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Received β€” 24 June 2026 ⏭ SCI-TECH

Small-molecule modulation of Ξ²-arrestins

βœ‡Nature
By: Alem W. Kahsai Β· Natalia Pakharukova Β· Henry Y. Kwon Β· Kunal S. Shah Β· Caroline T. del Real Β· Bowie N. Shreiber Β· Jason G. Liang-Lin Β· Paul J. Shim Β· Mason A. Lee Β· Van A. Ngo Β· Allison M. Schwalb Β· Uyen Pham Β· Anand Chundi Β· Haoran Jiang Β· Emmanuel Flores-Espinoza Β· Samuel Liu Β· Preston C. Nibley Β· Dana K. Bassford Β· Hyunggu Hahn Β· Cal A. Kunzle Β· Brittany N. Thomas Β· Jihee Kim Β· Yang Zhou Β· Jialu Wang Β· Xingdong Zhang Β· Jeffrey S. Smith Β· Lindsay A. M. Rein Β· Alex R. B. Thomsen Β· Sudha K. Shenoy Β· Sudarshan Rajagopal Β· Lei Shi Β· Seungkirl Ahn Β· Howard A. Rockman Β· Ali Masoudi Β· Robert J. Lefkowitz
24 June 2026 at 01:00

Nature, Published online: 24 June 2026; doi:10.1038/s41586-026-10683-5

Integrated pharmacological, biochemical, biophysical and structural analyses of small-molecule Ξ²-arrestin inhibitors show how they block Ξ²-arrestin engagement with activated GPCRs, revealing their mechanism of action and uncovering a previously unrecognized allosteric regulatory site.
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