JP2006514104A5 - - Google Patents
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- Publication number
- JP2006514104A5 JP2006514104A5 JP2005502348A JP2005502348A JP2006514104A5 JP 2006514104 A5 JP2006514104 A5 JP 2006514104A5 JP 2005502348 A JP2005502348 A JP 2005502348A JP 2005502348 A JP2005502348 A JP 2005502348A JP 2006514104 A5 JP2006514104 A5 JP 2006514104A5
- Authority
- JP
- Japan
- Prior art keywords
- conjugate
- amino acid
- activity
- hydrophobic
- gsk
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 230000002209 hydrophobic effect Effects 0.000 claims 20
- 108090000765 processed proteins & peptides Proteins 0.000 claims 17
- 230000000694 effects Effects 0.000 claims 13
- 102000001267 GSK3 Human genes 0.000 claims 12
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims 12
- 229920001184 polypeptide Polymers 0.000 claims 11
- 102000004196 processed proteins & peptides Human genes 0.000 claims 11
- 125000000539 amino acid group Chemical group 0.000 claims 8
- 150000001413 amino acids Chemical group 0.000 claims 7
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 6
- 235000014113 dietary fatty acids Nutrition 0.000 claims 6
- 229930195729 fatty acid Natural products 0.000 claims 6
- 239000000194 fatty acid Substances 0.000 claims 6
- 150000004665 fatty acids Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 230000002401 inhibitory effect Effects 0.000 claims 5
- 239000004480 active ingredient Substances 0.000 claims 4
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims 4
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 claims 4
- 239000004471 Glycine Substances 0.000 claims 3
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 3
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 3
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 3
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 3
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 3
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 3
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 3
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 3
- 208000019022 Mood disease Diseases 0.000 claims 3
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 3
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 3
- 235000004279 alanine Nutrition 0.000 claims 3
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 3
- 235000018417 cysteine Nutrition 0.000 claims 3
- 229960000310 isoleucine Drugs 0.000 claims 3
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 3
- 229930182817 methionine Natural products 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 3
- 125000000430 tryptophan group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12 0.000 claims 3
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 3
- 239000004474 valine Substances 0.000 claims 3
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 239000005022 packaging material Substances 0.000 claims 2
- 208000017194 Affective disease Diseases 0.000 claims 1
- 102000015735 Beta-catenin Human genes 0.000 claims 1
- 108060000903 Beta-catenin Proteins 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 230000035578 autophosphorylation Effects 0.000 claims 1
- 230000001268 conjugating effect Effects 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000001320 hippocampus Anatomy 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000035699 permeability Effects 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43264402P | 2002-12-12 | 2002-12-12 | |
| US48271903P | 2003-06-27 | 2003-06-27 | |
| PCT/IL2003/001057 WO2004052404A2 (en) | 2002-12-12 | 2003-12-11 | Glycogen synthase kinase-3 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006514104A JP2006514104A (ja) | 2006-04-27 |
| JP2006514104A5 true JP2006514104A5 (enExample) | 2007-01-25 |
Family
ID=32511656
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2005502348A Pending JP2006514104A (ja) | 2002-12-12 | 2003-12-11 | グリコーゲンシンターゼキナーゼ−３阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US7446092B2 (enExample) |
| EP (1) | EP1569956B1 (enExample) |
