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Get ready to stay up-to-date with the latest research, advancements, and news in the field. From the scientist’s view: a conversation with … Chris Tate AI is dreaming up drugs that no one has ever

surprising discovery that β-arrestin can bind GPCRs without receptor activation, to visualizing intermediate states the Symposia GPCR Publication Highlights     Arrestin recognizes GPCRs independently of the receptor state Triple Labeling Resolves a GPCR Intermediate State by Using Three-Color Single Molecule FRET .   A powerful three-color approach captures dynamic receptor states in real time. Whether you're decoding a hidden receptor state or hunting for the next orphan GPCR ligand, we're here

  ✅ Avoid costly errors:  Master vital models to confidently forecast outcomes, before it’s too late

☕ We are excited to announce our rescheduled Dr. GPCR Virtual Cafe session with Dr. Matthew E. on Friday, October 7th at 1 PM ET. Don't miss the chance to listen to his latest research on the field. It's a great opportunity to get warmed up for the upcoming Summit starting the next Monday. Get your ticket today on Eventbrite! ➡https://bit.ly/3CmntVn

September 2022 "Perception of threats is essential for survival. Previous findings suggest that parallel pathways independently relay innate threat signals from different sensory modalities to multiple brain areas, such as the midbrain and hypothalamus, for immediate avoidance. Yet little is known about whether and how multi-sensory innate threat cues are integrated and conveyed from each sensory modality to the amygdala, a critical brain area for threat perception and learning. Here, we report that neurons expressing calcitonin gene-related peptide (CGRP) in the parvocellular subparafascicular nucleus in the thalamus and external lateral parabrachial nucleus in the brainstem respond to multi-sensory threat cues from various sensory modalities and relay negative valence to the lateral and central amygdala, respectively. Both CGRP populations and their amygdala projections are required for multi-sensory threat perception and aversive memory formation. The identification of unified innate threat pathways may provide insights into developing therapeutic candidates for innate fear-related disorders." Read more at the source #DrGPCR #GPCR #IndustryNews

We've refreshed the schedule and can’t wait for you to join us on these new dates. New Course Dates: Principles of Pharmacology I :  October 3, 10, 17, 24 (four sessions) Principles Grab this chance to deepen your understanding of pharmacology and take your knowledge to the next level Take advantage of a 25% early bird discount for premium members! GPCR Event Spotlight    11th Adhesion GPCR Workshop    Location:  Mexico City Dates:  October 23-25,

February 2022 "InterAx Biotech AG and Boehringer Ingelheim take first steps towards collaborating to

Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and modulates intracellular binding partner is bound, in which case the receptor is only stabilized in an intermediate-active state

analyzes their significance in GPCR internalization dynamics, internalization routes, postinternalization fates

Our previous Markov State Model (MSM) analysis of molecular dynamics simulations of membrane-embedded

The conformational landscapes analyzed by Markov state models revealed that the overall conformation

Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris Insights into the Activation Mechanisms of 5-HT2A Receptors Investigating the Effect of GLU283 Protonation State

generation • Mid-term global expansion plans include drug discovery technology investments, licensing late-stage Chris Cargill appointed as President and Chief Executive Officer • Dr.

Read about the newest discoveries in GPCR research 🙌 Save the dates: November 2 - 4: We're sponsoring success Sosei and PharmEnable extend neurological disease drugs hunt Sosei Heptares’ President & CEO Chris SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 5 - 10, 2024

Save the dates: November 2 - 4: We're sponsoring the GPCR Retreat and would love to meet you there! USP34 as deubiquitinases that regulate GPCR-p38 MAPK signaling and distinct inflammatory responses State-dependent Topline Safety and Tolerability Data from Proof-of-Concept Studies Sosei Heptares’ President & CEO Chris SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 5 - 10, 2024

simulations of G protein-coupled receptor-ligand complexes: Impact of ligand type and receptor activation state Likewise, the relative importance of receptor activation state and ligand function differences have also This study compares performance when docking ligands of varied function into varied GPCR activation states , with higher accuracy expected when docking agonists into active state structures and inverse agonists or antagonists into inactive state structures.

This week's highlight includes congrats to Omolade Otun, Chris de Graaf, Cherine Bechara, et al. for We are pleased to announce the scheduled dates for our highly anticipated courses led by Dr. Pharmacology in Drug Discovery I - Techniques for Effective Lead Optimization of Candidate Molecules Dates of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate Selection Dates Take advantage of the chance to showcase your creativity by participating in the Logo Contest.

Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris Insights into the Activation Mechanisms of 5-HT2A Receptors Investigating the Effect of GLU283 Protonation State

INV-202, an Oral, Peripherally-acting CB1 Inverse Agonist, in Patients with Diabetic Kidney Disease Chris

receptor (β2AR; PDB ID: 2RH1); (B) A ligand-bound GPCR undergoes a conformational change to its active state Source: Kim J, Choi C. 2018 Feb;98:222-232. doi: 10.1016/j.biopha.2017.12.056 Azam S, Haque ME, Jakaria M, Jo SH, Kim IS, Choi Cells. 2020 Feb 23;9(2):506. doi: 10.3390/cells9020506   Kim J, Choi C.

Can the pharmaceutical industry reduce attrition rates? Manchanda Y, ElEid L, Oqua AI, Ramchunder Z, Choi J, Shchepinova MM, et al. Wan Q, Okashah N, Inoue A, Nehmé R, Carpenter B, Tate CG, et al. Carpenter B, Tate CG. García-Nafría J, Tate CG. Cryo-EM structures of GPCRs coupled to Gs, Gi and Go.

. ✅ Insight into Consequences:  How binding sites determine receptor state shifts, signaling outcomes  Why this knowledge reshapes dose–response interpretation and informs your pipeline’s next decision gate Orthosteric ligands preempt  natural signaling; they “take over” receptor behavior, forcing physiology safety margins, biased signaling, and combination therapy design, understanding which approach you’re taking By stabilizing certain receptor states over others, ligands literally remodel the energy landscape.

either as homodimers or heterodimers, with distinct conformations in both their inactive and active states ligands produce different signaling outcomes depending on the receptor conformation or dimerization state As a result, dimerized SecR receptors exhibit higher rates of G protein activation and release, improving Additionally, the dimeric state allows rotational movement of the receptor's extracellular domain (ECD Tate, New insights into GPCR coupling and dimerisation from cryo-EM structures.  

fail when protein stoichiometry shifts How two-stage GPCR binding creates “high” and “low” affinity states Take home message: interpret orthosteric binding data only after verifying that the biology behaved as True affinity requires correcting for occupancy state. The high-affinity state is undersupported, creating biphasic curves. ✅ Member-only pricing  — Preferred rates across Terry’s Corner and the broader Ecosystem Premium. 40

The Kinetic Edge You Can’t Afford to Ignore Steady state isn’t just about exposure anymore. When a compound’s off-rate is slower than its clearance, its biological effect outlives its plasma presence The on-rate/off-rate balance  matters: too tight, and penetration stalls; too loose, and efficacy dissipates The metrics shift: k_inact  (rate of inactivation) replaces static Ki values. k_inact/KI  becomes the Terry’s Corner: to build strategies that anticipate these collisions instead of reacting to them too late

Why Results Appear Too Late to Change the Outcome 👉 Most teams focus on results because results feel Tradeoffs have already been accepted. 👉 What looks like a performance gap late in the year is often This is why late-year analysis often leads to frustration instead of clarity. ✅ The real leverage never When does the year actually take shape ? Strong early decision-making starts with intention. 👉 Founders who take control of this phase do not

Some Nbs that have been use for GPCR research are: Nb80: This nanobody stabilized an active-state conformation activation and investigate the role of specific regions in the switching between different conformational states extracellular surface of the Rhodopsin receptor and stabilizes the photo-activated receptor in a ground-state-like G., Choi, H. J., Fung, J. J., Pardon, E., Casarosa, P., Chae, P. S., Devree, B. T., Rosenbaum, D. Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.

If you participated in our symposiums, please take a moment to complete this survey. GPCR University Save the date for our upcoming workshop, starting May 9th, 2024, featuring Dr.  Those on the waitlist will be notified first of the course dates, so hurry. Dr. Myers Squibb GPCR Events, Meetings, and Webinars March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 |

If you attended our 2023 Symposia, please take a moment to complete this survey. Dr. cellular signaling GPR101: Modeling a constitutively active receptor linked to X-linked acrogigantism State-dependent Biagon Officially Incorporated In The State Of Illinois Septerna divulges new TSHR antagonists for hyperthyroidism March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 |

and intracellular responses GPCR signaling is a complex process modulated by protein conformational states Probing GPCR and β-Arrestin conformational states: methods and implications The formation of functional complexes involving GPCRs and β-arrestins hinges on their specific conformational states, influenced protein and has evolved to achieve resolutions comparable to X-ray crystallography (García-Nafría, J., & Tate Understanding how specific active conformational states influence the interaction or dissociation of