@DrGPCR

Join the movement, connect, share, and speed GPCR drug discovery. #GPCR Ecosystem. https://xitter.cf/t.co/jPzcdANDn1

 Boston MA
DrGPCR.com/Ecosystem
Joined January 2020
  • Tweets3.2K
  • Following4.4K
  • Followers3.9K
1.7KMedia
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DrGPCR@DrGPCRAug 11
Obesity co-agonists hit amylin, GLP-1, and GIP at once. Profiling all three across cAMP and β-arrestin shows how one molecule splits its activity. AMY/CALCR, GLP1R, and GIPR assays from Eurofins DiscoverX: ecosystem.drgpcr.com/post/re… #DrGPCR #GPCR
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Happy to count Eurofins Discovery in the Dr. GPCR ecosystem: one partner for end-to-end GPCR drug discovery. Screening, selectivity, safety, biased signaling, deorphanization. 30+ yrs expertise, 2,750+ assays. ecosystem.drgpcr.com/post/dr… #DrGPCR #GPCR #DrugDiscovery
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Two hours out. Biophysical Approaches to Orphan GPCR Drug Discovery with Dmitry Veprintsev, 10 AM ET. ThermoBRET, G protein recruitment, Gi-CASE. Bring your questions. ecosystem.drgpcr.com/gpcr-ma… #DrGPCR #GPCR
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Tomorrow at 10 AM ET: Biophysical Approaches to Orphan GPCR Drug Discovery with Dmitry Veprintsev. Express the receptor, confirm engagement, measure function. Live, with Q&A. ecosystem.drgpcr.com/gpcr-ma… #DrGPCR #GPCR
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Tomorrow at 11 AM ET / 8 AM PT. Functional Volume Control with Dr. Terry Kenakin. In collaboration with @EurofinsDscvrx. Registration open until we go live. ecosystem.drgpcr.com/gpcr-we… #DrGPCR #GPCR
Dr. GPCR and Eurofins DiscoverX webinar card reading Live September 24, 11 AM ET / 8 AM PT.

ALT Dr. GPCR and Eurofins DiscoverX webinar card reading Live September 24, 11 AM ET / 8 AM PT.

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Two days out. Functional volume control, live with Terry Kenakin. Thursday Sept 24, 11 AM ET / 8 AM PT. Free. Live Q&A. Recording afterward. Bring your questions. ecosystem.drgpcr.com/gpcr-we… #DrGPCR #GPCR
Dr. GPCR and Eurofins DiscoverX webinar card reading Live September 24, 11 AM ET / 8 AM PT.

ALT Dr. GPCR and Eurofins DiscoverX webinar card reading Live September 24, 11 AM ET / 8 AM PT.

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Two agonists can look alike in a sensitive assay and reverse in a less sensitive one. One runs on affinity, the other on efficacy. Terry Kenakin shows how volume control tells them apart. Sept 24, 11 AM ET / 8 AM PT. With @EurofinsDscvrx. ecosystem.drgpcr.com/gpcr-we… #DrGPCR #GPCR
Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

ALT Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

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A neutral antagonist may not be neutral. Turn the system up, induce constitutive activity, and latent inverse agonism shows up. Terry Kenakin on functional volume control. Live Sept 24, 11 AM ET / 8 AM PT. With @EurofinsDscvrx. ecosystem.drgpcr.com/gpcr-we… #DrGPCR #GPCR
Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

ALT Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

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Volume control happens in vivo too. β-receptor density in the heart falls as heart failure worsens, so the same agonist does less. Terry Kenakin on tuning system sensitivity, live Sept 24, 11 AM ET / 8 AM PT. With @EurofinsDscvrx. ecosystem.drgpcr.com/gpcr-we… #DrGPCR #GPCR
Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

ALT Dr. GPCR and Eurofins DiscoverX webinar card reading The molecule did not change. The sensitivity of the system did.

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A third of all approved drugs act on GPCRs, and every one began at a lab bench. Reliable reagents are where discovery quietly begins, or quietly breaks. Full story: ecosystem.drgpcr.com/post/wh… #GPCR #drgpcr
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"Doomed before you even shoot the rabbit." Why GPCRs punish antibody programs early: low abundance, buried epitopes, near-identical family sequences. Full story: ecosystem.drgpcr.com/post/wh… #GPCR #drgpcr
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Where is the line between an antagonist and a weak partial agonist? Evan O'Brien solved one molecule bound to the mu opioid receptor in both active and inactive states to find out. He presents at #DOT2026, our chat: ecosystem.drgpcr.com/post/gp… #DrGPCR #GPCR
Can One Molecule Be an Agonist and an Antagonist? Evan O'Brien, PhD, Johns Hopkins University.

