February-2022

Dr. GPCR Ecosystem   -   Newsletter   -   February 2022

  

---

Meet Dr. GPCR Media Partner

---

  

    

Hello Readers,

This month we celebrate the second anniversary of the Dr. GPCR Podcast. Two years ago this month, we were recording the first episodes with Dr. Paul Insel and Dr. Terry Hebert.  This was the beginning of a new adventure that turned out to be life-altering for us. And for that, we have our guests and you, our supporters, to thank. 

We will have exciting news to share in the upcoming weeks which will bring the GPCR community closer than ever! Stay tuned!

While we put the finishing touches on our brand new surprise for you, let's dive into this month's news:
 

• Dr. GPCR at the GPCR-Targeted Drug Discovery Summit 2022: Now running digital between March 22nd and 24th. Register today and join us!
  
   View the full program and register here and don't forget to use coupon code DRGPCR10 to obtain a 10% discount.
   
• Dr. GPCR at the 6th ERNEST meeting: Join us and be the first to hear about our exciting news that will change the face of the GPCR community. Mark your calendars for the upcoming ERNEST meeting held between March 28th and 31st on Zoom and Wonder.
   
• Dr. GPCR at the Great Lakes GPCR Retreat: Come meet our team in person and hear fantastic GPCR talks between May 12-14, 2022 in Niagra on the Lake, Canada.
   
• Dr. GPCR Virtual Cafe: This week at the Virtual Cafe Dr. Ben Myers is our guest. Mark your calendar for February 24th, 2022 at 11 am EST. Get your tickets today! 
  
  Next month, we'll have Dr. Adriano Marchese as our guest at the Virtual Cafe.

 

• Dr. GPCR Podcast:  More fantastic episodes coming your way including from Dr. Antony Boucard, Dr. Graham Ladds, and Dylan Eiger. 
  
  Are you going to be our next podcast guest?
  
  Scientists at all levels are welcome! Schedule your podcast episode recording here

 

• Dr. GPCR Membership contribution. Some of you may have seen the GPCR focused beautiful pieces of art on social media. Thank you to artists and scientists Chahat Soni and 
  Jagannath Maharana both graduate students at the Indian Institute of Technology, Kanpur, for sharing their art.
   
• Dr. GPCR Summit Survey:  Mark your calendar, the 3rd edition of the Dr. GPCR Summit will be held between October 10th and 16th. Help us organize the next Dr. GPCR Summit 2022 for you! Please take a moment to fill out the Summit Survey today!
  
  The 2021 Summit talks are now available to view on our YouTube Channel. Don't forget to subscribe!
   

• Dr. GPCR Testimonials: We'd love to hear from you. Let us know how you think Dr. GPCR has affected you and the field today. 

   

1. Interesting papers published in January 2022
  

1.1 Receptor activation and signaling

• Biased Ligands at the Kappa Opioid Receptor: Fine-Tuning Receptor Pharmacology.

• Scaffolding of Mitogen-Activated Protein Kinase Signaling by β-Arrestins.

• In Vivo Metabolic Roles of G Proteins of the Gi Family Studied With Novel Mouse Models.

• Computational characterization of transducer recognition of β2 adrenergic receptor. 

• Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors.

• Angiotensin II Type 1 Receptor Tachyphylaxis Is Defined by Agonist Residence Time.

• Distinct Binding Mechanisms for Allosteric Sodium Ion in Cannabinoid Receptors.

• GqPCR-stimulated dephosphorylation of AKT is induced by an IGBP1-mediated PP2A switch.

• Selective Interactions of Mouse Melanocortin Receptor Accessory Proteins with Somatostatin Receptors.

• A Model for the Signal Initiation Complex Between Arrestin-3 and the Src Family Kinase Fgr.

• Differential voltage-dependent modulation of the ACh-gated K+ current by adenosine and acetylcholine.

• In vivo metabolic effects after acute activation of skeletal muscle Gs signaling.

• A network of Gαi signaling partners is revealed by proximity labeling proteomics analysis and includes PDZ-RhoGEF.

• GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation.

• Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias.
   

1.2 Structural and molecular insights into GPCR function

• Specific motifs mediate post-synaptic and surface transport of G protein-coupled receptors.

• Molecular mechanism of agonism and inverse agonism in ghrelin receptor.

• Atypical structural snapshots of human cytomegalovirus GPCR interactions with host G proteins.

• Molecular determinants of GPCR pharmacogenetics: Deconstructing the population variants in β2-adrenergic receptor.

• A single chemosensory GPCR is required for a concentration-dependent behavioral switching in C. elegans.

• Structural insights into MRGPRX2: a new vision of itch and allergy.

  

1.3 GPCRs in Oncology and Immunology

• The Role of Neuropeptide-Stimulated cAMP-EPACs Signalling in Cancer Cells.