| JP (1) | JP2006514104A (enExample) |
| KR (1) | KR20050091716A (enExample) |
| AU (1) | AU2003286411A1 (enExample) |
| CA (1) | CA2509374A1 (enExample) |
| WO (1) | WO2004052404A2 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001049709A1 (en) * | 2000-01-03 | 2001-07-12 | Ramot University Authority For Applied Research & Industrial Development Ltd. | Glycogen synthase kinase-3 inhibitors |
| US7378432B2 (en) | 2001-09-14 | 2008-05-27 | Tel Aviv University Future Technology Development L.P. | Glycogen synthase kinase-3 inhibitors |
| AU2003286411A1 (en) * | 2002-12-12 | 2004-06-30 | Tel Aviv University Future Technology Development L.P. | Glycogen synthase kinase-3 inhibitors |
| AU2005234687A1 (en) * | 2003-06-27 | 2005-12-08 | Tel Aviv Universtiy Future Technology Development L.P. | Glycogen Synthase Kinase-3 Inhibitors |
| WO2008075366A2 (en) * | 2006-12-20 | 2008-06-26 | Medwell Laboratories Ltd. | Novel conjugates of polyunsaturated fatty acids with amines and therapeutic uses thereof |
| US8263547B2 (en) * | 2008-05-28 | 2012-09-11 | Massachusetts Institute Of Technology | DISC-1 pathway activators in the control of neurogenesis |
| AU2008258150B1 (en) * | 2008-12-16 | 2009-03-19 | Jorge Miguel Pereira | An Improved Knee Pad |
| US9265764B2 (en) * | 2009-02-27 | 2016-02-23 | Massachusetts Institute Of Technology | Uses of chemicals to modulate GSK-3 signaling for treatment of bipolar disorder and other brain disorders |
| US9243034B2 (en) | 2011-01-27 | 2016-01-26 | Ramot At Tel-Aviv University Ltd. | Glycogen synthase kinase-3 inhibitors |
| EP2668200B1 (en) | 2011-01-27 | 2017-03-15 | Ramot at Tel-Aviv University Ltd. | Glycogen synthase kinase-3 inhibitors |
| US9718859B2 (en) | 2013-06-24 | 2017-08-01 | Ramot At Tel-Aviv University Ltd. | Glycogen synthase kinase-3 inhibitors |
| US20170165230A1 (en) | 2014-04-09 | 2017-06-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
| RS61853B1 (sr) | 2014-10-29 | 2021-06-30 | Bicyclerd Ltd | Biciklični peptidni ligandi specifični za mt1-mmp |
| CN110506049B (zh) * | 2016-12-23 | 2024-08-16 | 拜斯科技术开发有限公司 | 用于结合mt1-mmp的肽配体 |
| US11730819B2 (en) * | 2016-12-23 | 2023-08-22 | Bicycletx Limited | Peptide derivatives having novel linkage structures |
| EP3645549A1 (en) | 2017-06-26 | 2020-05-06 | BicycleRD Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
| JP7670481B2 (ja) | 2017-08-04 | 2025-04-30 | バイスクルテクス・リミテッド | Ｃｄ１３７に対して特異的な二環式ペプチドリガンド |
| KR20200128518A (ko) | 2018-02-23 | 2020-11-13 | 바이사이클티엑스 리미티드 | 다량체성 비사이클릭 펩타이드 리간드 |
| GB201810320D0 (en) * | 2018-06-22 | 2018-08-08 | Bicycletx Ltd | Peptide ligands for binding to CD38 |
| US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
| GB201810329D0 (en) * | 2018-06-22 | 2018-08-08 | Bicycletx Ltd | Peptide ligands for binding to integrin avB3 |
| GB201820325D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for psma |
| GB201820295D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for MT1-MMP |
| GB201820288D0 (en) | 2018-12-13 | 2019-01-30 | Bicycle Tx Ltd | Bicycle peptide ligaands specific for MT1-MMP |
| CN113474045A (zh) | 2018-12-21 | 2021-10-01 | 拜斯科技术开发有限公司 | Pd-l1特异性的双环肽配体 |
| WO2020128527A1 (en) | 2018-12-21 | 2020-06-25 | Bicyclerd Limited | Bicyclic peptide ligands specific for pd-l1 |
| GB201900529D0 (en) | 2019-01-15 | 2019-03-06 | Bicycletx Ltd | Bicyclic peptide ligands specific for CD38 |
| GB201900530D0 (en) * | 2019-01-15 | 2019-03-06 | Bicyclerd Ltd | Bicyclic peptide ligands specific for CD38 |
| TWI862640B (zh) | 2019-07-30 | 2024-11-21 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
| KR20230074119A (ko) | 2020-08-03 | 2023-05-26 | 바이사이클티엑스 리미티드 | 펩타이드 기반 링커 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1471621A (en) * | 1922-02-18 | 1923-10-23 | Arthur W Mccord | Soap-dispensing device |
| US2046068A (en) * | 1934-03-03 | 1936-06-30 | Arthur W Gray | Device for measuring materials |
| GB781806A (en) | 1955-04-29 | 1957-08-28 | Roche Products Ltd | Organic phosphate, salts thereof, and process for the manufacture thereof |
