Patent SG-11201407017W-A (SG)
Title: Site-specific labeling methods and molecules produced thereby
Inventor: GEIERSTANGER BERNHARD HUBERT
IPC: C07K16/32
Filed: 2013-05-31
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 12 December 2013 (12.12.2013) WIPOIPCT (10) International Publication Number WO 2013/184514 A1 (51) International Patent Classification: C07K16/00 (2006.01) C07K 7/08 (2006.01) C07K16/32 (2006.01) A61K 47/48 (2006.01) C07K 7/06 (2006.01) C12N 9/10 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/043684 31 May 2013 (31.05.2013) English (30) Priority Data: 61/655,143 61/777,430 4 June 2012 (04.06.2012) 12 March 2013 (12.03.2013) English US US (71) Applicant (for all designated States except US): IRM LLC [US/—]; A Delaware Limited Liability Company, 131 Front Street, PO Box HM 2899, Hamilton, HM LX (BM). (72) Inventors; and (71) Applicants (for US only): GEIERSTANGER, Bernhard Hubert [DE/US]; Novartis Institute for Functional Genom­ ics, Inc. Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, California 92121 (US). GRUNEWALD, Jan [DE/US]; Novartis Institute for Functional Genomics, Inc., Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, Cali­ fornia 92121 (US). BURSULAYA, Badry [US/US]; No­ vartis Institute for Functional Genomics, Inc., Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, California 92121 (US). (74) Agent: BENNI, Mei; c/o Novartis Pharmaceuticals Cor­ poration, IP Services Mail Data, One Health Plaza 101/2, East Hanover, New Jersey 07936 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, 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, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) — with sequence listing part of description (Rule 5.2(a)) (54) Title: SITE-SPECIFIC LABELING METHODS AND MOLECULES PRODUCED THEREBY PPTase is 4-phosphopantetheinyl transferase TG is Terminating Group Ser is serine ppan is 4-phosphopantetheine T-H oo T-H rn T-H o CJ ppan FIG.1 (57) Abstract: The present disclosure provides methods of site-specific labeling of antibodies, using proteins having 4'-phospho- pantetheinyl transferase activity that catalyze post-translational modification of peptide sequences (\"peptide tags\") incorporated into one or more specific sites of an antibody of interest. Enzymatic labeling enables quantitative and irreversible covalent modification of a specific serine residue within the peptide tags incorporated into the antibody, and thus creates desirable antibody conjugates.