Structure-guided design of a peripherally restricted chemogenetic system Hye Jin Kang , Brian E Krumm

References: Jin, B. K., Odongo, S., Radwanska, M., & Magez, S. (2023).

detection, receptor activation initiates conformational changes, exposing an intracellular cavity (Kang Despite multifocal signaling, recent studies indicate that signaling occurs within a 100 nm range from high-resolution protein structures, illuminating side chain orientations and overall conformational states (Kang

associate with the active parathyroid hormone 1 receptor (PTH1R) in different complex configurations ("hanging

The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors.

However, the receptors that these medicines target have been described as the ‘low-hanging’ fruit, and There are approximately 800 human GPCRs in the superfamily, controlling a broad range of physiological Orion’s receptor antagonist analogs have demonstrated powerful efficacies across a range of animal models