| US3193159A (en) * | 1964-02-24 | 1965-07-06 | Vernon E Swindler | Dispenser for comminuted material and the like |
| US4186646A (en) * | 1973-08-17 | 1980-02-05 | Martin Carl D | Adjustable charging bar |
| AU670704B2 (en) | 1993-06-30 | 1996-07-25 | Pharmacia & Upjohn S.P.A. | Peptide inhibitors of mitogenesis and motogenesis |
| US5861266A (en) | 1994-02-28 | 1999-01-19 | New York University | Treatment of diabetes mellitus and insulin receptor signal transduction |
| US5462101A (en) * | 1994-07-05 | 1995-10-31 | Mouchmouchian; Silva | Baby feeding system |
| US5807718A (en) | 1994-12-02 | 1998-09-15 | The Scripps Research Institute | Enzymatic DNA molecules |
| DE19524133A1 (de) | 1995-07-03 | 1997-01-09 | Bayer Ag | Die Verwendung von neuen und bekannten kationischen 4,5-Dihydro-1H-1,2,3-triazoliumverbindungen als Farbstoffe, neue kationische 4,5-Dihydro-1H-1,2,3-triazoliumverbindungen und deren Herstellung |
| US5948765A (en) | 1996-03-15 | 1999-09-07 | Washington University | Inhibition of intracellular signal transduction by 14-3-3-binding peptides |
| US6057117A (en) * | 1996-04-04 | 2000-05-02 | Chiron Corporation | Identification and use of selective inhibitors of glycogen synthase kinase 3 |
| EP1019043A4 (en) | 1996-05-07 | 2003-07-30 | Univ Pennsylvania | INHIBITORS OF GLYCOGEN SYNTHESIS KINASE 3 AND METHOD FOR THEIR IDENTIFICATION AND USE |
| US6077954A (en) | 1996-08-01 | 2000-06-20 | Isis Pharmaceuticals, Inc. | Substituted heterocyclic compounds |
| WO1998016528A1 (en) | 1996-10-11 | 1998-04-23 | Chiron Corporation | Purine inhibitors of glycogen synthase kinase 3 (gsk3) |
| US6441140B1 (en) | 1998-09-04 | 2002-08-27 | Cell Signaling Technology, Inc. | Production of motif-specific and context-independent antibodies using peptide libraries as antigens |
| WO2000045237A2 (en) | 1999-01-27 | 2000-08-03 | Enbaya Ltd. | Progressive compression of triangular meshes |
| US6495376B1 (en) | 1999-02-18 | 2002-12-17 | Beth Israel Deaconess Medical Center | Methods and compositions for regulating protein-protein interactions |
| GB9906245D0 (en) | 1999-03-19 | 1999-05-12 | Medical Res Council | Enzyme |
| IL133243A0 (en) | 1999-03-30 | 2001-03-19 | Univ Ramot | A method and system for super resolution |
| IL130325A0 (en) | 1999-06-07 | 2000-06-01 | Yeda Res & Dev | Pharmaceutical compositions comprising allicin |
| WO2001049709A1 (en) | 2000-01-03 | 2001-07-12 | Ramot University Authority For Applied Research & Industrial Development Ltd. | Glycogen synthase kinase-3 inhibitors |
| KR100564902B1 (ko) | 2000-08-21 | 2006-03-30 | 주식회사 태평양 | 신규 티오우레아 유도체 및 이를 함유하는 약제학적 조성물 |
| WO2002024941A2 (en) * | 2000-09-22 | 2002-03-28 | University Of Dundee | Protein kinase regulation |
| US7378432B2 (en) | 2001-09-14 | 2008-05-27 | Tel Aviv University Future Technology Development L.P. | Glycogen synthase kinase-3 inhibitors |
| AU2003286411A1 (en) | 2002-12-12 | 2004-06-30 | Tel Aviv University Future Technology Development L.P. | Glycogen synthase kinase-3 inhibitors |
| GB2396109B (en) | 2002-12-12 | 2006-04-19 | Johnson & Johnson Medical Ltd | Absorbent multilayer hydrogel wound dressings |
| AU2005234687A1 (en) | 2003-06-27 | 2005-12-08 | Tel Aviv Universtiy Future Technology Development L.P. | Glycogen Synthase Kinase-3 Inhibitors |
| CA2530111A1 (en) | 2003-06-27 | 2005-01-06 | Tel-Aviv University Future Technology Development L.P. | Glycogen synthase kinase-3 inhibitors |
-
2003
- 2003-12-11 AU AU2003286411A patent/AU2003286411A1/en not_active Abandoned
- 2003-12-11 WO PCT/IL2003/001057 patent/WO2004052404A2/en not_active Ceased
- 2003-12-11 EP EP03777156.5A patent/EP1569956B1/en not_active Expired - Lifetime
- 2003-12-11 CA CA002509374A patent/CA2509374A1/en not_active Abandoned
- 2003-12-11 US US10/538,171 patent/US7446092B2/en not_active Expired - Lifetime
- 2003-12-11 KR KR1020057010710A patent/KR20050091716A/ko not_active Ceased
- 2003-12-11 JP JP2005502348A patent/JP2006514104A/ja active Pending
-
2008
- 2008-05-29 US US12/155,087 patent/US7833974B2/en not_active Expired - Fee Related
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