- Linker, Antibody-Drug Conjugate Including Same and Use Thereof
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Provided are a linker represented by Formula I or I′, an antibody-drug conjugate containing the same, and use of thereof, a pharmaceutical composition comprising the antibody-drug conjugate, and use of the antibody-drug conjugate for treating and/or preventing a disease.
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Paragraph 0447; 0448
(2021/08/27)
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- ANTICANCER CONJUGATE
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An anticancer conjugate, which comprises a fusion protein comprising domain (a), which is the functional fragment of a sequence of soluble human TRAIL (hTRAIL) protein beginning with an amino acid at a position not lower than hTRAIL95 or a sequence having at least 70% identity with said functional fragment, domain (b) which is the sequence of an effector peptide having proapoptotic, antiangiogenic, antiproliferative or pore forming activity, and conjugation domain (d) for attachment of a chemical compound selected from the group consisting of the sequences Cys Ala Ala Ala Cys Ala Ala Cys and Cys Ala Ala Cys Ala Ala Ala Cys, and a molecule of a chemical compound Z having antiblastic activity, which is attached to said conjugation domain (d) of said fusion protein directly or via a conjugation linker L.
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Page/Page column 63
(2014/09/29)
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- In situ formation of N-trifluoroacetoxy succinimide (TFA-NHS): One-pot formation of succinimidyl esters, N-trifluoroacetyl amino acid succinimidyl esters, and N-maleoyl amino acid succinimidyl esters
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A method for the in situ formation of N-trifluoroacetoxy succinimide (TFA-NHS) and its application in the formation of succinimidyl esters is presented. The developed method provides N-trifluoroacetyl and N-maleoyl amino acid succinimidyl esters from a variety of amino acids using a one-pot, high-yielding protocol. Investigations into the formation of an N-maleoyl amino acid succinimidyl ester supported the proposal of a revised reaction mechanism, and contributed to the optimization of the reaction conditions.
- Leonard, Nicholas M.,Brunckova, Jarmila
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supporting information; experimental part
p. 9169 - 9174
(2011/12/16)
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- Convenient preparation of N-maleoyl amino acid succinimido esters using N-trifluoroacetoxysuccinimide
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One-pot cyclization and esterification of readily available maleamic acid derivatives using N-trifluoroacetoxysuccinimide provide a convenient and cost-effective route to a variety of useful N-maleoyl amino acid N-hydroxysuccinimido esters. Copyright Taylor & Francis Group, LLC.
- Paterson, Michael J.,Eggleston, Ian M.
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p. 303 - 308
(2008/03/17)
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- N-(3-Triethoxysilylpropyl)-4-(N′-maleimidylmethyl)cyclohexanamide (TPMC): A heterobifunctional reagent for immobilization of oligonucleotides on glass surface
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A new heterobifunctional reagent, namely, N-(3-triethoxysilylpropyl)-4-(N′-maleimidylmethyl)cyclohexanamide (TPMC) was developed and its potentiality for fixing of thiol (-SH) modified oligonucleotides were tested. The covalent attachment of oligonucleoti
- Misra, Arvind
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p. 3749 - 3753
(2008/02/10)
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