ALT Can One Molecule Be an Agonist and an Antagonist? Evan O'Brien, PhD, Johns Hopkins University.

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GLP-1 strips fat, but muscle can go with it. Hailong Zhang's biased APJ agonist YJ-015 is built to help keep muscle while the weight drops. He presents at #DOT2026, and we spoke with him first: ecosystem.drgpcr.com/post/gp… #DrGPCR #GPCR
Keeping the Muscle When the Fat Comes Off. Hailong Zhang, PhD, Shanghai Yogar Therapeutics.

ALT Keeping the Muscle When the Fat Comes Off. Hailong Zhang, PhD, Shanghai Yogar Therapeutics.

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Unreliable antibodies do not just fail. They fail quietly, and cost months before anyone notices. Why honest characterization is the fix. Full story: ecosystem.drgpcr.com/post/wh… #GPCR #drgpcr
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It's live. Jane Lamerdin and Gaurav Agrawal of Eurofins DiscoverX on physiological relevance, the assays that refuse to work, and why GPCRs are back at the front of drug discovery. Watch: ecosystem.drgpcr.com/dr-gpcr… #GPCR #DrGPCR
Dr. GPCR Podcast cover card reading Physiological Relevance Is The Whole Game.

ALT Dr. GPCR Podcast cover card reading Physiological Relevance Is The Whole Game.

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Where and when a GPCR signals inside the cell: endomembrane signaling on endosomes and the Golgi, resolved one molecule at a time. @DavideCalebiro live this Thursday, 10 AM ET. Direct Q&A. ecosystem.drgpcr.com/gpcr-ma… #DrGPCR #GPCR #DrGPCRUniversity
Orange Dr. GPCR banner reading Signaling Follows Receptors Into Endosomes

ALT Orange Dr. GPCR banner reading Signaling Follows Receptors Into Endosomes

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Who really knows if a GPCR antibody works? Not the vendor, but the researchers who use it daily. Why GeneTex ships free vials and asks for the honest verdict. Full story: ecosystem.drgpcr.com/post/wh… #GPCR #drgpcr
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Being in a room where you can ask the person whose lab produced the data, and get an answer is fabulous. That, plus the full archive, the Intelligence Hub, jobs and the community. 14 days. $49, credited toward the year if you stay. ecosystem.drgpcr.com/trial #DrGPCR #GPCR
Orange Dr. GPCR banner reading A Professional Home In GPCR Science

ALT Orange Dr. GPCR banner reading A Professional Home In GPCR Science

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Most attrition in drug discovery happens after you have the compound, not at the target. That is the stretch Terry Kenakin's new #DOT2026 course, The End Game, is built around. Our preview chat: ecosystem.drgpcr.com/post/gp… #DrGPCR #GPCR
The Part of Drug Discovery Where Most Compounds Die. Dr. Terry Kenakin, UNC and Terry's Corner.

ALT The Part of Drug Discovery Where Most Compounds Die. Dr. Terry Kenakin, UNC and Terry's Corner.

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How do you find chemical matter for an orphan GPCR with no known function? Kris Borzilleri leads with binding, NMR and SPR against the receptor itself. She talks and teaches at #DOT2026, and she talked with us first: ecosystem.drgpcr.com/post/gp… #DrGPCR #GPCR
Finding Chemical Matter for a Receptor With No Known Function. Kris Borzilleri, Pfizer.

ALT Finding Chemical Matter for a Receptor With No Known Function. Kris Borzilleri, Pfizer.

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Bulk assays average over the receptors that matter. Single-molecule microscopy follows one at a time: their transient G protein interactions, signaling on internal membranes. @DavideCalebiro on how. Sept 10. ecosystem.drgpcr.com/gpcr-ma… #DrGPCR #GPCR #SingleMoleculeMicroscopy
Orange Dr. GPCR banner reading Bulk Assays Average It Away

ALT Orange Dr. GPCR banner reading Bulk Assays Average It Away

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