pharmacology
North Carolina, USA Katılım Aralık 2015
337 Takip Edilen254 Takipçiler
🔬👩🔬 Exciting news! I'll soon start my lab @VAInstitute to research molecular mechanisms in Neurodegenerative diseases. 🧠💡 Now recruiting postdocs to join our dynamic research team! Email me if you're interested! #Postdoc #CryoEM #Neuroscience #ResearchOpportunity
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@zenbrainest @DR_WANG_SIBCB Congratulations on the great work @DR_WANG_SIBCB @chengjj_iHuman, and Eric Xu
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Amazing paper from @DR_WANG_SIBCB and others!
Flexible scaffold-based cheminformatics approach for polypharmacological drug design!
cell.com/cell/fulltext/…
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Discovery of Guanfacine as a Novel TAAR1 Agonist: A Combination Strategy through Molecular Modeling Studies and Biological Assays mdpi.com/2568246 #mdpipharmaceuticals via @MDPIOpenAccess
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XPHuang retweetledi
This is our latest study, about microglia and general anesthesia. The most important part is in the Discussion.
bioRxiv Neuroscience@biorxiv_neursci
Microglia facilitate and stabilize the response to general anesthesia biorxiv.org/cgi/content/sh… #biorxiv_neursci
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Nice review on GPCR intracellualr allosteric modulator sites. Brian Krumme's NTSR1 structure (PDB 8FNO) was used but his paper was not cited (pubmed.ncbi.nlm.nih.gov/36917754/).
Pharmacologically targeting intracellular allosteric sites of GPCRs for drug discovery pubmed.ncbi.nlm.nih.gov/37852356/
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@zenbrainest "Interestingly, the chemokine ligands CXCL11 and CXCL12 are not able to displace the binding of [3H]VUF15485 to ACKR3." The small ligand is a PAM agonist.
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Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3 biorxiv.org/content/10.110…
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XPHuang retweetledi
"N-Pyrrolidino protonitazene, ethyleneoxynitazene, N-desethyl protonitazene and N-desethyl etonitazene are potent Mu-opioid receptor (MOR) agonists."
Could the dihydrofuran analog be the odd one out? @Marthevdp
Christophe Stove@christophestove
👉 Quite a direct (& rapid) impact of our (even unpublished) work: #ACMD document refers to @Marthevdp's presentation on #ethyleneoxynitazene @ #TIAFT2023. 👉 Manuscript on N-pyrrolidino protonitazene & others submitted. Link to #ACMD advice & updates: #full-publication-update-history" target="_blank" rel="nofollow noopener">gov.uk/government/pub…
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XPHuang retweetledi
Tetracyclic antidepressants potently activate serotonin receptors 5-HT1e and 5-HT1F, explaining some of their clinically observed effects. @NeuroStructure @martafilizola @biorxivpreprint @biorxiv_neursci
biorxiv.org/content/10.110…
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Cool, structure based ligand design for GPR132, an oGPCR for endogenous lipids, once regarded as a proton-sensing GPCR.
Functional screening and rational design of compounds targeting GPR132 to treat diabetes pubmed.ncbi.nlm.nih.gov/37770763/
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Chloride ion is an allosteric modulator again, now at fish taste receptors.
Allosteric modulation of the fish taste receptor type 1 (T1R) family by the extracellular chloride ion pubmed.ncbi.nlm.nih.gov/37770555/
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Molecule of the week EN300-1604837
More details: bit.ly/461gAp3
#Enamine #molecule #chemistry #science #drugdiscovery
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Sucralose (aka Splendra) at GPR52, pEC50 is 0.23 mM and Emax of 3.43 fold change at 4 mM.
The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52 cdnsciencepub.com/doi/10.1139/cj…
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@GpcReid @GPCRHenry @Nedjma36193203 Here is a set of old Gs DREADD GloSensor cAMP data in transiently transfected HEK293 T cells.
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XPHuang retweetledi
An incredible study and resource with many important findings: including reclassification of group I mGluRs and some DREADDs, to name a few! Many congratulations to Kirill, Ikuo, and team.
Kirill Martemyanov Lab@KLabGPCR
Our systematic investigation of G protein coupling profiles of 100+ #GPCRs driven by the one and only Ikuo Masuho is out after ~10 years of work. We see many interesting patterns with the help of AI. Check it out- there is a useful reference table. doi.org/10.1016/j.celr…
Winnipeg, Manitoba 🇨🇦 English
@weinberz @LoydaMorales1 At room temperature, proton potency is about pH 7.5 in Gs GloSensor cAMP assays in HEK293 cells. GPR65 is 'constitutively' activated under neutral condition, assuming medium pH is about 7.4. pubmed.ncbi.nlm.nih.gov/32865988/
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