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This week's highlight includes congrats to: Makaía M Papasergi-Scott, Peter Gmeiner, Brian K Kobilka, in a High Fat Diet-induced Mouse Model of Obesity GPCRs in Neuroscience Xanthurenic acid: A role in brain

Katharina Grotsch, Bryan L Roth, Valery V Fokin  et al. for their research on Virtual Screening of a Frizzleds act as dynamic pharmacological entities Marina Casiraghi, Robert J Lefkowitz, Peter Gmeiner, Brian K Kobilka et al. for their investigation on Molecular insights into G protein coupling specificity at

receptor (GPCR) pharmacogenomics Miles D Thompson , David Reiner-Link , Alessandro Berghella , Brinda K a Family A GPCR Jun Xu , Geng Chen , Haoqing Wang , Sheng Cao , Jie Heng , Xavier Deupi , Yang Du , Brian K Kobilka Red and far-red cleavable fluorescent dyes for self-labelling enzyme protein tagging and interrogation

Kent Kobilka and Robert Joseph Lefkowitz for their work on GPCR function.[62–66] Lefkowitz was able Later on, Kobilka joined in with Lefkowitz to identify the shared architecture of the β-adrenergic receptor with that of rhodopsin.[67] In 2011, Kobilka further contributed to the field by obtaining the first Brian K. Kobilka – Facts - NobelPrize.org. https://www.nobelprize.org/prizes/chemistry/2012/kobilka/facts/. 63

International journal of molecular sciences, 24(6), 5994. https://doi.org/10.3390/ijms24065994 Manglik, A., Kobilka S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R. K., Gellman, S. I., & Kobilka, B. K. (2011). I., Garcia, K. C., Wess, J., & Kobilka, B. K. (2013). D., & Palczewski, K. (2023).

K., & Jacobson, K. A. (2010). Structure-based discovery of A2A adenosine receptor ligands. M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. M. (2023). L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L. T. (2016).

A., Kobilka, B. K., Strader, D. J., Benovic, J. L., Dohlman, H. G., Frielle, T., Bolanowski, M. B., Panova, O., Hilger, D., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B. K., Hildebrand, P. W., & Skiniotis, G. (2023).

M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. M. (2023). K., Hoppe, N., Huang, X. P., Macdonald, C. B., Mehrota, E., Grimes, P.

Brian K. Shoichet, Dr. Luc Van Hijfte and Dr. Wendy Young.

agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang ,  Yongfeng Liu ,  Marion Lanier ,   Brian K Shoichet ,  Esther Martinborough ,  Jonathan F Fay ,  Can Cao ,   Bryan L Roth , et al. adenocarcinoma, β-blockers and antihistamines: A clinical trial is needed Jillian G Baker ,  Erica K

K., Selent, J., Hill, S. J., & Calebiro, D. (2023). M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K. C., von Zastrow, M., Inoue, A., & Kobilka, B. K. (2022). Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics.

Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild traumatic brain injury "Traumatic brain injury (TBI) is a leading cause of disability in the US.

.; Vemuri, K.; Pu, M.; Qu, L.; Han, G. (3), 750-762.e14. https://doi.org/10.1016/j.cell.2016.10.004 . (5)         Li, X.; Hua, T.; Vemuri, K. -H.; Wu, Y.; Wu, L.; Popov, P.; Benchama, O.; Zvonok, N.; Locke, K.; Qu, L.; Han, G. W.; Iyer, M. 382–389. https://doi.org/10.1021/acs.bioconjchem.7b00680 . (13)      Gazzi, T.; Brennecke, B.; Atz, K. .; Van Der Wel, T.; Mandhair, H.; Honer, M.; Fingerle, J.; Scheffel, J.; Broichhagen, J.; Gawrisch, K.

Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular

To validate that the developed assay is suitable for measuring the K i of different ligands, competition The Log(IC50) change in time was fitted with equation  3  and k given is the weighted average from 3  D.; Hanada, K.; Pagano, R. E.; Miller, L. J. -J.; Veiksina, S.; Kõlvart, K. R.; Min, M.; Kopanchuk, S.; Rinken, A. C.; Chen, K. H.; Bates, M.; Zhuang, X.

K., Das, A. K., Eds.; Elsevier, 2023; Vol. 103, pp 59–103. https://doi.org/10.1016/bs.coac.2023.02.005 .

and mastering drug binding kinetics is essential for pipeline efficiency: How fast a ligand binds (k₁ ) and how long it stays bound (k₂)  can alter therapeutic profiles dramatically, even if two candidates

Pharmaceuticals (Basel, Switzerland), 14(5), 439. https://doi.org/10.3390/ph14050439 Chen, K. K., Karnik, S. S., Hunyady, L., Luttrell, L. M., & Lefkowitz, R. J. (2003). C., Götz, K., Sungkaworn, T., Lohse, M. J., & Calebiro, D. (2016). I., & O'Malley, K. L. (2017). A., Sriram, K., Wiley, S.

However, GPCRs are not simple on-off switches (Rosenbaum, Rasmussen, and Kobilka 2009), since they are to the presence of both robust and less potent (partial) inverse agonism (Rosenbaum, Rasmussen, and Kobilka topographically distinct from (do not exhibit any overlap with) the orthosteric site (Rosenbaum, Rasmussen, and Kobilka

assays):  Displacement of specific radiolabeled ligands in CHO, HeLa, or HEK-293 cells, expressed as K References Kumar V, Chunchagatta Lakshman PK, Prasad TK, Manjunath K, Bairy S, Vasu AS, Ganavi B, Jasti

Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian

Bryan Roth and Brian Krumm for their study on Molecular glues as potential GPCR therapeutics Drs.

Structure-guided design of a peripherally restricted chemogenetic system Hye Jin Kang , Brian E Krumm , Adrien Tassou , Bryan L Roth , et al. 🕶 University CheatSheet is here!

Practical approaches to evaluating and optimizing brain exposure in early drug discovery. Schlander M, Hernandez-Villafuerte K, Cheng CY, Mestre-Ferrandiz J, Baumann M. Dave K, Gelman H, Thu CT, Guin D, Gruebele M. Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, et al. Truong ME, Bilekova S, Choksi SP, Li W, Bugaj LJ, Xu K, et al.

Bryan L Roth study on Illuminating the understudied GPCR-ome Save the dates: February 8 - 29: Dr. Research Transcriptome analysis of Schizothorax oconnori (Cypriniformes: Cyprinidae) oocytes: The role of K+

Lin S, Schorpp K, Rothenaigner I, Hadian K. Image-based high-content screening in drug discovery.

Brian Krumm and Bryan Roth studied CryoEM structures of adhesion in GPCR CD97, filling gaps.

essential for developing new treatments for these disorders and advancing our understanding of the brain K ´ onigstorfer, M. Mozhayeva, Y. Sara, T.C. Südhof, and ¨ E.T. Kavalali. 2001.

extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial respiration and Na+/K+