A “Target Class” Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels

SLAS Discovery - Tập 26 - Trang 428-438 - 2021
David McCoull1, Emma Ococks1, Jonathan M. Large1, David C. Tickle1, Alistair Mathie2, Jeffrey Jerman1, Paul D. Wright1
1LifeArc, Stevenage, UK
2Medway School of Pharmacy, University of Kent, Chatham Maritime, Kent, UK

Tài liệu tham khảo

Enyedi, 2010, Molecular Background of Leak K+ Currents: Two-Pore Domain Potassium Channels, Physiol. Rev., 90, 559, 10.1152/physrev.00029.2009 Mathie, 2015, Two-Pore Domain Potassium Channels: Potential Therapeutic Targets for the Treatment of Pain, Pflugers Arch., 467, 931, 10.1007/s00424-014-1655-3 Barel, 2008, Maternally Inherited Birk Barel Mental Retardation Dysmorphism Syndrome Caused by a Mutation in the Genomically Imprinted Potassium Channel Kcnk9, Am. J. Hum. Genet., 83, 193, 10.1016/j.ajhg.2008.07.010 Toncheva, 2014, Ngs Nominated Cela1, Hspg2, and Kcnk5 as Candidate Genes for Predisposition to Balkan Endemic Nephropathy, Biomed. Res. Int., 2014, 920723, 10.1155/2014/920723 Cazals, 2015, Kcnk5 Channels Mostly Expressed in Cochlear Outer Sulcus Cells Are Indispensable for Hearing, Nat. Commun., 6, 8780, 10.1038/ncomms9780 Ma, 2013, A Novel Channelopathy in Pulmonary Arterial Hypertension, N. Engl. J. Med., 369, 351, 10.1056/NEJMoa1211097 Mu, 2003, Genomic Amplification and Oncogenic Properties of the Kcnk9 Potassium Channel Gene, Cancer Cell, 3, 297, 10.1016/S1535-6108(03)00054-0 Alvarez-Baron, 2011, The Two-Pore Domain Potassium Channel Kcnk5: Induction by Estrogen Receptor Alpha and Role in Proliferation of Breast Cancer Cells, Mol. Endocrinol., 25, 1326, 10.1210/me.2011-0045 Alloui, 2006, TREK-1, a K+ Channel Involved in Polymodal Pain Perception, EMBO J., 25, 2368, 10.1038/sj.emboj.7601116 Vivier, 2017, Development of the First Two-Pore Domain Potassium Channel TWIK-Related K(+) Channel 1-Selective Agonist Possessing In Vivo Antinociceptive Activity, J. Med. Chem., 60, 1076, 10.1021/acs.jmedchem.6b01285 Acosta, 2014, TREK2 Expressed Selectively in Ib4-Binding C-Fiber Nociceptors Hyperpolarizes Their Membrane Potentials and Limits Spontaneous Pain, J. Neurosci., 34, 1494, 10.1523/JNEUROSCI.4528-13.2014 Noel, 2009, The Mechano-Activated K+ Channels TRAAK and TREK-1 Control Both Warm and Cold Perception, EMBO J., 28, 1308, 10.1038/emboj.2009.57 Pereira, 2014, Role of the TREK2 Potassium Channel in Cold and Warm Thermosensation and in Pain Perception, Pain, 155, 2534, 10.1016/j.pain.2014.09.013 Blanc, 2019, Genetics and Postsurgical Neuropathic Pain: An Ancillary Study of a Multicentre Survey, Eur. J. Anaesthesiol., 36, 342, 10.1097/EJA.0000000000000986 Gormley, 2016, Meta-Analysis of 375,000 Individuals Identifies 38 Susceptibility Loci for Migraine, Nat. Genet., 48, 856, 10.1038/ng.3598 Medhurst, 2001, Distribution Analysis of Human Two Pore Domain Potassium Channels in Tissues of the Central Nervous System and Periphery, Brain Res. Mol. Brain Res., 86, 101, 10.1016/S0169-328X(00)00263-1 Flegel, 2015, RNA-Seq Analysis of Human Trigeminal and Dorsal Root Ganglia with a Focus on Chemoreceptors, PLoS One, 10, e0128951, 10.1371/journal.pone.0128951 Reyes, 1998, Cloning and Expression of a Novel pH-Sensitive Two Pore Domain K+ Channel from Human Kidney, J. Biol. Chem., 273, 30863, 10.1074/jbc.273.47.30863 Langford, 2014, Variations in Potassium Channel Genes Are Associated with Breast Pain in Women Prior to Breast Cancer Surgery, J. Neurogenet., 28, 122, 10.3109/01677063.2013.856430 Marsh, 2012, Leak K(+) Channel mRNAs in Dorsal Root Ganglia: Relation to Inflammation and Spontaneous Pain Behaviour, Mol. Cell. Neurosci., 49, 375, 10.1016/j.mcn.2012.01.002 Garcia, 2019, Spinal TASK-1 and TASK-3 