Monoclonal Antibodies Targeting Ion Channels and Their Therapeutic Potential

Aida, 2012, Overstimulation of NMDA receptors impairs early brain development in vivo, PLoS One, 7, 10.1371/journal.pone.0036853

Amrutkar, 2012, Fine mapping of a monoclonal antibody to the N-methyl d-aspartate receptor reveals a short linear epitope, Biopolymers, 98, 567, 10.1002/bip.22165

Bagal, 2013, Ion channels as therapeutic targets: a drug discovery perspective, J. Med. Chem., 56, 593, 10.1021/jm3011433

Baklaushev, 2009, Immunofluorescent analysis of connexin-43 using monoclonal antibodies to its extracellular domain, Bull. Exp. Biol. Med., 148, 725, 10.1007/s10517-010-0802-x

Balse, 2017, Ion channel trafficking: control of ion channel density as a target for arrhythmias, Front. Physiol., 8, 10.3389/fphys.2017.00808

Bandell, 2004, Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin, Neuron, 41, 849, 10.1016/S0896-6273(04)00150-3

Bao, 2011, Connexon-mediated cell adhesion drives microtissue self-assembly, FASEB J., 25, 255, 10.1096/fj.10-155291

Brüggemann, 1997, Mitosis-promoting factor-mediated suppression of a cloned delayed rectifier potassium channel expressed in Xenopus oocytes, Proc. Natl. Acad. Sci. U. S. A., 94, 537, 10.1073/pnas.94.2.537

Buell, 1998, Blockade of human P2X7 receptor function with a monoclonal antibody, Blood, 92, 3521, 10.1182/blood.V92.10.3521

Caterina, 1999, A capsaicin-receptor homologue with a high threshold for noxious heat, Nature, 398, 436, 10.1038/18906

Catterall, 2015, Structural basis for pharmacology of voltage-gated sodium and calcium channels, Mol. Pharmacol., 88, 141, 10.1124/mol.114.097659

Chen, 1995, A P2X purinoceptor expressed by a subset of sensory neurons, Nature, 377, 428, 10.1038/377428a0

Choi, 1990, The role of glutamate neurotoxicity in hypoxic–ischemic neuronal death, Ann. Rev. Neurosci., 13, 171, 10.1146/annurev.ne.13.030190.001131

Choi, 2005, Kv1.5 surface expression is modulated by retrograde trafficking of newly endocytosed channels by the dynein motor, Circ. Res., 97, 363, 10.1161/01.RES.0000179535.06458.f8

Clapham, 2001, The TRP ion channel family, Nat. Rev. Neurosci., 2, 387, 10.1038/35077544

Cox, 2013, Antibody-mediated targeting of the Orai1 calcium channel inhibits T cell function, PLoS One, 8, 10.1371/journal.pone.0082944

Cox, 2006, An SCN9A channelopathy causes congenital inability to experience pain, Nature, 444, 894, 10.1038/nature05413

Danquah, 2016, Nanobodies that block gating of the P2X7 ion channel ameliorate inflammation, Sci. Transl. Med., 8, 10.1126/scitranslmed.aaf8463

Davis, 2000, Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia, Nature, 405, 183, 10.1038/35012076

Derzi, 2016, Nonclinical evaluation of PF-06438179: a potential biosimilar to Remicade® (Infliximab), Adv. Ther., 33, 1964, 10.1007/s12325-016-0403-9

Ecker, 2015, The therapeutic monoclonal antibody market, MAbs, 7, 9, 10.4161/19420862.2015.989042

Elitt, 2006, Artemin overexpression in skin enhances expression of TRPV1 and TRPA1 in cutaneous sensory neurons and leads to behavioral sensitivity to heat and cold, J. Neurosci., 26, 8578, 10.1523/JNEUROSCI.2185-06.2006

