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TitleStructure-guided design of a peripherally restricted chemogenetic system.
Journal, issue, pagesCell, Vol. 187, Issue 26, Page 7433-7449.e20, Year 2024
Publish dateDec 26, 2024
AuthorsHye Jin Kang / Brian E Krumm / Adrien Tassou / Matan Geron / Jeffrey F DiBerto / Nicholas J Kapolka / Ryan H Gumpper / Kensuke Sakamoto / D Dewran Kocak / Reid H J Olsen / Xi-Ping Huang / Shicheng Zhang / Karen L Huang / Saheem A Zaidi / MyV T Nguyen / Min Jeong Jo / Vsevolod Katritch / Jonathan F Fay / Grégory Scherrer / Bryan L Roth /
PubMed AbstractDesigner receptors exclusively activated by designer drugs (DREADDs) are chemogenetic tools for remotely controlling cellular signaling, neural activity, behavior, and physiology. Using a structure- ...Designer receptors exclusively activated by designer drugs (DREADDs) are chemogenetic tools for remotely controlling cellular signaling, neural activity, behavior, and physiology. Using a structure-guided approach, we provide a peripherally restricted Gi-DREADD, hydroxycarboxylic acid receptor DREADD (HCAD), whose native receptor is minimally expressed in the brain, and a chemical actuator that does not cross the blood-brain barrier (BBB). This was accomplished by combined mutagenesis, analoging via an ultra-large make-on-demand library, structural determination of the designed DREADD receptor via cryoelectron microscopy (cryo-EM), and validation of HCAD function. Expression and activation of HCAD in dorsal root ganglion (DRG) neurons inhibit action potential (AP) firing and reduce both acute and tissue-injury-induced inflammatory pain. The HCAD chemogenetic system expands the possibilities for studying numerous peripheral systems with little adverse effects on the central nervous system (CNS). The structure-guided approach used to generate HCAD also has the potential to accelerate the development of emerging chemogenetic tools for basic and translational sciences.
External linksCell / PubMed:39631393 / PubMed Central
MethodsEM (single particle)
Resolution2.62 - 3.24 Å
Structure data

42538

8utd

EMDB-42538, PDB-8utd:
CryoEM Structure of HCA2-Gi1 in complex with MK-1903
Method: EM (single particle) / Resolution: 3.24 Å

42587

8uuj

EMDB-42587, PDB-8uuj:
CryoEM Structure of HCA2 DREADD Gi1 in complex with FCH-2296413
Method: EM (single particle) / Resolution: 2.62 Å

45616

9cib

EMDB-45616, PDB-9cib:
CryoEM Structure of HCA2 DREADD Gi1 in complex with FCH-2296413 (Local Refinement)
Method: EM (single particle) / Resolution: 2.62 Å

Chemicals


ChemComp, No image

ChemComp-XOT:
Unknown entry


ChemComp, No image

ChemComp-XI9:
Unknown entry

Source
  • homo sapiens (human)
  • lama glama (llama)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / GPCR / HCA2 / MK 1903 / DREADD

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