Mark Estacion, PhD

• Betsy Schulman
• Carolina Gomis Perez
• Mohammad-Reza Ghovanloo
• Peng Zhao
• Shujun Liu
• Stephen Waxman
• Sulayman Dib-Hajj
• Xiaoyang Cheng

Biophysics; Electrophysiology; Neurophysiology; Neurosciences; Physiology

• Kv7-specific activators hyperpolarize resting membrane potential and modulate human iPSC-derived sensory neuron excitabilityEstacion M, Liu S, Cheng X, Dib-Hajj S, Waxman S. Kv7-specific activators hyperpolarize resting membrane potential and modulate human iPSC-derived sensory neuron excitability. Frontiers In Pharmacology 2023, 14: 1138556. DOI: 10.3389/fphar.2023.1138556.
• Kv7-specific activators hyperpolarize resting membrane potential and modulate human iPSC-derived sensory neuron excitabilityEstacion M, Liu S, Cheng X, Dib-Hajj S, Waxman S. Kv7-specific activators hyperpolarize resting membrane potential and modulate human iPSC-derived sensory neuron excitability. Frontiers In Pharmacology 2023, 14: 1138556. PMID: 36923357, PMCID: PMC10008904, DOI: 10.3389/fphar.2023.1138556.
• A novel high throughput combined voltage-clamp/current-clamp analysis of single primary neuronsGhovanloo M, Tyagi S, Zhao P, Kiziltug E, Estacion M, Dib-Hajj S, Waxman S. A novel high throughput combined voltage-clamp/current-clamp analysis of single primary neurons. Biophysical Journal 2023, 122: 101a. DOI: 10.1016/j.bpj.2022.11.734.
• High-throughput combined voltage-clamp/current-clamp analysis of freshly isolated neuronsGhovanloo M, Tyagi S, Zhao P, Kiziltug E, Estacion M, Dib-Hajj S, Waxman S. High-throughput combined voltage-clamp/current-clamp analysis of freshly isolated neurons. Cell Reports Methods 2023, 3: 100385. PMID: 36814833, PMCID: PMC9939380, DOI: 10.1016/j.crmeth.2022.100385.
• Fibroblast growth factor homologous factor 2 attenuates excitability of DRG neuronsEffraim PR, Estacion M, Zhao P, Sosniak D, Waxman SG, Dib-Hajj SD. Fibroblast growth factor homologous factor 2 attenuates excitability of DRG neurons. Journal Of Neurophysiology 2022, 128: 1258-1266. PMID: 36222860, PMCID: PMC9909838, DOI: 10.1152/jn.00361.2022.
• Cannabigerol inhibits sodium conductance to reduce neuronal dorsal root ganglion excitabilityGhovanloo M, Estacion M, Zhao P, Dib-Hajj S, Waxman S. Cannabigerol inhibits sodium conductance to reduce neuronal dorsal root ganglion excitability. Biophysical Journal 2022, 121: 93a. DOI: 10.1016/j.bpj.2021.11.2240.
• Differential effect of lacosamide on Nav1.7 variants from responsive and non-responsive patients with small fibre neuropathyLabau JI, Estacion M, Tanaka BS, de Greef B, Hoeijmakers J, Geerts M, Gerrits MM, Smeets H, Faber CG, Merkies I, Lauria G, Dib-Hajj SD, Waxman SG. Differential effect of lacosamide on Nav1.7 variants from responsive and non-responsive patients with small fibre neuropathy. Brain 2020, 143: 771-782. PMID: 32011655, PMCID: PMC7089662, DOI: 10.1093/brain/awaa016.
• A 49-residue sequence motif in the C terminus of Nav1.9 regulates trafficking of the channel to the plasma membraneSizova D, Huang J, Akin E, Estacion M, Gomis-Perez C, Waxman S, Dib-Hajj S. A 49-residue sequence motif in the C terminus of Nav1.9 regulates trafficking of the channel to the plasma membrane. Journal Of Biological Chemistry 2020, 295: 1077-1090. DOI: 10.1016/s0021-9258(17)49917-0.
