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Academic Journal

Science

4 Papers Indexed in Blossom

Published Papers

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AlphaFold2 structures guide prospective ligand discovery

Prospective docking of large libraries against unrefined AlphaFold2 (AF2) models of the σ2 and 5‑HT2A receptors yielded hit rates and affinities similar to those from experimental structures, and cryo‑EM of a potent 5‑HT2A ligand showed residue accommodations resembling the AF2 prediction. This demonstrates that AF2 models can sample alternative low‑energy conformations relevant for ligand discovery, extending the utility of structure‑based drug design.

Published
Journal
Science
Authors
Lyu, J., Kapolka, N., Gumpper, R., Alon, A., Wang, L., Jain, M. K., Barros-Álvarez, X., Sakamoto, K., Kim, Y., DiBerto, J., Kim, K., Glenn, I. S., Tummino, T. A., Huang, S., Irwin, J. J., Tarkhanova, O. O., Moroz, Y., Skiniotis, G., Kruse, A. C., Shoichet, B. K., Roth, B. L.
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Psychedelics promote neuroplasticity through the activation of intracellular 5-HT2A receptors

The study shows that psychedelics promote cortical neuroplasticity by selectively activating intracellular 5-HT2A receptors rather than surface receptors, explaining why serotonin does not elicit the same growth effects. This identifies location-biased 5-HT2A signalling as a therapeutic target and raises the possibility that serotonin may not be the endogenous ligand for intracellular 5-HT2ARs.

Published
Journal
Science
Authors
Vargas, M. V., Dunlap, L. E., Dong, C., Carter, S. J., Tombari, R. J., Jami, S. A., Cameron, L. P., Patel, S. D., Hennessey, J. J., Saeger, H. N., Mccorvy, J. D., Gray, J. A., Tian, L., Olson, D. E.
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Structure-based discovery of nonhallucinogenic psychedelic analogs

This cell and mice study (2022) presents structures of the serotonin receptor 5-HT2RA bound to psilocin, LSD, serotonin and the non-hallucinogenic analogue lisuride. The researchers were then able to design arrestin-biased ligands that displayed antidepressant-like activity in mice without hallucination effects. The research presented here provides a foundation for the design of safe and effective non-hallucinogenic psychedelic analogues.

Published
Journal
Science
Authors
Cao, D., Yu, J., Wang, H., Luo, Z., Liu, X., He, L., Qi, J., Fan, L., Tang, L., Chen, Z., Li, J., Cheng, J., Wang, S.
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Pyretogenic effect of lysergic acid diethylamide

This early (1954) animal study (n=9) investigated the pyrogenic (fever-inducing) properties of LSD (50μg/kg), which produced a rise in body temperature of normal rabbits, cats, and dogs. This rise in temperature which lasted up to 9 hours is antagonized by the administration of sodium pentobarbital but not by antipyrine or adrenergic blocking agents.

Published
Journal
Science
Authors
Horita, A., Dille, J. M.

Quick Facts

Papers Indexed
4
h-Index
1382
Open Access
No
Publisher
American Association for the Advancement of Science
Country
United States
Website
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