198545-00-5Relevant articles and documents
Hydrophilic carbonate type antibody drug conjugate
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Paragraph 0218-0220, (2020/04/29)
The invention provides a hydrophilic carbonate type antibody drug conjugate or a pharmaceutically acceptable salt thereof. The hydrophilic carbonate type antibody drug conjugate or the pharmaceutically acceptable salt thereof provided by the invention can be used for effectively releasing drugs in a tumor weakly acidic microenvironment to obtain a better in-vivo drug effect on tumors, and can be used for obtaining very good in-vivo PK under high DAR.
Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: Discovery of nanomolar, nonselective, and use-dependent antagonists
Fr?lund, Sidsel,Bella, Angelo,Kristensen, Anders S.,Ziegler, Hanne L.,Witt, Matthias,Olsen, Christian A.,Str?mgaard, Kristian,Franzyk, Henrik,Jaroszewski, Jerzy W.
experimental part, p. 7441 - 7451 (2011/02/24)
An array of analogues of the wasp toxin philanthotoxin-433, in which the asymmetric polyamine moiety was exchanged for spermine and the headgroup replaced with a variety of structurally diverse moieties, was prepared using parallel solid-phase synthesis a
Nε-carbonyl> Derivatives of Tri-L-lysine and Tetra-L-lysine as Potential Intermediates in the Block Polymer Synthesis of Macromolecular Drug Conjugates
Rosowsky, Andre,Wright, Joel E.
, p. 5551 - 5558 (2007/10/02)
Tri-L-lysine and tetra-L-lysine derivatives were synthesized with Nε-carbonyl>(Nε-Teoc) protecting groups an all the lysines, or on all but the N-terminal lysine, and with Nα-(tert-butyloxycarbonyl) (Nα-Boc) or Nα-(9-fluorenylmethyloxycarbonyl) (Nα-Fmoc) groups on the N-terminal lysines.Treatment of the Boc/Teoc peptides with p-toluenesulfonic or 2,4,6-trimethylbenzenesulfonic acid led to Boc cleavage with Teoc retention only when the Teoc/Boc ratio was 1:1 or 2:1.In contrast, treatment of the Fmoc/Teoc peptides with liquid ammonia in a sealed vessel cleaved the Fmoc group without significant loss of Teoc groups even when the Fmoc/Teoc ratio was 3:1, showing that Fmoc and Teoc groups provide more selectivity than the Boc and Teoc combination.Nα-Fmoc and Nε-Teoc groups were both stable under catalytic hydrogenolysis conditions.This made it possible to prepare Nα-Fmoc-tri-L-lysine and Nα-Fmoc-tetra-L-lysine derivatives with Nε-Teoc groups on all but the N-terminal lysine and demonstrated that the triad Fmoc/Cbz/Teoc is superior to Boc/Cbz/Teoc in peptide synthesis involving the orthogonal protection strategy.
