7 Photos and videos
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 retweeted
28 Oct 2023
This is our latest study, about microglia and general anesthesia. The most important part is in the Discussion.
10 Oct 2023
Microglia facilitate and stabilize the response to general anesthesia biorxiv.org/cgi/content/shor… #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/3691…).
Pharmacologically targeting intracellular allosteric sites of GPCRs for drug discovery pubmed.ncbi.nlm.nih.gov/3785…
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XPHuang retweeted
8 Oct 2023
"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
8 Oct 2023
👉 Quite a direct (& rapid) impact of our (even unpublished) work: #ACMD document refers to @Marthevdp's presentation on #ethyleneoxynitazene @ #TIAFT2023.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:
gov.uk/government/publicatio…
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XPHuang retweeted
8 Oct 2023
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/10.1101/…
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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/3777…
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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/3777…
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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/10.113…
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XPHuang retweeted
25 Sep 2023
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.
25 Sep 2023
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.celrep.202…
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XPHuang retweeted
19 Sep 2023
Looking for two highly motivated postdocs to work on accelerated molecular simulations and AI-driven drug discovery. Please feel free to submit application to one of the following postings & retweet:
unc.peopleadmin.com/postings…
unc.peopleadmin.com/postings…
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A glucose-sensing GPCR and glucose could be an allosteric modulator for the adhesion receptor.
ADGRL1 is a glucose receptor involved in mediating energy and glucose homeostasis pubmed.ncbi.nlm.nih.gov/3771…
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XPHuang retweeted
12 Sep 2023
This #TriviaTuesday is a real stinker. What metal found in the human body is necessary for mammals to smell skunk spray, among other foul sulfur-based odors?
29%
Iron
14%
Magnesium
29%
Zinc
29%
Copper
7 votes • Final results
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Interesting compounds, sounds like biased antagonists at OXE receptor? Unfortunately, UNC does not have access to the full paper.
Mining the ZINC database of natural products for specific, testosterone-like, OXER1 antagonists pubmed.ncbi.nlm.nih.gov/3769…
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NIMH PDSP (pdsp.unc.edu/), part of the Roth lab at UNC, is hiring a Research Specialist to perform binding & functional assays with GPCRs. If you have life science background with molecular biology experience, please apply using the link below.
unc.peopleadmin.com/postings…
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"...G protein-biased agonism of LPAR1 as a promising target for the development of novel antidepressants."
G protein-biased LPAR1 agonism of prototypic antidepressants: Implication in the identification of novel therapeuti… pubmed.ncbi.nlm.nih.gov/3767…
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"The hypothesis is proposed that ligand-free signaling of 5-HT2A receptors mediate therapeutic effects of psychedelic drugs."
Ligand-Free Signaling of G-Protein-Coupled Receptors: Physiology, Pharmacology, and Genetics pubmed.ncbi.nlm.nih.gov/3768…
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