• NaV1.7 as a Pharmacogenomic Target for Pain: Moving Toward Precision MedicineYang Y, Mis MA, Estacion M, Dib-Hajj SD, Waxman SG. NaV1.7 as a Pharmacogenomic Target for Pain: Moving Toward Precision Medicine. Trends In Pharmacological Sciences 2018, 39: 258-275. PMID: 29370938, DOI: 10.1016/j.tips.2017.11.010.
• Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trialZakrzewska JM, Palmer J, Morisset V, Giblin GM, Obermann M, Ettlin DA, Cruccu G, Bendtsen L, Estacion M, Derjean D, Waxman SG, Layton G, Gunn K, Tate S, investigators S. Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trial. The Lancet Neurology 2017, 16: 291-300. PMID: 28216232, DOI: 10.1016/s1474-4422(17)30005-4.
• Nav1.7-A1632G Mutation from a Family with Inherited Erythromelalgia: Enhanced Firing of Dorsal Root Ganglia Neurons Evoked by Thermal StimuliYang Y, Huang J, Mis MA, Estacion M, Macala L, Shah P, Schulman BR, Horton DB, Dib-Hajj SD, Waxman SG. Nav1.7-A1632G Mutation from a Family with Inherited Erythromelalgia: Enhanced Firing of Dorsal Root Ganglia Neurons Evoked by Thermal Stimuli. Journal Of Neuroscience 2016, 36: 7511-7522. PMID: 27413160, PMCID: PMC6705539, DOI: 10.1523/jneurosci.0462-16.2016.
• Pharmacotherapy for Pain in a Family With Inherited Erythromelalgia Guided by Genomic Analysis and Functional ProfilingGeha P, Yang Y, Estacion M, Schulman BR, Tokuno H, Apkarian AV, Dib-Hajj SD, Waxman SG. Pharmacotherapy for Pain in a Family With Inherited Erythromelalgia Guided by Genomic Analysis and Functional Profiling. JAMA Neurology 2016, 73: 659. PMID: 27088781, DOI: 10.1001/jamaneurol.2016.0389.
• Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic ReleaseAlexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLOS ONE 2016, 11: e0152405. PMID: 27050761, PMCID: PMC4822888, DOI: 10.1371/journal.pone.0152405.
• Intra- and Interfamily Phenotypic Diversity in Pain Syndromes Associated with a Gain-of-Function Variant of NaV1.7Estación M, Han C, Choi JS, Hoeijmakers J, Lauria G, Drenth J, Gerrits MM, Dib-Hajj SD, Faber CG, Merkies I, Waxman SG. Intra- and Interfamily Phenotypic Diversity in Pain Syndromes Associated with a Gain-of-Function Variant of NaV1.7. Molecular Pain 2011, 7: 1744-8069-7-92. PMID: 22136189, PMCID: PMC3248882, DOI: 10.1186/1744-8069-7-92.
• Can robots patch‐clamp as well as humans? Characterization of a novel sodium channel mutationEstacion M, Choi JS, Eastman EM, Lin Z, Li Y, Tyrrell L, Yang Y, Dib‐Hajj S, Waxman SG. Can robots patch‐clamp as well as humans? Characterization of a novel sodium channel mutation. The Journal Of Physiology 2010, 588: 1915-1927. PMID: 20123784, PMCID: PMC2901980, DOI: 10.1113/jphysiol.2009.186114.
• A sodium channel mutation linked to epilepsy increases ramp and persistent current of Nav1.3 and induces hyperexcitability in hippocampal neuronsEstacion M, Gasser A, Dib-Hajj SD, Waxman SG. A sodium channel mutation linked to epilepsy increases ramp and persistent current of Nav1.3 and induces hyperexcitability in hippocampal neurons. Experimental Neurology 2010, 224: 362-368. PMID: 20420834, DOI: 10.1016/j.expneurol.2010.04.012.
• Maitotoxin converts the plasmalemmal Ca2+ pump into a Ca2+-permeable nonselective cation channelSinkins W, Estacion M, Prasad V, Goel M, Shull G, Kunze D, Schilling W. Maitotoxin converts the plasmalemmal Ca2+ pump into a Ca2+-permeable nonselective cation channel. American Journal Of Physiology - Cell Physiology 2009, 297: c1533-c1543. PMID: 19794142, PMCID: PMC2793065, DOI: 10.1152/ajpcell.00252.2009.