• The emerging roles of Gα12/13 proteins on the hallmarks of cancer in solid tumors.

• The α-Arrestin ARRDC3 Is an Emerging Multifunctional Adaptor Protein in Cancer.

• P17 induces chemotaxis and differentiation of monocytes via MRGPRX2-mediated mast cell-line activation.

• Cross-Talk of Cholinergic and β-Adrenergic Receptor Signalling in Chronic Myeloid Leukemia K562 Cells.
   

1.4 GPCRs in Cardiology & Endocrinology 

• The relevance of adhesion G protein-coupled receptors in metabolic functions.

• The regulation of PKA signaling in obesity and in the maintenance of metabolic health.

• Antibodies against Angiotensin II Type 1 and Endothelin 1 Type A Receptors in Cardiovascular Pathologies.

• Intestinal Gpr17 deficiency improves glucose metabolism by promoting GLP-1 secretion.

• Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gastrointestinal motility disorders.

• Association of autoantibodies to muscarinic acetylcholine receptors with gastrointestinal symptoms and disease severity in patients with postural orthostatic tachycardia syndrome.
   

1.5 GPCRs in Neuroscience

• RTN4/NoGo-receptor binding to BAI adhesion-GPCRs regulates neuronal development

• Relationships between constitutive and acute gene regulation, and physiological and behavioral responses, mediated by the neuropeptide PACAP.

• Latrophilin-1 drives neuron morphogenesis and shapes chemo- and mechanosensation-dependent behavior in C. elegans via a trans function.

• Mu opioid receptors acutely regulate adenosine signaling in striatal glutamate afferents.
   

1.6 Methods & Updates in GPCR Research

• Development of enhanced conformational sampling methods to probe the activation landscape of GPCRs.

• Identification and characterization of G protein-coupled receptors in Spodoptera frugiperda (Insecta: Lepidoptera).

• Enabling QTY Server for Designing Water-Soluble α-Helical Transmembrane Proteins.

• GPCR-FEX: A Fluoride-Based Selection System for Rapid GPCR Screening and Engineering.

• Binding site identification of G protein-coupled receptors through a 3D Zernike polynomials-based method: application to C. elegans olfactory receptors.
   

1.7 GPCR Binders, Drugs, and More

•  ​​Disrupting GPCR Complexes with Smart Drug-like Peptides.

• Lipopeptide Pepducins as Therapeutic Agents.

• GABAB Receptor Chemistry and Pharmacology: Agonists, Antagonists, and Allosteric Modulators.

• Structural Characterization of KOR Inactive and Active States for 3D Pharmacology and Drug Discovery.

• Targeting Gαi/s Proteins with Peptidyl Nucleotide Exchange Modulators.

• Identification of G protein-coupled receptor 55 (GPR55) as a target of curcumin.

• In Silico Prediction and Validation of CB2 Allosteric Binding Sites to Aid the Design of Allosteric Modulators.

• Inhibitors of protease activated receptor 4 (PAR4): a review of recent patents (2013-2021).
   

1.8 Reviews

• Novel advances in understanding fatty acid-binding G protein-coupled receptors and their roles in controlling energy balance.

• Structural perspective of class B1 GPCR signaling.

• Arrestin-dependent internalization of rhodopsin-like G protein-coupled receptors.
   

2. Industry news

• Septerna emerges with $100M to use allosterism as a means to drug target GPCRs with Bob Lefkowitz, Patrick Sexton, and Arthur Christopoulos as co-founders

• ShouTi Introduces Basecamp Bio as a Wholly Owned Subsidiary to Expand Pipeline and Partnerships

• AELIS PHARMA launches their IPO for €25 million

• InterAx Biotech AG and Boehringer Ingelheim take collaborate to unlock orphan targets leveraging InterAx AI-driven discovery platform.

• Sosei Heptares reported its FY2021 financial results and provided an update on operational activities

• Ermium Therapeutics has constituted its SAB

• Carola Weiss has joined InterAx Biotech as VP Business Development

• Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner Jiangsu Nhwa Pharmaceutical
   

3- Meetings and webinars

• 8th Fragment-Based Drug Discovery meeting in Cambridge will be held from March 27th-29th 2022, UK.

• Keystone Symposia in-person meeting- GPCRs: An Odyssey from Structure, Signaling, and Regulation to Therapeutics joint with Micropeptides: Biogenesis and Function, April 6-9, 2022 

• 4GPCRnet - International Symposium  in Leipzig, Germany. September 26-29, 2022 

• GPCRs in Medicinal Chemistry in Verona, Italy, from October 5th to 7th, 2022

 
4. Resources

• TeachOpenCADD - A teaching platform for computer-aided drug design

   
    

---

Meet Dr. GPCR Media Partners