HRP20181055T1 - Antagonisti kv1.3 i postupci upotrebe - Google Patents
Antagonisti kv1.3 i postupci upotrebe Download PDFInfo
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- HRP20181055T1 HRP20181055T1 HRP20181055TT HRP20181055T HRP20181055T1 HR P20181055 T1 HRP20181055 T1 HR P20181055T1 HR P20181055T T HRP20181055T T HR P20181055TT HR P20181055 T HRP20181055 T HR P20181055T HR P20181055 T1 HRP20181055 T1 HR P20181055T1
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- 239000005557 antagonist Substances 0.000 title claims 18
- 101000994669 Homo sapiens Potassium voltage-gated channel subfamily A member 3 Proteins 0.000 title claims 14
- 238000000034 method Methods 0.000 title claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 18
- 229940083963 Peptide antagonist Drugs 0.000 claims 17
- 210000004899 c-terminal region Anatomy 0.000 claims 11
- 229940024606 amino acid Drugs 0.000 claims 10
- 150000001413 amino acids Chemical class 0.000 claims 10
- 125000005647 linker group Chemical group 0.000 claims 9
- 102000009027 Albumins Human genes 0.000 claims 6
- 108010088751 Albumins Proteins 0.000 claims 6
- 210000004027 cell Anatomy 0.000 claims 6
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- 210000002966 serum Anatomy 0.000 claims 5
- 102000046611 human KCNA3 Human genes 0.000 claims 4
- 230000006044 T cell activation Effects 0.000 claims 3
- 229910052700 potassium Inorganic materials 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 102000008100 Human Serum Albumin Human genes 0.000 claims 2
- 108091006905 Human Serum Albumin Proteins 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 108020001507 fusion proteins Proteins 0.000 claims 2
- 102000037865 fusion proteins Human genes 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 102000040430 polynucleotide Human genes 0.000 claims 2
- 108091033319 polynucleotide Proteins 0.000 claims 2
- 239000002157 polynucleotide Substances 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Natural products NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 1
- 239000004471 Glycine Substances 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 102000007562 Serum Albumin Human genes 0.000 claims 1
- 108010071390 Serum Albumin Proteins 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000004113 cell culture Methods 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000004907 flux Effects 0.000 claims 1
- 125000003630 glycyl group Chemical class [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 125000000741 isoleucyl group Chemical group [H]N([H])C(C(C([H])([H])[H])C([H])([H])C([H])([H])[H])C(=O)O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 238000011084 recovery Methods 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229910052716 thallium Inorganic materials 0.000 claims 1
- BKVIYDNLLOSFOA-UHFFFAOYSA-N thallium Chemical compound [Tl] BKVIYDNLLOSFOA-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
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- C07K14/43504—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates
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Claims (15)
1. Izolirani peptidni antagonist Kv1.3 naznačen time da ima sekvencu aminokiselina koja sadrži sekvencu aminokiselina koja je barem 84% identična sa SEQ ID NO: 1, koja nadalje ima supstituciju glicina s izoleucinom u položaju 10 (G10I).
