182918-73-6Relevant articles and documents
PRODRUGS WITH A TRIDENTATE SELF-IMMOLATIVE LINKER
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, (2020/07/08)
The present application provides a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein L1, L2, L3, n, m, p, X, T, TR, and D are as described herein. Methods of using of these compounds to treat diseases advantageously treatable by drug D are also described.
SELF-IMMOLATIVE LINKERS CONTAINING MANDELIC ACID DERIVATIVES, DRUG-LIGAND CONJUGATES FOR TARGETED THERAPIES AND USES THEREOF
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, (2015/03/28)
The invention provides a therapeutic drug and targeting conjugate, pharmaceutical compositions containing these conjugates in pharmaceutical composition, and uses of these conjugates in anti-neoplastic and other therapeutic regimens. Also provided are novel intermediates thereof. The conjugates provide a therapeutic drug fragment or prodrug fragment bound to a targeting moiety via a linker which comprises a substrate cleavable by a protease such as Cathepsin B. The targeting moiety is a ligand which targets a cell surface molecule, such as a cell surface receptor on an anti-neoplastic cell. The ligand may function solely as a targeting moiety or may itself have a therapeutic effect. Following administration of the therapeutic drug and targeting conjugate of formula I and exposure of the conjugate to the protease specific for the substrate, the linker is cleaved and the targeting moiety is separated from the conjugate, which causes the drug fragment or prodrug fragment to convert to the drug or prodrug. The recited conjugates are useful in anti-neoplastic therapies. Also provided are methods of making the therapeutic drug and targeting conjugates and intermediates thereof, and kits comprising the therapeutic drug and targeting conjugates.
Developing novel activity-based fluorescent probes that target different classes of proteases.
Zhu, Qing,Girish, Aparna,Chattopadhaya, Souvik,Yao, Shao Q
, p. 1512 - 1513 (2007/10/03)
In this article, we report the design and synthesis of a group of novel activity-based probes that target different protease sub-classes based on their substrate specificities, rather than their enzymatic mechanisms. The feasibility of our approach has be
