@ahuangxp

@xphuang.bsky.social Biased for GPCRs, NIMH Psychoactive Drug Screening Program (PDSP), Roth Lab, UNC Pharmacology

 North Carolina, USA
Joined December 2015
  • Tweets380
  • Following337
  • Followers254
7Media
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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This is our latest study, about microglia and general anesthesia. The most important part is in the Discussion.
bioRxiv Neuroscience@biorxiv_neursci10 Oct 2023
Microglia facilitate and stabilize the response to general anesthesia biorxiv.org/cgi/content/shor… #biorxiv_neursci
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If you need Blue Sky invite code, let me know.
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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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I have one invite code for Blue Sky to share
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"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@christophestove8 Oct 2023
Replying to @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👉 Quite a direct (& rapid) impact of our (even unpublished) work: #ACMD document refers to @Marthevdp's presentation on #ethyleneoxynitazene @ #TIAFT2023.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: gov.uk/government/publicatio… 3/3

ACMD advice on 2-benzyl benzimidazole and piperidine benzimidazolone opioids

A review of the evidence on the use and harms of 2-benzyl benzimidazole (nitazene) and piperidine benzimidazolone (brorphine-like) opioids.

gov.uk
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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/…

Structural Insights into the Unexpected Agonism of Tetracyclic Antidepressants at Serotonin...

Serotonin (5-hydroxytryptamine, 5-HT) acts via 13 different receptors in humans. Of these receptor subtypes, all but 5-HT1eR have confirmed roles in native tissue and are validated drug targets....

biorxiv.org
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I am now on the other site, color code = 09f, it is pure!
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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…

Functional screening and rational design of compounds targeting GPR132 to treat diabetes - PubMed

Chronic inflammation due to islet-residing macrophages plays key roles in the development of type 2 diabetes mellitus. By systematically profiling intra-islet lipid-transmembrane receptor signalling...

pubmed.ncbi.nlm.nih.gov
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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…

Allosteric modulation of the fish taste receptor type 1 (T1R) family by the extracellular chloride...

Many G protein-coupled receptors (GPCRs) are allosterically modulated by inorganic ions. Although the intraoral ionic composition of the oral cavity varies depending on the living environment and...

pubmed.ncbi.nlm.nih.gov
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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…

The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively active...

Non-nutritive sweeteners are popular food additives owing to their low caloric density and powerful sweetness relative to natural sugars. Their lack of metabolism contributes to evidence proclaiming...

cdnsciencepub.com
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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. – at Winnipeg, Manitoba
Kirill Martemyanov Lab@KLabGPCR25 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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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…

ADGRL1 is a glucose receptor involved in mediating energy and glucose homeostasis - PubMed

Altogether, our findings demonstrate that ADGRL1 binds glucose and is involved in energy as well as glucose homeostasis in a sex-dependent manner. Targeting ADGRL1 may introduce a new class of drugs...

pubmed.ncbi.nlm.nih.gov
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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…

Mining the ZINC database of natural products for specific, testosterone-like, OXER1 antagonists -...

OXER1, the receptor for the oxidized arachidonic acid metabolite 5-oxo-ETE has been reported to play a significant role in inflammatory responses, being responsible for leucocyte chemotactic respon...

pubmed.ncbi.nlm.nih.gov
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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…

G protein-biased LPAR1 agonism of prototypic antidepressants: Implication in the identification of...

Prototypic antidepressants, such as tricyclic/tetracyclic antidepressants (TCAs), have multiple pharmacological properties and have been considered to be more effective than newer antidepressants,...

pubmed.ncbi.nlm.nih.gov
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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…

Ligand-Free Signaling of G-Protein-Coupled Receptors: Physiology, Pharmacology, and Genetics -...

G-protein-coupled receptors (GPCRs) are ubiquitous sensors and regulators of cellular functions. Each GPCR exists in complex aggregates with multiple resting and active conformations. Designed to...

pubmed.ncbi.nlm.nih.gov
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