2. Antagonist prema zahtjevu 1 naznačen time da:
(i) sekvenca sadrži GVPXaa1Xaa2VKCXaa3ISRQCXaa4Xaa5PCKDAGMRFGKCMNGKCHCTPK; gdje
a) Xaa1 je I ili T, Q ili E;
b) Xaa2 je N ili D;
c) Xaa3je K ili R, E, A ili Q;
d) Xaa4 je I, E, L, D, Q, H,V, K ili A;
e) Xaa5 je E K, L, Q, D, V ili H; i
peptidni antagonist Kvl.3 ima proizvoljno C-terminalno produljenje od četiri aminokiseline;
(ii) antagonist je kombinirani protein koji sadrži peptidni antagonist Kv1.3 koji je konjugiran s ostatkom za produljivanje polu-života, gdje peptidni antagonist Kv1.3 sadrži sekvencu GVPXaa1Xaa2VKCXaa3ISRQCXaa4Xaa5PCKDAGMRFGKCMNGKCHCTPK; gdje
a) Xaa1 je I ili T, Q ili E;
b) Xaa2 je N ili D;
c) Xaa3 je K ili R, E, A ili Q;
d) Xaa4 je I, E, L, D, Q, H,V, K ili A;
e) Xaa5 je E K, L, Q, D, V ili H; i
peptidni antagonist Kvl.3 ima proizvoljno C-terminalno produljenje od četiri aminokiseline;
(iii) sekvenca sadrži GVPXaalXaa2VKCXaa3ISRQCXaa4Xaa5PCKDAGMRFGKCMNGKCHCTPK; gdje
a) Xaa1 je I ili T
b) Xaa2 je N ili D;
c) Xaa3 je K ili R;
d) Xaa4 je I ili E;
e) Xaa5 je E ili K; i
peptidni antagonist Kvl.3 ima proizvoljno C-terminalno produljenje od četiri aminokiseline; i/ili
(iv) peptidni antagonist Kvl.3 sadrži sekvencu aminokiselina SEQ ID NOs: 42, 3, 13, 21, 22, 24, 26, 29, 30, 32, 34, 38, 39, 43, 44, 45, 46, 49, 51, 59, 63, 65, 69, 71, 73, 76, 78, 81, 82, 83, 85, 87, 89, 92, 96, 101, 103, 104, i 108, proizvoljno gdje peptidni antagonist Kvl.3 sadrži sekvencu aminokiselina SEQ ID NOs: 3, 22, 34 ili 42.
3. Antagonist prema zahtjevu 1 ili zahtjevu 2, naznačen time da:
(i) C-terminalni produžetak sadrži sekvencu aminokiselina SEQ ID NOs: 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267 ili 268, proizvoljno gdje C-terminalni produžetak sadrži sekvencu aminokiselina SEQ ID NOs: 128, 143, 155, 188, 206-210, 212, 214, 216, 219, 223, 224, 227, 230, 232 -235, 237, 239, 240, 243, 252, 261, 262, 263, ili 268; i/ili
(ii) ostatak koji produljuje polu-život je albumin iz seruma, domena za vezanje albumina (ADB), ili polietilen glikol (PEG), proizvoljno gdje ostatak za produljenje polu-života je albumin iz seruma čovjeka.
4. Antagonisti prema zahtjevima 1-3, naznačen time da je ostatak za produljenje polu-života konjugiran na peptidni antagonist Kv1.3 pomoću skupine za povezivanje, proizvoljno gdje skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NOs: 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122 ili 428.
5. Antagonist prema zahtjevu 4, naznačen time da
(i)
a) peptidni antagonist Kvl.3 sadrži sekvencu aminokiselina od SEQ ID NOs: 3, 22, 34 ili 42;
b) proizvoljno C-terminalni produžetak sadrži sekvencu aminokiselina od SEQ ID NOs: 128, 143, 155, 188, 206-210, 212, 214, 216, 219, 223, 224, 227, 230, 232 -235, 237, 239, 240, 243, 252, 261, 262, 263, ili 268;
c) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NO: 116 ili SEQ ID NO:119; i d) ostatak koji produljuje polu-život je albumin iz ljudskog seruma;
(ii)
a) peptidni antagonist Kv1.3 sadrži sekvencu aminokiselina SEQ ID NO: 42;
b) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NO: 116; i
c) skupina za produljenje polu-života je albumin iz ljudskog seruma;
(iii)
a) peptidni antagonist Kv1.3 sadrži sekvencu aminokiselina SEQ ID NO: 42;
b) C-terminalno produljenje sadrži sekvencu aminokiselina SEQ ID NO: 209;
c) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NO: 116; i
d) skupina za produljenje polu-života je albumin iz ljudskog seruma;
(iv)
a) peptidni antagonist Kv1.3 sadrži sekvencu aminokiselina SEQ ID NO: 3;
b) C- terminalno produljenje sadrži sekvencu aminokiselina SEQ ID NO: 235;
c) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NO: 116; i
d) skupina za produljenje polu-života je albumin iz ljudskog seruma; ili
(v)
a) peptidni antagonist Kvl.3 sadrži sekvencu aminokiselina SEQ ID NO: 42;
b) C- terminalno produljenje sadrži sekvencu aminokiselina SEQ ID NO: 235;
c) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NO: 116; i
d) skupina za produljenje polu-života je albumin iz ljudskog seruma.
