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signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T receptor in intestinal stem cells to exacerbate colitis The EBI2 receptor is coexpressed with CCR5 in CD4+ T

Kenakin, T. (2019). Biased receptor signaling in drug discovery. Sugiura, R., Satoh, R., & Takasaki, T. (2021). ERK: a double-edged sword in cancer.

In CD8 + T cells, the chemokines promote unique transcriptional responses predicted to regulate inflammatory

but they also suppress the pro-inflammatory interleukin-17A+ population in TH 17-differentiated CD4+ T

Non-specific binding (NS, open symbols) was determined in the presence and total binding (T, filled symbols Scientific Reports . (16)      Laasfeld, T.; Ehrminger, R.; Tahk, M.-J.; Veiksina, S.; Kõlvart, K. -J.; Kopanchuk, S.; Laasfeld, T.; Weinhart, M.; Schollmeyer, D.; Betschart, M. T.; Vaughan, J. C.; Chen, K. H.; Bates, M.; Zhuang, X. T.; Schwille, P.; Jungmann, R.

al. for their fantastic work on Germline mutations in a G protein identify signaling cross-talk in T position GPCR Activation and Signaling Germline mutations in a G protein identify signaling cross-talk in T

Oliver Hartley, was at the PEGS Europe Novartis pays Legend $100M upfront to give solid tumor CAR-T the T-Charge treatment Innovation And Healthcare Meet At Novartis Neurocrine Biosciences Announces Settlement

Long-Term Outcomes in Patients With Multiple Myeloma and Lymphoma Undergoing Chimeric Antigen Receptor T-Cell RNAi library screening reveals Gβ1, Casein Kinase 2 and ICAP-1 as novel regulators of LFA-1-mediated T

without operational structure ✅ Scattered data = missed insights = wasted time ✅ You can’t fail fas t

T., Rosenbaum, D. M., Thian, F. S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R.

Butlen-Ducuing F, Pétavy F, Guizzaro L, Zienowicz M, Salmonson T, Haas M, et al. Kenakin T. The mass action equation in pharmacology. Kenakin T. Biased Receptor Signaling in Drug Discovery. Pearce A, Redfern-Nichols T, Wills E, Rosa M, Manulak I, Sisk C, et al. Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, et al.

mutant-as-the-basis-for-personalized-high-throughput-drug-screening References Grimes, J., Koszegi, Z., Lanoiselée, Y., Miljus, T. L., Stepniewski, T.

you with the kinetic models and biological context needed to design drugs that actually work where it matters But as Kenakin shows, t½ is a surface metric —a combination of clearance and volume of distribution.

Results and Discussion The TR-FRET assay performed in living HEK-293 T cells expressing CB1R using CELT

distinct GPCR phosphorylation patterns, which influence their conformational states and functions (Matthees between GPCRs and β-arrestins, paving the way for capturing challenging protein complexes (Böttke, T. role in determining the formation of protein complexes and their functions within specific tissues (Matthees

GI tract OR ligands drive an intracellular cascade that results in enhanced serotonin release (Braun T. The chimeric antigen receptor T cell therapy could also be a way to target tumor cells expressing ectopic

T. & Gainetdinov, R. R. Physiological roles of G protein-coupled receptor kinases and arrestins.

This week's highlight includes congrats to Edda Matthees, Drs. 

receptors induces IFN-γ but suppresses IL-2 production by inhibiting activation of pAKT pathways in primary T

GPCRs in Oncology and Immunology A GPCR checkpoint drives CD8+ T cell dysfunction and immunotherapy failure

GPCRs in Immunology and Oncology The GPCR–Gαs–PKA signaling axis promotes T cell dysfunction and cancer

hedgehog pathway repression in tissue morphogenesis TIPE proteins control directed migration of human T

Malignancy Bispecific antibodies targeting BCMA or GPRC5D are highly effective in relapsed myeloma after CAR T-cell

G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. E., Mumford, R.

Kenakin, T. and A.

for the treatment of mycosis fungoides or Sézary syndrome in adults which are subtypes of cutaneous T-cell

advantages: it is usually very robust, good yields, reagents are found in most chem labs (like HATU, HoBT, EDCI

T. Gilliland et. al 2013).

authors set out to investigate GalNAc-Ts candidates involved in CCR5 O-glycosylation with CHO GalNAc-T

Sridharan R, Zuber J, Connelly SM, Mathew E, Dumont ME.