• NaV1.7 Gain-of-function Mutations As A Continuum: A1632E Displays Physiological Changes Associated With Erythromelalgia And Paroxysmal Extreme Pain Disorder Mutations And Produces Symptoms Of Both DisordersEstacion M, Dib-Hajj S, Benke P, Morsche R, Eastman E, Macala L, Drenth J, Waxman S. NaV1.7 Gain-of-function Mutations As A Continuum: A1632E Displays Physiological Changes Associated With Erythromelalgia And Paroxysmal Extreme Pain Disorder Mutations And Produces Symptoms Of Both Disorders. Biophysical Journal 2009, 96: 12a. DOI: 10.1016/j.bpj.2008.12.960.
• NaV1.7 Gain-of-Function Mutations as a Continuum: A1632E Displays Physiological Changes Associated with Erythromelalgia and Paroxysmal Extreme Pain Disorder Mutations and Produces Symptoms of Both DisordersEstacion M, Dib-Hajj SD, Benke PJ, Morsche R, Eastman EM, Macala LJ, Drenth JP, Waxman SG. NaV1.7 Gain-of-Function Mutations as a Continuum: A1632E Displays Physiological Changes Associated with Erythromelalgia and Paroxysmal Extreme Pain Disorder Mutations and Produces Symptoms of Both Disorders. Journal Of Neuroscience 2008, 28: 11079-11088. PMID: 18945915, PMCID: PMC6671384, DOI: 10.1523/jneurosci.3443-08.2008.
• Paroxysmal Extreme Pain Disorder M1627K Mutation in Human Nav1.7 Renders DRG Neurons HyperexcitableDib-Hajj SD, Estacion M, Jarecki BW, Tyrrell L, Fischer TZ, Lawden M, Cummins TR, Waxman SG. Paroxysmal Extreme Pain Disorder M1627K Mutation in Human Nav1.7 Renders DRG Neurons Hyperexcitable. Molecular Pain 2008, 4: 1744-8069-4-37. PMID: 18803825, PMCID: PMC2556659, DOI: 10.1186/1744-8069-4-37.
• Palytoxin-induced cell death cascade in bovine aortic endothelial cellsSchilling W, Snyder D, Sinkins W, Estacion M. Palytoxin-induced cell death cascade in bovine aortic endothelial cells. American Journal Of Physiology - Cell Physiology 2006, 291: c657-c667. PMID: 16672692, DOI: 10.1152/ajpcell.00063.2006.
• Identification and localization of TRPC channels in the rat kidneyGoel M, Sinkins W, Zuo C, Estacion M, Schilling W. Identification and localization of TRPC channels in the rat kidney. American Journal Of Physiology. Renal Physiology 2005, 290: f1241-f1252. PMID: 16303855, DOI: 10.1152/ajprenal.00376.2005.
• Association of immunophilins with mammalian TRPC channels. Vol. 279 (2004) 34521–34529Sinkins W, Goel M, Estacion M, Schilling W. Association of immunophilins with mammalian TRPC channels. Vol. 279 (2004) 34521–34529. Journal Of Biological Chemistry 2004, 279: 42350. DOI: 10.1016/s0021-9258(20)72708-0.
• Maitotoxin Induces Biphasic Interleukin-1β Secretion and Membrane Blebbing in Murine MacrophagesVerhoef P, Kertesy S, Estacion M, Schilling W, Dubyak G. Maitotoxin Induces Biphasic Interleukin-1β Secretion and Membrane Blebbing in Murine Macrophages. Molecular Pharmacology 2004, 66: 909-920. PMID: 15385641, DOI: 10.1124/mol.66.4.909.
• Association of Immunophilins with Mammalian TRPC Channels*Sinkins W, Goel M, Estacion M, Schilling W. Association of Immunophilins with Mammalian TRPC Channels*. Journal Of Biological Chemistry 2004, 279: 34521-34529. PMID: 15199065, DOI: 10.1074/jbc.m401156200.
