DI-SULFIDE CONTAINING CELL PENETRATING PEPTIDES AND METHODS OF MAKING AND USING THEREOF
Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pa...
Saved in:
| Main Authors | , |
|---|---|
| Format | Patent |
| Language | English |
| Published |
26.05.2022
|
| Subjects | |
| Online Access | Get full text |
Cover
Loading…
| Abstract | Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction. |
|---|---|
| AbstractList | Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction. |
| Author | PEI, Dehua QIAN, Ziqing |
| Author_xml | – fullname: QIAN, Ziqing – fullname: PEI, Dehua |
| BookMark | eNrjYmDJy89L5WQId_HUDQ71cfN0cVVw9vcLcfT08_RzV3B29fFRCHD1cw0JcgwBCQS4BoQA1QQrOPq5KPi6hnj4uwQr-Lsp-Dp6g6RBoqHBIFaIh2uQq78bDwNrWmJOcSovlOZmUHZzDXH20E0tyI9PLS5ITE7NSy2JDw02MjAyMjQzsDC0dDQ0Jk4VAKHKM1Y |
| ContentType | Patent |
| DBID | EVB |
| DatabaseName | esp@cenet |
| DatabaseTitleList | |
| Database_xml | – sequence: 1 dbid: EVB name: esp@cenet url: http://worldwide.espacenet.com/singleLineSearch?locale=en_EP sourceTypes: Open Access Repository |
| DeliveryMethod | fulltext_linktorsrc |
| Discipline | Medicine Chemistry Sciences |
| ExternalDocumentID | US2022160819A1 |
| GroupedDBID | EVB |
| ID | FETCH-epo_espacenet_US2022160819A13 |
| IEDL.DBID | EVB |
| IngestDate | Fri Aug 02 08:57:10 EDT 2024 |
| IsOpenAccess | true |
| IsPeerReviewed | false |
| IsScholarly | false |
| Language | English |
| LinkModel | DirectLink |
| MergedId | FETCHMERGED-epo_espacenet_US2022160819A13 |
| Notes | Application Number: US202117538330 |
| OpenAccessLink | https://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20220526&DB=EPODOC&CC=US&NR=2022160819A1 |
| ParticipantIDs | epo_espacenet_US2022160819A1 |
| PublicationCentury | 2000 |
| PublicationDate | 20220526 |
| PublicationDateYYYYMMDD | 2022-05-26 |
| PublicationDate_xml | – month: 05 year: 2022 text: 20220526 day: 26 |
| PublicationDecade | 2020 |
| PublicationYear | 2022 |
| RelatedCompanies | Ohio State Innovation Foundation |
| RelatedCompanies_xml | – name: Ohio State Innovation Foundation |
| Score | 3.3984625 |
| Snippet | Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is... |
| SourceID | epo |
| SourceType | Open Access Repository |
| SubjectTerms | CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES |
| Title | DI-SULFIDE CONTAINING CELL PENETRATING PEPTIDES AND METHODS OF MAKING AND USING THEREOF |
| URI | https://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20220526&DB=EPODOC&locale=&CC=US&NR=2022160819A1 |
| hasFullText | 1 |
| inHoldings | 1 |
| isFullTextHit | |
| isPrint | |
| link | http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwfV3dS8MwEA9jivqmU_FjSkDpW3Htuq59GNIl6Vpd07KmurexZi0I0g1X8d83CZvuaU9J7kJIDn65y8fdAfDYt5xSWKFzXZRctwrL1h3uyHzEjlF2FnnZU5nnImoHmfUy7U0b4HPrC6PihP6o4IgCUVzgvVb79er_Egurv5Xrp_xDkJbPPhtgbXM6ll6jpq3h4YAkMY6RhtAgSzU6UTzDlvrPE2elA2FI9yUeyNtQ-qWsdpWKfwoOEzFeVZ-BRlG1wDHa5l5rgaNo8-Qtqhv0rc_BOw71NBv7ISYQxZR5IQ3pCCIyHsOEUMLkhZMgJCRhok8KPYphRFgQ4xTGPoy8V8mWVJltYwRZQCYk9i_Ag08YCnQxw9mfQGZZuruc7iVoVsuquAKwnxtWOTe7fGFwyzW5a85zt8OF0eYucrfk16C9b6Sb_exbcCKb8u3ctNugWX99F3dCJdf5vZLkLwF1h18 |
| link.rule.ids | 230,309,783,888,25576,76876 |
| linkProvider | European Patent Office |
| linkToHtml | http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwfR1dS8MwMIwpzjedih9TA0rfimvXde3DkK5J17o2LWuqextr1oIg3XAV_75J2NSnPSXchSM5uNxdLncHwOPAsEpuhS5UPjLVKAxTtZgl-hFbWtld5mVfdp6LiOlnxsusP2uAj10ujKwT-i2LI3KJYlzea3lfr_8esZD8W7l5yt85aPXs0SFStt6xyBrVTQWNhjiJUewqrjvMUoVMJU4zhf5zuK90wI3sgZAH_DoSeSnr_0rFOwGHCadX1aegUVRt0HJ3vdfa4Cjahrz5dCt9mzPwhgI1zUIvQBi6MaFOQAIyhi4OQ5hggql4cOKABCeUr0mhQxCMMPVjlMLYg5EzEWgBFd02xpD6eIpj7xw8eJi6vsp3OP9lyDxL_x-ndwGa1aoqLgEc5JpRLvQeW2rMsHVm64vc7jJutNnL3C7ZFejso3S9H30PWj6NwnkYkMkNOBYoEUfXzQ5o1p9fxS1Xz3V-J7n6A4dHilI |
| openUrl | ctx_ver=Z39.88-2004&ctx_enc=info%3Aofi%2Fenc%3AUTF-8&rfr_id=info%3Asid%2Fsummon.serialssolutions.com&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Apatent&rft.title=DI-SULFIDE+CONTAINING+CELL+PENETRATING+PEPTIDES+AND+METHODS+OF+MAKING+AND+USING+THEREOF&rft.inventor=QIAN%2C+Ziqing&rft.inventor=PEI%2C+Dehua&rft.date=2022-05-26&rft.externalDBID=A1&rft.externalDocID=US2022160819A1 |