6. Antagonist prema zahtjevima 2-5, naznačen time da je antagonist barem 100 puta selektivniji prema humanom Kv1.3 nego u odnosu na humani Kv1.1, pri čemu se selektivnost mjeri kao omjer IC50 vrijednosti izoliranog kombiniranog proteina za Kv1.1 prema IC50 vrijednosti izoliranog kombiniranog proteina za Kv1.3 u „patch clamp“ testu u stanicama u kojima je izvršena transfekcija s Kv1.1 i Kvl.3, redom; proizvoljno gdje antagonist inhibira struje kalija s IC50 vrijednosti koja je barem 10 puta manja od IC50 vrijednosti za matični KV1C2 kombinirani protein koji ima SEQ ID NO: 425 u „patch clamp“ testu u stanicama u kojima je izvršena transfekcija s ljudskim Kv1.3; poželjno pri čemu kombinirani protein inhibira struje s IC50 vrijednosti od oko 1,5x10-8 M ili manje u „patch clamp“ kod stanica u kojima je izvršena transfekcija s ljudskim Kv1.3; proizvoljno pri čemu kombinirani protein inhibira in vitro fluks talija s IC50 vrijednosti od oko 2,2x10-8 M ili manje kod stanica u kojima je izvršena transfekcija s ljudskim Kv1.3.
7. Antagonist prema zahtjevu 1 koji sadrži bilo koju sekvencu od SEQ ID NOs: 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 85, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109 ili 110.
8. Antagonist prema zahtjevu 7, naznačen time da je antagonist kombinirani protein koji sadrži peptidni antagonist Kvl.3 koji je konjugiran s ostatkom za produljenje polu-života pomoću skupine za povezivanje, peptidni antagonist Kvl.3 ima proizvoljno C-terminalno produljenje s četiri aminokiseline, gdje
a) peptidni antagonist Kv1.3 koji sadrži sekvencu aminokiselina SEQ ID NOs: 3-54, 56-83, 85 ili 87-110;
b) C-terminalno produljenje sadrži sekvencu aminokiselina SEQ ID NOs: 123-268;
c) skupina za povezivanje sadrži sekvencu aminokiselina SEQ ID NOs: 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122 ili 428; i
d) ostatak za produljenje polu-života je albumin iz ljudskog seruma.
9. Izolirani polinukleotid naznačen time da kodira antagonist prema bilo kojem prethodnom zahtjevu.
10. Vektor naznačen time da sadrži izolirani polinukleotid prema zahtjevu 9.
11. Stanica domaćina naznačena time da sadrži vektor prema zahtjevu 10.
12. Postupak za proizvodnju izoliranog antagonista prema zahtjevima 1-7, naznačen time da sadrži uzgoj u kulturi stanice domaćina prema zahtjevu 11 i ponovno dobivanje antagonista koji je eksprimiran od strane stanice domaćina.