Fertleman, 2006, SCN9A mutations in paroxysmal extreme pain disorder: allelic variants underlie distinct channel defects and phenotypes, Neuron, 52, 767, 10.1016/j.neuron.2006.10.006

Feske, 2006, A mutation in Orai1 causes immune deficiency by abrogating CRAC channel function, Nature, 441, 179, 10.1038/nature04702

Furukawa, 2005, Subunit arrangement and function in NMDA receptors, Nature, 438, 185, 10.1038/nature04089

Geppetti, 2010, Cough: the emerging role of the TRPA1 channel, Lung, 188, 10.1007/s00408-009-9201-3

Ghilardi, 2005, Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain, J. Neurosci., 25, 3126, 10.1523/JNEUROSCI.3815-04.2005

Gilbert, 2019, ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival, Oncogene, 38, 194, 10.1038/s41388-018-0426-6

Gilbert, 2017, A phase I clinical trial demonstrates that nfP2X 7-targeted antibodies provide a novel, safe and tolerable topical therapy for basal cell carcinoma, Br. J. Dermatol., 177, 117, 10.1111/bjd.15364

Gómez-Varela, 2007, Monoclonal antibody blockade of the human Eag1 potassium channel function exerts antitumor activity, Cancer Res., 67, 7343, 10.1158/0008-5472.CAN-07-0107

Grek, 2018, Novel approach to temozolomide resistance in malignant glioma: connexin43-directed therapeutics, Curr. Opin. Pharmacol., 41, 79, 10.1016/j.coph.2018.05.002

Gutman, 2005, International Union of Pharmacology, Pharmacol. Rev., 57, 473, 10.1124/pr.57.4.10

Gwack, 2008, Hair loss and defective T- and B-cell function in mice lacking ORAI1, Mol. Cell Biol., 28, 5209, 10.1128/MCB.00360-08

Haring, 1991, Glycine-like modulation of N-methyl-d-aspartate receptors by a monoclonal antibody that enhances long-term potentiation, J. Neurochem., 57, 323, 10.1111/j.1471-4159.1991.tb02131.x

Harris, 1997, Refined structure of an intact IgG2a monoclonal antibody, Biochemistry, 36, 1581, 10.1021/bi962514+

Harris, 1998, Crystallographic structure of an intact IgG1 monoclonal antibody, J. Mol. Biol., 275, 861, 10.1006/jmbi.1997.1508

Hemmerlein, 2006, Overexpression of Eag1 potassium channels in clinical tumours, Mol. Cancer, 5, 41, 10.1186/1476-4598-5-41

Honore, 2005, A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats, J. Pharmacol. Exp. Ther., 314, 410, 10.1124/jpet.105.083915

Hou, 2008, Humanization of an anti-CD34 monoclonal antibody by complementarity-determining region grafting based on computer-assisted molecular modelling, J. Biochem., 144, 115, 10.1093/jb/mvn052

Igawa, 2013, Preparation and characterization of a monoclonal antibody against the refolded and functional extracellular domain of rat P2X4 receptor, J. Biochem., 153, 275, 10.1093/jb/mvs143

Jimenez-Andrade, 2010, Bone cancer pain, Ann. N. Y. Acad. Sci., 1198, 173, 10.1111/j.1749-6632.2009.05429.x

Jordt, 2004, Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1, Nature, 427, 260, 10.1038/nature02282

Ju, 2002, Molecular identification and characterisation of the human eag2 potassium channel, FEBS Lett., 524, 204, 10.1016/S0014-5793(02)03055-7

Klionsky, 2006, A polyclonal antibody to the prepore loop of transient receptor potential vanilloid type 1 blocks channel activation, J. Pharmacol. Exp. Ther., 319, 192, 10.1124/jpet.106.108092

Kremeyer, 2010, A gain-of-function mutation in TRPA1 causes familial episodic pain syndrome, Neuron, 66, 671, 10.1016/j.neuron.2010.04.030

