Patent SG-11201900085T-A (SG)
Title: Modified ligand-gated ion channels and methods of use
Inventor: STERNSON SCOTT
IPC: G01N33/68
Filed: 2017-07-07
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1111111011111111101 0111011101111101001H011101111111111111111011111111111110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/009832 Al 11 January 2018 (11.01.2018) W I PO I PCT (51) International Patent Classification: C07K 14/705 (2006.01) Cl 2N 5/071 (2010.01) Published: G01N 33/58 (2006.01) A61K 48/00 (2006.01) — with international search report (Art. 21(3)) G01N 33/68 (2006.01) A61K 38/00 (2006.01) — with sequence listing part of description (Rule 5.2(a)) (21) International Application Number: PCT/US2017/041147 (22) International Filing Date: 07 July 2017 (07.07.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/359,534 07 July 2016 (07.07.2016) US 62/486,779 18 April 2017 (18.04.2017) US (72) Inventors; and (71) Applicants: STERNSON, Scott [US/US]; 4000 Jones Bridge Road, Chevy Chase, Maryland 20815-6789 (US). LEE, Peter [US/US]; 4000 Jones Bridge Road, Chevy _ Chase, Maryland 20815-6789 (US). MAGNUS, Christo- pher — [US/US]; 4000 Jones Bridge Road, Chevy Chase, Maryland 20815-6789 (US). = Agent: WILLIS, Margaret S. J. et al.; Fish & Richardson (74) = _ P.C., P.O. Box 1022, Minneapolis, Minnesota 55440-1022 = (US). = = (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, _ _= = MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, = — = OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. = Designated States (unless otherwise indicated, for every (84) = kind of regional protection available): ARIPO (BW, GH, = — GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, = UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, = — Il KM, ML, MR, NE, SN, TD, TG). . 4 ei M X ) (54) Title: MODIFIED LIGAND-GATED ION CHANNELS AND METHODS OF USE 01 C ::: : (57) : This document relates to materials and methods for controlling ligand gated ion channel (LGIC) activity. For example, 0 —. modified LGICs including at least one LGIC subunit having a modified ligand binding domain (LBD) and/or a modified ion pore GC , 1 domain (IPD) are provided. Also provided are exogenous LGIC ligands that can bind to and activate the modified LGIC, as well as © methods of modulating ion transport across the membrane of a cell of a mammal, methods of modulating the excitability of a cell in N a mammal, and methods of treating a mammal having a channelopathy. 0