Kimberly Gomez, Ulises Santiago, Tyler S Nelson, Heather N Allen, Aida Calderon-Rivera, Sara Hestehave, Erick J Rodríguez Palma, Yuan Zhou, Paz Duran, Santiago Loya-Lopez, Elaine Zhu, Upasana Kumar, Rory Shields, Eda Koseli, Bryan McKiver, Denise Giuvelis, Wanhong Zuo, Kufreobong E Inyang, Angie Dorame, Aude Chefdeville, Dongzhi Ran, Samantha Perez-Miller, Yi Lu, Xia Liu, Handoko, Paramjit S Arora, Marcel Patek, Aubin Moutal, May Khanna, Huijuan Hu, Geoffroy Laumet, Tamara King, Jing Wang, M Imad Damaj, Olga A Korczeniewska, Carlos J Camacho, Rajesh Khanna
Transmembrane Cav 2.2 (N-type) voltage-gated calcium channels are genetically and pharmacologically validated, clinically relevant pain targets. Clinical block of Cav 2.2 (e.g., with Prialt/Ziconotide) or indirect modulation [e.g., with gabapentinoids such as Gabapentin (GBP)] mitigates chronic pain but is encumbered by side effects and abuse liability. The cytosolic auxiliary subunit collapsin response mediator protein 2 (CRMP2) targets Cav 2.2 to the sensory neuron membrane and regulates their function via an intrinsically disordered motif...
November 21, 2023: Proceedings of the National Academy of Sciences of the United States of America