7F61: Human histamine receptor H3R

Crystal structure of human histamine receptor H3R in complex with antagonist PF03654746. Determined by X-ray diffraction at 2.6 Å resolution. Released 26 Oct 2022.

Method: X-ray diffraction
Resolution: 2.6 Å
Organisms: Homo sapiens, Escherichia coli
Chains: 2
Atoms: 3,314
Mol. weight: 62.55 kDa
Ligands: CLR, 1IB
Released: 26 Oct 2022

Explore 7F61 in 3D Show helices and sheets RCSB PDB PDBe

Secondary structure: helices and β-sheets

7F61 contains 21 α-helices and 0 β-strands across 2 chains. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.

Chain A: 14 helices, 0 β-strands

Element	Residues	Length
α-helix	31-61	31
α-helix	63-65	3
α-helix	68-82	15
α-helix	83-87	5
α-helix	88-97	10
α-helix	103-137	35
α-helix	139-145	7
α-helix	149-177	29
α-helix	196-229	34
α-helix	235-240	6
α-helix	348-383	36
α-helix	391-415	25
α-helix	417-427	11
α-helix	429-431	3

Chain B: 7 helices, 0 β-strands

Element	Residues	Length
α-helix	2-19	18
α-helix	23-41	19
α-helix	46-48	3
α-helix	56-79	24
α-helix	84-97	14
α-helix	98-102	5
α-helix	103-105	3

Molecules and chains

Molecule	Chains	Type	Length	Organism	UniProt
Histamine H3 receptor	A	protein	407	Homo sapiens	Q9Y5N1 (AlphaFold model)
Soluble cytochrome b562	B	protein	147	Escherichia coli	P0ABE7 (AlphaFold model)

Sequence of entity 1 (A), FASTA

>7F61_1 Histamine H3 receptor (chains A)
RGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAF
CIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSKAFNIVLISYDRFLSVTRAVSYRAQQ
GDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLE
FFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGH
GEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKP
SASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHG
HCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLK

Sequence of entity 2 (B), FASTA

>7F61_2 Soluble cytochrome b562 (chains B)
MKTIIALSYIFCLVFADYKDDDDKHHHHHHHHHHENLYFQGADLEDNWETLNDNLKVIEK
ADNAAQVKDALTKMRAAALDAQKATPPKLEDKSPDSPEMKDFRHGFDILVGQIDDALKLA
NEGKVKEAQAAAEQLKTTRNAYIQKYL

Ligands and cofactors

ID	Name	Formula	Copies
CLR	Cholesterol	C27 H46 O	1
1IB	N-ethyl-3-fluoranyl-3-[3-fluoranyl-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-…	C18 H24 F2 N2 O	1

Primary citation

Structural basis for recognition of antihistamine drug by human histamine receptor. Peng, X., Yang, L., Liu, Z. et al. Nat Commun (2022) 13:6105-6105. DOI 10.1038/s41467-022-33880-y · PubMed

Other PDB entries of the same protein (UniProt Q9Y5N1 (AlphaFold model), which also has an AlphaFold model), best resolution first:

8YN5 2.7 Å, Cryo-EM structure of histamine H3 receptor in complex with histamine and Gi
8YUU 2.7 Å, Cryo-EM structure of the histamine-bound H3R-Gi complex
8YN6 2.77 Å, Cryo-EM structure of histamine H3 receptor in complex with imetit and Gi
8YN7 2.77 Å, Cryo-EM structure of histamine H3 receptor in complex with immethridine and miniGo
8YN8 2.77 Å, Cryo-EM structure of histamine H3 receptor in complex with proxyfan and miniGo
8YUV 3.0 Å, Cryo-EM structure of the immepip-bound H3R-Gi complex
9JEQ 3.05 Å, Cryo-EM structure of Histamine-bound Histamine receptor 3 H3R G protein complex

Browse structure collections

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