Lee, 2017, Glycosylation profile and biological activity of Remicade® compared with Flixabi® and Remsima®, MAbs, 9, 968, 10.1080/19420862.2017.1337620

Lee, 2014, A monoclonal antibody that targets a NaV1.7 channel voltage sensor for pain and itch relief, Cell, 157, 1393, 10.1016/j.cell.2014.03.064

Lee, 2014, Mouse monoclonal antibodies to transient receptor potential ankyrin 1 act as antagonists of multiple modes of channel activation, J. Pharmacol. Exp. Ther., 350, 223, 10.1124/jpet.114.215574

Lee, 2013, Liver tumor-initiating cells as a therapeutic target for hepatocellular carcinoma, Cancer Lett., 338, 101, 10.1016/j.canlet.2012.05.001

Li, 2009, Memory and the NMDA receptors, N. Engl. J. Med., 361, 302, 10.1056/NEJMcibr0902052

Lin, 2013, Generation and characterization of fully human monoclonal antibodies against human Orai1 for autoimmune disease, J. Pharmacol. Exp. Ther., 345, 225, 10.1124/jpet.112.202788

Liu, 2016, Evaluation of recombinant monoclonal antibody SVmab1 binding to NaV1.7 target sequences and block of human NaV1.7 currents, F1000Res., 5, 2764, 10.12688/f1000research.9918.1

Liu, 2014, Upregulation of store-operated Ca(2+) entry in the naïve CD4(+) T cells with aberrant cytokine releasing in active rheumatoid arthritis, Immunol. Cell. Biol., 92, 752, 10.1038/icb.2014.45

Luini, 1981, Distinct pharmacological properties of excitatory amino acid receptors in the rat striatum: study by Na+ efflux assay, Proc. Natl. Acad. Sci. U. S. A., 78, 3250, 10.1073/pnas.78.5.3250

Lynch, 2017, Potential functional and pathological side effects related to off-target pharmacological activity, J. Pharmacol. Toxicol. Methods, 87, 108, 10.1016/j.vascn.2017.02.020

Morris, 1990, Hippocampal synaptic plasticity and NMDA receptors: a role in information storage, Philos. Trans. R. Soc. Lond. B. Biol. Sci., 329, 187, 10.1098/rstb.1990.0164

Morris, 2013, N-methyl-d-aspartate receptors, learning and memory: chronic intraventricular infusion of the NMDA receptor antagonist d-AP5 interacts directly with the neural mechanisms of spatial learning, Eur. J. Neurosci., 37, 700, 10.1111/ejn.12086

Moskal, 2017, The development of Rapastinel (formerly GLYX-13); a rapid acting and long lasting antidepressant, Curr. Neuropharmacol., 15, 47, 10.2174/1570159X14666160321122703

Napp, 2016, In vivo imaging of tumour xenografts with an antibody targeting the potassium channel K, Eur. Biophys. J., 45, 721, 10.1007/s00249-016-1152-z

Nasu-Tada, 2006, Possible involvement of increase in spinal fibronectin following peripheral nerve injury in upregulation of microglial P2X4, a key molecule for mechanical allodynia, Glia, 53, 769, 10.1002/glia.20339

North, 2002, Molecular physiology of P2X receptors, Physiol. Rev., 82, 1013, 10.1152/physrev.00015.2002

Obata, 2005, TRPA1 induced in sensory neurons contributes to cold hyperalgesia after inflammation and nerve injury, J. Clin. Invest., 115, 2393, 10.1172/JCI25437

Oshima, 2014, Structure and closure of connexin gap junction channels, FEBS Lett., 588, 1230, 10.1016/j.febslet.2014.01.042

Ouadid-Ahidouch, 2016, Kv10.1 K(+) channel: from physiology to cancer, Pflugers Arch., 468, 751, 10.1007/s00424-015-1784-3

Pardo, 1998, Cell cycle-related changes in the conducting properties of r-eag K+ channels, J. Cell Biol., 143, 767, 10.1083/jcb.143.3.767