13. Farmaceutski pripravak naznačen time da sadrži antagonist prema zahtjevima 1-7 i farmaceutski prihvatljivi nosač.
14. Antagonist prema zahtjevima 1-7 naznačen time da je za upotrebu u suprimiranju T stanične aktivacije kod subjekta koji ima stanje koje je povezano s nepoželjnom T staničnom aktivacijom, proizvoljno gdje stanje povezano s neželjenom T staničnom aktivacijom je upalno stanje, imuni i proliferativni poremećaj, reumatoidni artritis (RA), ankilozantni spondilitis, psorijazni artritis, osteoartritis, osteoporoza, uveitis, fibroza uzrokovana upalnim stanjem, sklerodermija, fibroza pluća, ciroza, upalna bolest crijeva, Crohnova bolest, ulcerozni kolitis, astma, alergijska astma, alergije, kronična opstruktivna bolest pluća (KOPB), multipla skleroza, psorijaza, kontaktom posredovani dermatitis, sistemski eritemski lupus (SLE) i drugi oblici lupusa, dijabetes, dijabetes tip I, pretilost, karcinom, lupus, restenoza, sistemska skleroza, sklerodermija, glomerulonefritis, Sjögrenov sindrom, resorpcija kostiju koja je povezana s upalom, odbacivanje transplantata, ili bolesti presatka protiv domaćina.
15. Antagonist prema zahtjevima 1-7 naznačen time da je za upotrebu u terapiji.
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| EP14743871.7A EP2948559B1 (en) | 2013-01-25 | 2014-01-24 | Kv1.3 antagonists and methods of use |
| PCT/US2014/012932 WO2014116937A1 (en) | 2013-01-25 | 2014-01-24 | Kv1.3 antagonists and methods of use |
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| US10246496B2 (en) * | 2014-08-15 | 2019-04-02 | La Trobe University | Potassium channel blockers and use thereof in the treatment of autoimmune diseases |
| US10259122B2 (en) | 2015-03-05 | 2019-04-16 | President And Fellows Of Harvard College | Compliant adaptive robot grasper |
| US11597763B2 (en) | 2016-05-02 | 2023-03-07 | Tetragenetics, Inc. | Anti-Kv1.3 antibodies, and methods of production and use thereof |
| US10336812B2 (en) * | 2016-05-10 | 2019-07-02 | Janssen Biotech, Inc. | GDF15 fusion proteins and uses thereof |
| TW201808987A (zh) * | 2016-06-08 | 2018-03-16 | 健生生物科技公司 | Ｇｍ－ｃｓｆ變體及使用方法 |
| CN106589092A (zh) * | 2016-12-22 | 2017-04-26 | 中国科学技术大学先进技术研究院 | 一种蝎毒素多肽及制备拥有类似天然生理功能的蝎毒素多肽的方法 |
| CN106957357B (zh) * | 2017-04-01 | 2021-02-19 | 合肥科生景肽生物科技有限公司 | 一种蝎毒素多肽及其合成方法 |
| JP2022548956A (ja) | 2019-09-20 | 2022-11-22 | ジーランド・ファーマ・ア／エス | Ｋｖ１．３遮断剤 |
| KR20230159403A (ko) | 2021-03-23 | 2023-11-21 | 질랜드 파마 에이/에스 | Kv1.3 차단제 |
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| DK1015576T3 (da) | 1997-09-16 | 2005-08-29 | Egea Biosciences Llc | Fremgangsmåde til fuldstændig kemisk syntese og aggregering af gener og genomer |
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| EP2474316B1 (en) | 2004-10-07 | 2016-04-06 | The Regents of The University of California | Analogs of shk toxin and their uses in selective inhibition of kv1.3 potassium channels |
| US7833979B2 (en) * | 2005-04-22 | 2010-11-16 | Amgen Inc. | Toxin peptide therapeutic agents |
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| AU2008262490B2 (en) | 2007-05-22 | 2011-11-17 | Amgen Inc. | Compositions and methods for producing bioactive fusion proteins |
| WO2009075773A2 (en) | 2007-12-07 | 2009-06-18 | Goldstein Steven A | Identification of toxin ligands |
| WO2010017632A1 (en) | 2008-08-13 | 2010-02-18 | The University Of British Columbia | Methods for stimulating chondrogenesis utilizing a potassium channel inhibitor |
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| US9695228B2 (en) * | 2012-11-21 | 2017-07-04 | Janssen Biotech, Inc. | EGFR and c-Met fibronectin type III domain binding molecules |
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