• Maitotoxin-induced cell death cascade in bovine aortic endothelial cells: divalent cation specificity and selectivityWisnoskey B, Estacion M, Schilling W. Maitotoxin-induced cell death cascade in bovine aortic endothelial cells: divalent cation specificity and selectivity. American Journal Of Physiology - Cell Physiology 2004, 287: c345-c356. PMID: 15044153, DOI: 10.1152/ajpcell.00473.2003.
• Activation of Human TRPC6 Channels by Receptor Stimulation*Estacion M, Li S, Sinkins W, Gosling M, Bahra P, Poll C, Westwick J, Schilling W. Activation of Human TRPC6 Channels by Receptor Stimulation*. Journal Of Biological Chemistry 2004, 279: 22047-22056. PMID: 15023993, DOI: 10.1074/jbc.m402320200.
• P2X7 Receptor-Dependent Blebbing and the Activation of Rho-Effector Kinases, Caspases, and IL-1β ReleaseVerhoef P, Estacion M, Schilling W, Dubyak G. P2X7 Receptor-Dependent Blebbing and the Activation of Rho-Effector Kinases, Caspases, and IL-1β Release. The Journal Of Immunology 2003, 170: 5728-5738. PMID: 12759456, DOI: 10.4049/jimmunol.170.11.5728.
• Blockade of maitotoxin-induced endothelial cell lysis by glycine and l-alanineEstacion M, Weinberg J, Sinkins W, Schilling W. Blockade of maitotoxin-induced endothelial cell lysis by glycine and l-alanine. American Journal Of Physiology - Cell Physiology 2002, 284: c1006-c1020. PMID: 12477666, DOI: 10.1152/ajpcell.00258.2002.
• Blockade of maitotoxin-induced oncotic cell death reveals zeiosisEstacion M, Schilling W. Blockade of maitotoxin-induced oncotic cell death reveals zeiosis. BMC Physiology 2002, 2: 2. PMID: 11825342, PMCID: PMC65053, DOI: 10.1186/1472-6793-2-2.
• Regulation of Drosophila TRPL Channels by Immunophilin FKBP59*Goel M, Garcia R, Estacion M, Schilling W. Regulation of Drosophila TRPL Channels by Immunophilin FKBP59*. Journal Of Biological Chemistry 2001, 276: 38762-38773. PMID: 11514552, DOI: 10.1074/jbc.m104125200.
• Maitotoxin-induced membrane blebbing and cell death in bovine aortic endothelial cellsEstacion M, Schilling W. Maitotoxin-induced membrane blebbing and cell death in bovine aortic endothelial cells. BMC Physiology 2001, 1: 2. PMID: 11231888, PMCID: PMC32181, DOI: 10.1186/1472-6793-1-2.
• Regulation of Drosophila transient receptor potential‐like (TrpL) channels by phospholipase C‐dependent mechanismsEstacion M, Sinkins W, Schilling W. Regulation of Drosophila transient receptor potential‐like (TrpL) channels by phospholipase C‐dependent mechanisms. The Journal Of Physiology 2001, 530: 1-19. PMID: 11136854, PMCID: PMC2278390, DOI: 10.1111/j.1469-7793.2001.0001m.x.
• Ciguatera ToxinsEstacion M. Ciguatera Toxins. 2000, 103 DOI: 10.1201/9780203909539.ch22.
• Maitotoxin activates a nonselective cation channel and a P2Z/P2X7-like cytolytic pore in human skin fibroblastsSchilling W, Sinkins W, Estacion M. Maitotoxin activates a nonselective cation channel and a P2Z/P2X7-like cytolytic pore in human skin fibroblasts. American Journal Of Physiology 1999, 277: c755-c765. PMID: 10516106, DOI: 10.1152/ajpcell.1999.277.4.c755.
• Stimulation of Drosophila TrpL by capacitative Ca2+ entry.Estacion M, Sinkins W, Schilling W. Stimulation of Drosophila TrpL by capacitative Ca2+ entry. Biochemical Journal 1999, 341 ( Pt 1): 41-9. PMID: 10377243, PMCID: PMC1220328, DOI: 10.1042/0264-6021:3410041.