Modulate Inflammatory and Neuropathic Pain, Eur. J. Pharmacol., 862, 172631, 10.1016/j.ejphar.2019.172631 Liao, 2019, Selective Activation of TWIK-Related Acid-Sensitive K(+) 3 Subunit-Containing Channels Is Analgesic in Rodent Models, Sci. Transl. Med., 11, eaaw8434, 10.1126/scitranslmed.aaw8434 Lafreniere, 2010, A Dominant-Negative Mutation in the TRESK Potassium Channel Is Linked to Familial Migraine with Aura, Nat. Med., 16, 1157, 10.1038/nm.2216 Lafreniere, 2011, Migraine: Role of the TRESK Two-Pore Potassium Channel, Int J. Biochem. Cell Biol., 43, 1533, 10.1016/j.biocel.2011.08.002 Bagriantsev, 2013, A High-Throughput Functional Screen Identifies Small Molecule Regulators of Temperature- and Mechano-Sensitive K2p Channels, ACS Chem. Biol., 8, 1841, 10.1021/cb400289x Dadi, 2017, Selective Small Molecule Activators of TREK-2 Channels Stimulate Dorsal Root Ganglion C-Fiber Nociceptor Two-Pore-Domain Potassium Channel Currents and Limit Calcium Influx, ACS Chem. Neurosci., 8, 558, 10.1021/acschemneuro.6b00301 Tian, 2019, A Small-Molecule Compound Selectively Activates K2p Channel TASK-3 by Acting at Two Distant Clusters of Residues, Mol. Pharmacol., 96, 26, 10.1124/mol.118.115303 Wright, 2013, Cloxyquin (5-Chloroquinolin-8-ol) Is an Activator of the Two-Pore Domain Potassium Channel TRESK, Biochem. Biophys. Res. Commun., 441, 463, 10.1016/j.bbrc.2013.10.090 Wright, 2017, Terbinafine Is a Novel and Selective Activator of the Two-Pore Domain Potassium Channel TASK3, Biochem. Biophys. Res. Commun., 493, 444, 10.1016/j.bbrc.2017.09.002 Wright, 2019, Pranlukast Is a Novel Small Molecule Activator of the Two-Pore Domain Potassium Channel TREK2, Biochem. Biophys. Res. Commun., 520, 35, 10.1016/j.bbrc.2019.09.093 Loucif, 2018, Gi-530159, a Novel, Selective, Mechanosensitive Two-Pore-Domain Potassium (K2p) Channel Opener, Reduces Rat Dorsal Root Ganglion Neuron Excitability, Br. J. Pharmacol., 175, 2272, 10.1111/bph.14098 Lolicato, 2017, K2p2.1 (TREK-1)-Activator Complexes Reveal a Cryptic Selectivity Filter Binding Site, Nature, 547, 364, 10.1038/nature22988 Takahira, 2005, Fenamates and Diltiazem Modulate Lipid-Sensitive Mechano-Gated 2p Domain K(+) Channels, Pflugers Arch., 451, 474, 10.1007/s00424-005-1492-5 Monteillier, 2016, Investigation of the Structure Activity Relationship of Flufenamic Acid Derivatives at the Human TRESK Channel K2p18.1, Bioorg. Med. Chem. Lett., 26, 4919, 10.1016/j.bmcl.2016.09.020 Veale, 2014, Recovery of Current through Mutated TASK3 Potassium Channels Underlying Birk Barel Syndrome, Mol. Pharmacol., 85, 397, 10.1124/mol.113.090530 Tertyshnikova, 2005, Bl-1249 [(5,6,7,8-Tetrahydro-Naphthalen-1-yl)-[2-(1H-Tetrazol-5-yl)-Phenyl]-Amine]: A Putative Potassium Channel Opener with Bladder-Relaxant Properties, J. Pharmacol. Exp. Ther., 313, 250, 10.1124/jpet.104.078592 Veale, 2014, Influence of the N Terminus on the Biophysical Properties and Pharmacology of TREK1 Potassium Channels, Mol. Pharmacol., 85, 671, 10.1124/mol.113.091199 Pope, 2018, Protein and Chemical Determinants of Bl-1249 Action and Selectivity for K2p Channels, ACS Chem. Neurosci., 9, 3153, 10.1021/acschemneuro.8b00337 Schewe, 2019, A Pharmacological Master Key Mechanism That Unlocks the Selectivity Filter Gate in K(+) Channels, Science, 363, 875, 10.1126/science.aav0569 Barnash, 2017, Target Class Drug Discovery, Nat. Chem. Biol., 13, 1053, 10.1038/nchembio.2473 Birchall, 2019, Design of the Lifearc Index Set and Retrospective Review of Its Performance: A Collection for Sharing, SLAS Discov., 24, 332, 10.1177/2472555218803696 Lengyel, 2019, Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2p18.1) Background Potassium Channel, Mol. Pharmacol., 95, 652, 10.1124/mol.118.115626