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TitleStructures of TRPV1 bound by hyperthermia-inducing analgesics.
Journal, issue, pagesCell Rep, Vol. 45, Issue 1, Page 116765, Year 2026
Publish dateJan 27, 2026
AuthorsYu-Hao Gao / Yi-Zhe Huang / Zhao-Xing Li / Xiao-Ying Chen / Chang-Yan Shao / Han-Wen Li / Bin Liu / Fán Yang / Mei-Rong Chen / Mei-Ling Lu / Michael X Zhu / Fan Yang / Yi-Bei Xiao / Ye Yu /
PubMed AbstractTRPV1, a member of the transient receptor potential vanilloid subfamily, mediates nociception and thermoregulation. TRPV1-targeting analgesics frequently induce hyperthermia, underscoring the need ...TRPV1, a member of the transient receptor potential vanilloid subfamily, mediates nociception and thermoregulation. TRPV1-targeting analgesics frequently induce hyperthermia, underscoring the need for structural insights to guide the development of safer compounds. Here, we determined the structures of rat TRPV1 bound to the clinical candidate analgesics AMG517, AMG9810, and SB366791. AMG517 and AMG9810 are deeply situated within the S3-S4 interface of the vanilloid pocket, where they interact with residues from the S3-S6 helices, as well as the S4-S5 linker. These interactions induce local deformations in the TRP-box and lower S6 helix, accompanied by a modest rotation of the S1-S4 bundle, leading to partial dilation of the lower gate. The distinct allosteric changes of AMG517 and AMG9810, compared with the non-hyperthermic ligand SB366791, suggest a structural basis by which TRPV1-targeting analgesics influence thermoregulation and provide insights for designing safer analogs.
External linksCell Rep / PubMed:41447532
MethodsEM (single particle)
Resolution2.7 - 3.25 Å
Structure data

65638

9w4m

EMDB-65638, PDB-9w4m:
ratTRPV1 bound with antagonist AMG517
Method: EM (single particle) / Resolution: 2.7 Å

65639

9w4n

EMDB-65639, PDB-9w4n:
Structure of rat TRPV1 in complex with SB-366791
Method: EM (single particle) / Resolution: 3.25 Å

65644

9w4t

EMDB-65644, PDB-9w4t:
ratTRPV1 bound with antagonist AMG9810
Method: EM (single particle) / Resolution: 2.87 Å

Chemicals

PDB-1d6r:
CRYSTAL STRUCTURE OF CANCER CHEMOPREVENTIVE BOWMAN-BIRK INHIBITOR IN TERNARY COMPLEX WITH BOVINE TRYPSIN AT 2.3 A RESOLUTION. STRUCTURAL BASIS OF JANUS-FACED SERINE PROTEASE INHIBITOR SPECIFICITY

ChemComp-NA:
Unknown entry

ChemComp-ZEI:
(2E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)prop-2-enamide

PDB-1d6w:
STRUCTURE OF THROMBIN COMPLEXED WITH SELECTIVE NON-ELECTROPHILIC INHIBITORS HAVING CYCLOHEXYL MOIETIES AT P1

Source
  • rattus norvegicus (Norway rat)
  • escherichia coli k-12 (bacteria)
KeywordsMEMBRANE PROTEIN / antagonist / complex / TRANSPORT PROTEIN / TRPV1 / protein complex

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