• Stimulation of Drosophila TrpL by capacitative Ca2+ entryESTACION M, SINKINS W, SCHILLING W. Stimulation of Drosophila TrpL by capacitative Ca2+ entry. Biochemical Journal 1999, 341: 41-49. DOI: 10.1042/bj3410041.
• Functional expression of TrpC1: a human homologue of the Drosophila Trp channelSINKINS W, ESTACION M, SCHILLING W. Functional expression of TrpC1: a human homologue of the Drosophila Trp channel. Biochemical Journal 1998, 331: 331-339. PMID: 9512497, PMCID: PMC1219356, DOI: 10.1042/bj3310331.
• PDGF-Stimulated Calcium Influx Changes During In Vitro Cell TransformationEstacion M, Mordan L. PDGF-Stimulated Calcium Influx Changes During In Vitro Cell Transformation. Cellular Signalling 1997, 9: 363-366. PMID: 9376215, DOI: 10.1016/s0898-6568(96)00184-2.
• Mutations Causing Achondroplasia and Thanatophoric Dysplasia Alter bFGF-Induced Calcium Signals in Human Diploid FibroblastsNguyen H, Estacion M, Gargus J. Mutations Causing Achondroplasia and Thanatophoric Dysplasia Alter bFGF-Induced Calcium Signals in Human Diploid Fibroblasts. Human Molecular Genetics 1997, 6: 681-688. PMID: 9158142, DOI: 10.1093/hmg/6.5.681.
• Calcium is permeable through a maitotoxin-activated nonselective cation channel in mouse L cellsEstacion M, Nguyen H, Gargus J. Calcium is permeable through a maitotoxin-activated nonselective cation channel in mouse L cells. American Journal Of Physiology 1996, 270: c1145-c1152. PMID: 8928742, DOI: 10.1152/ajpcell.1996.270.4.c1145.
• Ca2+ influx via T-type channels modulates PDGF-induced replication of mouse fibroblastsWang Z, Estacion M, Mordan L. Ca2+ influx via T-type channels modulates PDGF-induced replication of mouse fibroblasts. American Journal Of Physiology 1993, 265: c1239-c1246. PMID: 8238477, DOI: 10.1152/ajpcell.1993.265.5.c1239.
• Competence induction by PDGF requires sustained calcium influx by a mechanism distinct from storage-dependent calcium influxEstacion M, Mordan L. Competence induction by PDGF requires sustained calcium influx by a mechanism distinct from storage-dependent calcium influx. Cell Calcium 1993, 14: 439-454. PMID: 8395338, DOI: 10.1016/0143-4160(93)90003-o.
• Expression of voltage-gated calcium channels correlates with PDGF-stimulated calcium influx and depends upon cell density in C3H 10T12 mouse fibroblastsEstacion M, Mordan L. Expression of voltage-gated calcium channels correlates with PDGF-stimulated calcium influx and depends upon cell density in C3H 10T12 mouse fibroblasts. Cell Calcium 1993, 14: 161-171. PMID: 8384532, DOI: 10.1016/0143-4160(93)90085-k.
• Characterization of ion channels seen in subconfluent human dermal fibroblasts.Estacion M. Characterization of ion channels seen in subconfluent human dermal fibroblasts. The Journal Of Physiology 1991, 436: 579-601. PMID: 1712040, PMCID: PMC1181523, DOI: 10.1113/jphysiol.1991.sp018568.
• Acute electrophysiological responses of bradykinin‐stimulated human fibroblasts.Estacion M. Acute electrophysiological responses of bradykinin‐stimulated human fibroblasts. The Journal Of Physiology 1991, 436: 603-620. PMID: 1648132, PMCID: PMC1181524, DOI: 10.1113/jphysiol.1991.sp018569.
• Inhibition of voltage-dependent Na+ current in cell-fusion hybrids containing activated c-Ha-rasEstacion M. Inhibition of voltage-dependent Na+ current in cell-fusion hybrids containing activated c-Ha-ras. The Journal Of Membrane Biology 1990, 113: 169-175. PMID: 2157017, DOI: 10.1007/bf01872890.