Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T30286 | Target Info | |||
| Target Name | Hyperpolarization cyclic nucleotide-gated channel 4 (HCN4) | ||||
| Synonyms | Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | HCN4 | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Cysteine Sulfenic Acid | Ligand Info | |||
| Canonical SMILES | C(C(C(=O)O)N)SO | ||||
| InChI | 1S/C3H7NO3S/c4-2(1-8-7)3(5)6/h2,7H,1,4H2,(H,5,6)/t2-/m0/s1 | ||||
| InChIKey | FXIRVRPOOYSARH-REOHCLBHSA-N | ||||
| PubChem Compound ID | 165339 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 3U11 Tetramerization dynamics of the C-terminus underlies isoform-specific cAMP-gating in HCN channels | ||||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [1] |
| PDB Sequence |
DSSRRQYQEK
530 YKQVEQYMSF540 HKLPPDTRQR550 IHDYYEHRYQ560 GKMFDEESIL570 GELSEPLREE 580 IINFNRKLVA591 SMPLFANADP601 NFVTSMLTKL611 RFEVFQPGDY621 IIREGTIGKK 631 MYFIQHGVVS641 VLTKGNKETK651 LADGSYFGEI661 CLLTRGRRTA671 SVRADTYCRL 681 YSLSVDNFNE691 VLEEYPMMRR701 AFETVALDRL711 DRIGKKN
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| PDB ID: 4NVP Structure of the cyclic nucleotide-binding domain of HCN4 channel complexed with 7-CH-cAMP | ||||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [2] |
| PDB Sequence |
SPMDSSRRQY
527 QEKYKQVEQY537 MSFHKLPPDT547 RQRIHDYYEH557 RYQGKMFDEE567 SILGELSEPL 577 REEIINFNRK588 LVASMPLFAN598 ADPNFVTSML608 TKLRFEVFQP618 GDYIIREGTI 628 GKKMYFIQHG638 VVSVLTKGNK648 ETKLADGSYF658 GEICLLTRGR668 RTASVRADTY 678 CRLYSLSVDN688 FNEVLEEYPM698 MRRAFETVAL708 DRLDRIGKKN718 |
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| PDB ID: 4KL1 HCN4 CNBD in complex with cGMP | ||||||
| Method | X-ray diffraction | Resolution | 2.70 Å | Mutation | No | [3] |
| PDB Sequence |
DSSRRQYQEK
530 YKQVEQYMSF540 HKLPPDTRQR550 IHDYYEHRYQ560 GKMFDEESIL570 GELSEPLREE 580 IINFNRKLVA591 SMPLFANADP601 NFVTSMLTKL611 RFEVFQPGDY621 IIREGTIGKK 631 MYFIQHGVVS641 VLTKGNKETK651 LADGSYFGEI661 CLLTRGRRTA671 SVRADTYCRL 681 YSLSVDNFNE691 VLEEYPMMRR701 AFETVALDRL711 DR
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Tetramerization dynamics of C-terminal domain underlies isoform-specific cAMP gating in hyperpolarization-activated cyclic nucleotide-gated channels. J Biol Chem. 2011 Dec 30;286(52):44811-20. | ||||
| REF 2 | Cyclic nucleotide mapping of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. ACS Chem Biol. 2014 May 16;9(5):1128-37. | ||||
| REF 3 | Cyclic dinucleotides bind the C-linker of HCN4 to control channel cAMP responsiveness. Nat Chem Biol. 2014 Jun;10(6):457-62. | ||||
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