Universiteit Utrecht Holding B.v.

Pamgene Bv

Cristal Delivery B.v.

Robertus Matthias Joseph Liskamp

Wilhelmus Everhardus Hennink

Isil Altintas

Cristianne Johanna Ferdinand Rijcken

Robby Ruijtenbeek

Cornelis Franciscus Van Nostrum

Jeroen Van Ameijde

Steffen Van Der Wal

Johannes Anna Wilhelmus Kruijtzer

The present invention relates to a method and tools which allow the kinetic monitoring of hydrolase enzyme activity. The present invention also aims to provide synthetic peptides and peptide residues modified such that they can be used in assays for monitoring hydrolase enzyme activity, and preferably phosphatase activity. Also claimed are modified tyrosine amino acid derivatives of formula (IV), wherein Y is chosen from &#x2014;POwith y equal to 2 or 3 and esters thereof, &#x2014;SOwith z equal to 2 or 3 and esters thereof, a carbohydrate or carbohydrate derivatives; and; wherein Xand/or Xis selected from &#x2014;N, &#x2014;NO, &#x2014;CI, or &#x2014;CN, &#x2014;SCN, a Cto Calkyl, or H, wherein either Xor Xis not H. 

Modified tyrosine amino acids, peptides containing them, and their use for detecting hydrolase enzyme activity

The present invention relates to a particular class of biodegradable linkers, ensuring transiently stable conjugation of building blocks and/or bioactive compounds into drug delivery systems (DDS), such as DDS based on polymeric micelles or hydrogels. In addition, the present invention relates to compounds, comprising said linkers, such compounds preferably being prodrugs. Further, the invention is directed to the use of said linkers, and especially said biodegradable linkers, in a drug delivery system. Moreover, the invention relates to controlled release system comprising a polymer matrix, capable of releasing an active ingredient, wherein the active ingredient is covalently linked to the polymer molecules of the polymer matrix through said linkers, as well as to a method of synthesizing these linkers and preparing such controlled release systems.

Tunable, biodegradable linker molecules for transient conjugation of components in drug delivery systems, and drug delivery systems prepared therewith

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Utrecht, Netherlands

Robertus Matthias Joseph Liskamp