Editorial Cite This: ACS Med. Chem. Lett. 2018, 9, 398−399
Allosteric Modulation of Ionotropic Glutamate Receptors Special Issue ABSTRACT: Call for papers! ACS Medicinal Chemistry Letters is now accepting manuscript submissions for a special issue entitled “Allosteric Modulation of Ionotropic Glutamate Receptors”. This special issue is a cross-thematic issue with Journal of Medicinal Chemistry and ACS Chemical Neuroscience. The ACS Medicinal Chemistry Letters special issue is scheduled for publication in early 2019.
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knowledge and stimulate new collaborations and new research directions. The Guest Editors, Carrie Haskell-Luevano (University of Minnesota) for Journal of Medicinal Chemistry, Craig Lindsley (Vanderbilt University) for ACS Chemical Neuroscience, and Nicholas Carruthers (Janssen Research & Development, LLC), Timothy Lovenberg (Janssen Research & Development, LLC), and Stephen Traynelis (Emory University) for ACS Medicinal Chemistry Letters, will be working together to publish these thematic issues in early 2019. We encourage you to submit your manuscripts at https:// acsparagonplus.acs.org by the end of September 2018. Please select “Allosteric Modulation of Ionotropic Glutamate Receptors” from the special issue dropdown box in the ACS Paragon Plus submission system. We are looking for original research manuscripts in the form of Letters, Notes, and Technology Notes, as well as Viewpoints and Innovations. If you are interested in submitting an Innovations manuscript for this Special Issue, please contact the journal’s Innovations Editor Stevan Djuric at djuric-offi
[email protected]. We invite you to be part of ACS history and contribute to the field’s knowledge of “Allosteric Modulators of Drug Targets”.
lutamate receptors are ligand-gated ion channels that play important roles in many important neurological processes, including synaptic transmission, development, learning, and memory. They comprise three different subgroups; AMPA, kainate, and N-methyl-D-aspartate (NMDA) receptors. This class of receptors, for decades, has been postulated to contribute to multiple neurological disorders or have been suggested to serve as drug targets for treatment of neurological diseases. Vigorous developmental activity in the 1990s through the early 2000s led to multiple clinical trials of NMDA receptor antagonists for neuroprotection and other indications, virtually none of which yielded results that allowed FDA approval for candidate drugs.1 To date, only the relatively nonselective drugs dextromethorphan, ketamine, memantine, and perampanel have been approved for use in humans, with relatively limited indications and utility. Part of the problem with early drug development that targeted glutamate receptors was the nonselective nature of compounds that progressed to clinical development, which strongly blocked all forms of the targeted receptors, leading to dose-lowering side effects that complicated clinical trial design and outcomes. This reduced enthusiasm in particular for NMDA receptors as a therapeutic target.2 However, the identification of multiple AMPA, kainate, and NMDA receptor subunits, the enablement of structural resolution, coupled with basic science showing unique distribution and roles created an opportunity to target glutamate receptor function with subunit-selective agents.3 Furthermore, the appreciation that allosteric modulators interact with less conserved portions of the receptor to tune function up or down in a graded fashion offered an opportunity to circumvent side effects while retaining efficacious actions at the desired glutamate receptor subunit. This idea has driven considerable work on the glutamate receptor modulators. Furthermore, advances in our understanding of accessory subunits has opened new opportunities to modulate AMPA and kainate receptors.4 This special issue is an opportunity to bring together work from leading laboratories in this intellectual space to showcase new developments, present new ideas, and elucidate mechanism and utility of new modulators. ACS Medicinal Chemistry Letters welcomes contributions within the scope of the journal and call for papers for this crossthematic special issue. The simultaneous publication of a series of communications, articles, and review-type manuscripts in the three journals should provide an excellent forum for researchers to share their most important recent findings and offer exceptional exposure of the published articles to the scientific community. We hope that the special issues will advance © 2018 American Chemical Society
Nicholas I. Carruthers,† Guest Editor Timothy W. Lovenberg,† Guest Editor Stephen F. Traynelis,*,‡ Guest Editor †
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Janssen Research & Development, LLC, La Jolla, California 92121, United States ‡ Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia 30322, United States
AUTHOR INFORMATION
ORCID
Stephen F. Traynelis: 0000-0002-3750-9615 Notes
Views expressed in this editorial are those of the authors and not necessarily the views of the ACS.
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REFERENCES
(1) Yuan, H.; Myers, S. J.; Wells, G.; Nicholson, K. L.; Swanger, S. A.; Lyuboslavsky, P.; Tahirovic, Y. A.; Menaldino, D. S.; Ganesh, T.; Wilson, L. J.; Liotta, D. C.; Snyder, J. P.; Traynelis, S. F. Contextdependent GluN2B-selective inhibitors of NMDA receptor function
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DOI: 10.1021/acsmedchemlett.8b00174 ACS Med. Chem. Lett. 2018, 9, 398−399
ACS Medicinal Chemistry Letters
Editorial
are neuroprotective with minimal side effects. Neuron 2015, 85 (6), 1305−1318. (2) Ogden, K. K.; Traynelis, S. F. New advances in NMDA receptor pharmacology. Trends Pharmacol. Sci. 2018, 32 (12), 726−33. (3) Burnell, E. S.; Irvine, M.; Fang, G.; Sapkota, K.; Jane, D. E.; Monaghan, D. T. J. Med. Chem. 2018, DOI: 10.1021/acs.jmedchem.7b01640. (4) Maher, M. P.; Matta, J. A.; Gu, S.; Seierstad, M.; Bredt, D. S. Getting a handle on Neuropharmacology bvy targeting receptorassociated proteins. Neuron 2017, 96, 989−1001.
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DOI: 10.1021/acsmedchemlett.8b00174 ACS Med. Chem. Lett. 2018, 9, 398−399
