2018
DOI: 10.3390/molecules23092094
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HCN Channels: New Therapeutic Targets for Pain Treatment

Abstract: Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are highly regulated proteins which respond to different cellular stimuli. The HCN currents (Ih) mediated by HCN1 and HCN2 drive the repetitive firing in nociceptive neurons. The role of HCN channels in pain has been widely investigated as targets for the development of new therapeutic drugs, but the comprehensive design of HCN channel modulators has been restricted due to the lack of crystallographic data. The three-dimensional structure of th… Show more

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Cited by 34 publications
(32 citation statements)
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References 152 publications
(277 reference statements)
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“…Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels drive the repetitive firing in nociceptive neurons, and thus play a crucial role in pace making activity [ 45 ]. To further underpin the mature phenotype of iDNs, expression of HCN1–4 was assessed on D26 iDNs and mouse sensory neurons.…”
Section: Resultsmentioning
confidence: 99%
“…Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels drive the repetitive firing in nociceptive neurons, and thus play a crucial role in pace making activity [ 45 ]. To further underpin the mature phenotype of iDNs, expression of HCN1–4 was assessed on D26 iDNs and mouse sensory neurons.…”
Section: Resultsmentioning
confidence: 99%
“…Nupr1 is known to form functional complexes with several transcriptional regulators, including estrogen receptors [51, 53]. Hcn1 (hyperpolarization activated cyclic nucleotide gated potassium channel 1) is being explored as a candidate target for pain treatment [54].…”
Section: Resultsmentioning
confidence: 99%
“…NEK2 (never in mitosis gene A-related kinase 2) promotes tumor development through the Wnt signaling pathway, and may be a potential target for cancer treatment ( Cappello et al, 2014 ; Wen et al, 2016 ; Tang et al, 2018 ). HCN2 (hyperpolarization-activated cyclic nucleotide-gated 2) plays an important role in neuronal excitability ( Wu et al, 2018 ; Ramírez et al, 2018 ), whereas its role in tumors is unclear. According to the existing literature, except for NEK2 the expression and prognostic significance of the NEIL3 , CDC25C, and HCN2 genes are still unknown in breast cancer.…”
Section: Discussionmentioning
confidence: 99%