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Enrolled in Phase 1/2 “ELUCIDATE” Trial Assessing GTAEXS617 in Advanced Solid Tumours A Conversation with Murat Tunaboylu, Antiverse Co-Founder and CEO GPCR Events, Meetings, and Webinars ONCORNET2.0 Final Symposium

Deep mutational scanning (DMS) is a powerful method for studying the functional consequences of various DMS can be used to comprehensively assess the functional impact of mutations in a candidate protein, Deep mutational scanning: assessing protein function on a massive scale. Measuring the activity of protein variants on a large scale using deep mutational scanning. Predicting Drug Resistance Using Deep Mutational Scanning.

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz However, the underlying molecular mechanism of the enhanced sensitivity or toxicity of amitraz to mutated

September 2022 "Background Cancer driver genes are usually ranked by mutation frequency, which does not We hypothesize that driver strength is higher for genes preferentially mutated in patients with few driver mutations overall, because these few mutations should be strong enough to initiate cancer. Strength Index (DSI) and the Normalized Driver Strength Index (NDSI), the latter independent of gene mutation

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling We hypothesized that somatic mutations in tumor samples may not be enriched within a single gene but To test this possibility, we systematically aggregated somatic cancer mutations across class A GPCRs Phenotypic characterization suggests these mutations induce perturbation of G protein activation and/

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Seventeen FSHR mutations described in patients with reproductive dysfunction were expressed in HEK 293T These findings aid in advancing the understanding of the effects of genetic mutations on GPCR function

You’ll get a framework to predict duration, penetration, and PK/PD separation—so decisions move faster define “irreversible” in real systems, anticipate PK/PD separation, and use target turnover to tune duration It’s an operating system for discovery decisions, featuring practical frameworks, trusted curations, The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, and on-demand scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need fast, curated

Get curated content at your own pace.   Subscribe to The Kenakin Brief below to stay in the know. this week:  – Phosphorylation’s selective role in β-arrestin recruitment across class B1 GPCRs  – GPCR mutations GPCR mutations in cancer   show both driver-like patterns and high redundancy, prompting a call for multiomics

GPCR Premium: Sneak Peek Here’s a curated, high-signal preview of what Premium Members get this week—no week —NIH’s new GPCR biosensor push, a leadership shift at Septerna, and a bold thesis on stabilizing mutated GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, on-demand scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need fast, curated

Breakthroughs this week: Eli Lilly cuts Zepbound prices; GNAI1 missense mutation study; rapid Gαs endosomal Must-read publications:  Gαi1 neurodevelopmental mutation; Gαs endosomal signaling; primary cilia as Members access deep-dive lectures, expert frameworks, curated jobs, upcoming events, and classified more

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It’s a curated lens—just enough signal to guide your week, with the full depth available inside. pharmacology—Protein Expression, Drug Discovery Scientist, and Staff Scientist in Molecular Pharmacology—curated GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week The complete Weekly News digest, curated jobs and upcoming events, must-read GPCR publications, exclusive scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need fast, curated

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This week we’ve curated 20 GPCR papers, 3 new events, 9 industry news, and 3 job opportunities! Matthew T Eddy and his team's research on A2A adenosine receptor activation by G protein and mutations visualization of human A2A adenosine receptor activation by a G protein and constitutively activating mutations

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Plus: new research on CaSR, leptin signaling, and inflammation-linked GPCRs — and curated roles in computational GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive GPCR scientists, translational pharmacologists, discovery teams, and decision-makers who need fast, curated

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September 2022 "Over 100 mutations in the rhodopsin gene have been linked to a spectrum of retinopathies most of these variants exhibit a loss of function, the molecular defects caused by these underlying mutations In this work, we utilize deep mutational scanning to quantitatively compare the plasma membrane expression However, the magnitude of the response to this molecule varies considerably across this spectrum of mutations

This week's Premium content offers a curated look at what's moving the industry and scientific community GPCR Premium Membership delivers curated, noise-free intelligence every week: deep-dive expert lectures The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated

form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism and anosmia, is due to mutations activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations modulatory activity, although data from GST pull-down (glutathione-S-transferase) and analysis of the N267K mutation

bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic diabetes insipidus "Loss-of-function mutations Recent studies showed that some AVPR2 mutations could cause biased Gαq/11 protein coupling rather than give insights into the relationship between the conformational change of the receptor because of the mutation

interactions between VFT units and HH bundles, and the impacts of heterozygous or homozygous inactivating mutations Transfected HEK-293 cells were assessed for Ca2+o -stimulated Ca2+i mobilization using mutations in either When the same mutation was present in both VFT domains of receptor dimers, analogous to homozygous neonatal insufficient for maximal signaling and there was no functional difference between heterodimers in which the mutation

Through an in-depth mutational analysis of β2AR, the researchers identified specific residues that influence that residues critical for β2AR function are under intense selective pressure, while others are more mutation-tolerant Deep mutational scanning, for instance, is gaining popularity as a strategy due to its ability to comprehensively

Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just activation Methods & Updates in GPCR Research A combination treatment based on drug repurposing demonstrates mutation-agnostic