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Juan Jose Fung, Principal Scientist, at GPCR Therapeutics.

foundational lesson from Terry Kenakin’s Pharmacology Vault , we unlock the visual language of pharmacology: dose-response In classic Terry style, the lecture walks you through: What dose-response curves are and why they’re 👉 Discover why dose-response curves are the backbone of all pharmacology. Unlock "Dose-Response Curves" now

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture of fungi by macrophages "The fungal pathogen Histoplasma capsulatum (Hc) invades, replicates within, and destroys and release of small peptide fragments such as C3a, a role for C3aR in macrophage interactions with fungi phagocytosis of bacteria and latex beads, it is critical for optimal macrophage capture of pathogenic fungi Hc-macrophage interactions and uncover a novel and specific role for C3aR in macrophage recognition of fungi

.- Jan Steyaert, scientific director of the VIB-VUB Center for Structural Biology, Vlaams Instituut Biotechnologie Jan Steyaert will be presented with the Gabbay Award at Brandeis University on October 27 when he will

March 2022 Inversago Pharma Announces Dosing of First Participant with Metabolic Syndrome in Phase 1B clinical stage biotech company with a unique portfolio of CB1 inverse agonists, announced today the dosing

Why Misreading Antagonism Delays GPCR Drug Discovery If a dose-response curve shifts to the right, you How do the binding kinetics  of an antagonist influence what we actually observe in a dose-response experiment Consider this: Two dose-response curves, side by side.

March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment medicines targeting G-protein coupled receptors (GPCRs), today announced that the first subjects have been dosed

March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers.

However, blind assessments of ligand pose quality and affinity prediction have thus far not provided Median ligand RMSD values for top-scored poses were 1.2 Å and 2.0 Å for self-docking and StateMatch/FunctionMatch

promoted to partner at Third Rock Ventures as the firm raised just over $600 million for its fourth fund Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far That money has gone to some 60 biotechs, much of it as early funding."

That choice determines whether you risk over- or under-dosing, miss safety windows, or miss therapeutic shifts, signaling outcomes, and efficacy profiles. ✅ Practical Perspective:  Why this knowledge reshapes dose–response is not just cleaner assay design but a sharper decision framework for selecting, prioritizing, and dosing Translational Relevance: From Bench to Clinic Misjudging orthosteric vs allosteric behavior can derail dose Recognizing how your ligand interacts with the receptor lets you predict safety margins, dose–response

Funding models rewarded independence, not shared resources. The Power of GPCR Collaboration: Funding as a Force Multiplier Collaboration sounds warm and fuzzy. Shared funding gave us leverage. This changed not just what got funded, but what was possible . What mattered was how leadership leveraged luck into durable structure  — through funding strategies,

In a LPS-induced lung inflammation model in mice, ACT-660602 led to significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment when administered orally at a dose

Solubility poses significant challenges. of adjustments, a scientist on his team presented a data set that transformed everything: a clean, dose-dependent The biological validation came from Jean-Philippe Pin’s group at the Genomic Functional Institute in

“We did a full dose-response and saw antagonism—all in one plate-based assay. layered collaborations—with Durham University chemist David Parker on the probe chemistry, and with Jean-Philippe

Their “aha” moment came when they ran a dose-response with Exendin-4 on GLP-1 receptors—and saw clean → Discovery of pH-sensitive dual response (brightness + lifetime) → Application to GPCR models with Jean-Philippe The fun is what you do with the other 10%. 🎯 From Launch to Legacy For Dr.

discovery teams, this means a shorter exposure can yield longer efficacy windows—opening doors to lower dosing Dose prediction models need kinetic nuance—not just Cmax and AUC. For teams running early-stage programs, recognizing this decoupling early can sharpen dose optimization Dosing regimens aligned with biology, not just exposure.

It quantifies the degree of agonist blockade using dose ratios . analysis turns receptor pharmacology into detective work, spotlighting mechanistic fingerprints buried in dose–response Derive dose ratios  from those sections only.

In addition, Structure Therapeutics has completed dosing in a single ascending dose (SAD) Phase 1 study

is designing covalent or tight-binding candidates, these principles reduce surprises and accelerate dose missteps by: Preventing kinetic traps —spot PK/PD decoupling early so washouts and C_max don’t mislead dosing

of max in calcium assays to rapidly rank offset rates, and predict in vivo coverage before you ever dose Suddenly, at higher doses, you see an exaggerated ‘bang’ of effect.

ORs are highly expressed by olfactory sensory neurons of the nose where they are activated by different analyses, have indicated that OR genes are also expressed in non-olfactory tissues including the testis, lung epithelial cells proliferation via activation by β-ionone which initiates prostate cancer cell cycle arrest (Jones In non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and

bioinformatics analysis to construct a risk model for ovarian cancer prognosis GprC of the nematode-trapping fungus Arthrobotrys flagrans activates mitochondria and reprograms fungal cells for nematode hunting Role and Biophysicists decipher functionality of adrenaline-binding receptor Tectonic plates more than $130m in new funding

June 2022 "Published on juin 22, 2022 On June 22, 2022, Michel Bouvier, Chief Executive Officer of IRIC

development, today announced that it has entered into a definitive agreement with Armistice Master Fund Additionally, Addex has agreed to issue to Armistice Capital unregistered pre-funded warrants to purchase up to 11,700,000 shares in the form of 1,950,000 ADSs (the “Unregistered Pre-Funded Warrants”) at a funded amount of $1.69 with $0.01 payable on exercise as well as unregistered warrants to purchase up in the form of 2,500,000 ADSs (the “Unregistered Warrants” and together with the “Unregistered Pre-Funded

This week in Terry’s Corner , we go beyond the dose-response curves to explore the kinetic and pharmacologic Bridge science and strategy:  Ensure data and decision-making align with funding and milestones.

cortisol excretion in the presence of sustained, disease-like ACTH concentrations in multiple-ascending dose

9,230,772 shares in the form of 1,538,462 ADSs (the “Unregistered Warrants”), as well as unregistered pre-funded warrants to purchase up to 5,478,570 shares in the form of 913,095 ADSs (the “Unregistered Pre-Funded The Unregistered Pre-Funded Warrants have been funded to the amount of $6.49 with $0.01 payable on exercise

1984 (Cerione et al. 1984), where reconstitution of purified β2-adrenergic receptors from guinea pig lung of adjustability in terms of pharmacological effects, allowing for the administration of substantial doses

Complex in Stress and Anxiety Disorders GPCRs in Oncology and Immunology Exacerbating effects of single-dose by the American College of Clinical Pharmacology Sosei and Cancer Research UK announce first patient dosed