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Inkorporation von pharmakologisch wirksamen Aminosaeureanaloga in Proteine

Composition containing peptide that includes amino acid analogue, especially thio-proline - used for delivery of active analogues, e.g. for cancer therapy, provides targetting and reduction in dose and side effects
: Budisa, N.; Huber, R.; Minks, C.; Moroder, L.

Frontpage ()

DE 1997-19724670 A: 19970611
DE 1997-19724670 A: 19970611
EP 1998-936310 AW: 19980605
WO 1998-EP3398 A: 19980605
DE 19724670 A1: 19981224
EP 998487 A1: 20000510
Patent, Elektronische Publikation
Fraunhofer IME ()

Die Erfindung betrifft eine pharmazeutische Zusammensetzung, die als Wirkstoff mindestens ein pharmakologisch wirksames Aminosaeureanalogon eingebaut in ein Peptid oder Polypeptid als Traeger oder Vehikel enthaelt. Weiterhin werden Verfahren zur Herstellung solcher pharmazeutischer Zusammensetzungen offenbart.


WO 9856824 A UPAB: 19990302 Pharmaceutical composition (A) contains as active ingredient at least one amino acid analogue (I) incorporated into a carrier (poly)peptide (II), and optionally usual auxiliaries, additives and carriers. Also new are polypeptides (IIa) containing at least one thioproline (sPro) residue. USE - (A) are used to deliver active (I) to humans and other mammals. The peptides containing (I) are broken down in vivo, releasing (I). Typically (I) is sPro, used as anticancer agent; a selenium-containing amino acid (aa) for use as anticancer agent or antimicrobial (particularly antimycotic), or diodotyrosine or melatonin, for increasing production of hormones. ADVANTAGE - Peptides containing (I) retain the steric properties, folding and functional properties (including immunogenicity and antigenicity) of the Wild-type peptide, and avoid many of the side effects associated with administration of free (I). Biological methods for production of the new peptides ensure that only L-(I) is incorporated, eliminating side effects caused by the D-enantiomer. By appropriate choice of carrier, (I) can be targetted to specific sites in the body (including crossing of the blood-brain barrier).