Naphthoquinone amino acid derivatives, synthesis and biological activity as proteasome inhibitors
The ubiquitin-proteasome system has been largely investigated for its key role in protein degradation mechanisms that regulate both apoptosis and cell division. Because of their antitumour activity, different classes of proteasome inhibitors have been identified to date. Some of these compounds are currently employed in the clinical treatment of several types of cancer among which multiple myeloma. Here, we describe the design, chemistry, biological activity and modelling studies of a large series of amino acid derivatives linked to a naphthoquinone pharmacophoric group through variable spacers. Some analogues showed interesting inhibitory potency for the β1 and β5 subunits of the proteasome with IC50 values in the sub-μm range.
Kinetically Controlled Stepwise Self-Assembly of AuI-Metallopeptides in Water
The combination of attractive supramolecular interactions of a hydrophobic AuI-metallopeptide with the shielding effect of flexible oligoethylene glycol chains provides access to a stepwise self-assembly of a AuI-metalloamphiphile in water. Kinetic control of the supramolecular polymer morphology is achieved using a temperature-dependent assembly protocol, which yields low dispersity supramolecular polymers (metastable state I) or helical bundled nanorods (state II).
Kemper, Benedict,Zengerling, Lydia,Spitzer, Daniel,Otter, Ronja,Bauer, Tobias,Besenius, Pol
supporting information
p. 534 - 537
(2018/01/26)
CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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Page/Page column 221
(2013/06/05)
CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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Page/Page column
(2013/06/04)
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