Pierri, 2010, Computational approaches for protein function prediction: a combined strategy from multiple sequence alignment to molecular docking-based virtual screening, Biochim. Biophys. Acta., 1804, 1695, 10.1016/j.bbapap.2010.04.008

Pierri, 2016, Molecular modeling of antibodies for the treatment of TNFα-related immunological diseases, Pharmacol. Res. Perspect., 4, 10.1002/prp2.197

Revel, 1985, Chemistry of gap junctions, Annu. Rev. Physiol., 47, 263, 10.1146/annurev.ph.47.030185.001403

Saez, 2003, Plasma membrane channels formed by connexins: their regulation and functions, Physiol. Rev., 83, 1359, 10.1152/physrev.00007.2003

Saganich, 1999, Cloning of components of a novel subthreshold-activating K(+) channel with a unique pattern of expression in the cerebral cortex, J. Neurosci., 19, 10789, 10.1523/JNEUROSCI.19-24-10789.1999

Saphire, 2001, Crystal structure of a neutralizing human IGG against HIV-1: a template for vaccine design, Science, 293, 1155, 10.1126/science.1061692

Schönherr, 2002, Functional distinction of human EAG1 and EAG2 potassium channels, FEBS Lett., 514, 204, 10.1016/S0014-5793(02)02365-7

Global markets for bioengineered protein drugs Shalini ShahaniD. 2017

Shcherbatko, 2016, Modulation of P2X3 and P2X2/3 receptors by monoclonal antibodies, J. Biol. Chem., 291, 12254, 10.1074/jbc.M116.722330

Sikandar, 2012, Visceral pain: the ins and outs, the ups and downs, Curr. Opin. Support Palliat Care, 6, 17, 10.1097/SPC.0b013e32834f6ec9

Siller-Jackson, 2008, Adaptation of connexin 43-hemichannel prostaglandin release to mechanical loading, J. Biol. Chem., 283, 26374, 10.1074/jbc.M803136200

Smani, 2015, Functional and physiopathological implications of TRP channels, Biochim. Biophys. Acta., 1853, 1772, 10.1016/j.bbamcr.2015.04.016

Snyder, 2014, An SCN9A variant, known to cause pain, is now found to cause itch, Pain, 155, 1677, 10.1016/j.pain.2014.05.028

Taylor-Clark, 2009, TRPA1: a potential target for anti-tussive therapy, Pulm. Pharmacol. Ther., 22, 71, 10.1016/j.pupt.2008.12.019

Thompson, 1992, Hippocampus-dependent learning facilitated by a monoclonal antibody or D-cycloserine, Nature, 359, 638, 10.1038/359638a0

Ufartes, 2013, Behavioural and functional characterization of Kv10.1 (Eag1) knockout mice, Hum. Mol. Genet., 22, 2247, 10.1093/hmg/ddt076

Valera, 1994, A new class of ligand-gated ion channel defined by P2x receptor for extracellular ATP, Nature, 371, 516, 10.1038/371516a0

Viana, 2009, TRPA1 modulators in preclinical development, Expert. Opin. Ther. Pat., 19, 1787, 10.1517/13543770903393771

Weiss, 2011, Loss-of-function mutations in sodium channel Nav1.7 cause anosmia, Nature, 472, 186, 10.1038/nature09975

Wickenden, 2012, Ion channel drug discovery: challenges and future directions, Future Med. Chem., 4, 661, 10.4155/fmc.12.4

Wilkinson, 2015, Discovery of functional antibodies targeting ion channels, J. Biomol. Screen, 20, 454, 10.1177/1087057114560698

Zhao, 2013, 1B50-1, a mAb raised against recurrent tumor cells, targets liver tumor-initiating cells by binding to the calcium channel α2δ1 subunit, Cancer Cell, 23, 541, 10.1016/j.ccr.2013.02.025