Centre National De La Recherche Scientifique

UniversitÉde Strasbourg

Syndivia

Commissariat &#xc0; L'&#xc9;nergie Atomique Et Aux &#xc9;nergies Alternatives

Oleksandr Koniev

Alain Wagner

Sergii Kolodych

Igor Dovgan

Frédéric Taran

Jean-yves Bonnefoy

Disclosed is a process for preparation of heterogeneous monodisperse mixtures of protein conjugates with a defined degree of conjugation (1-8) obtained by using a tri-functional reagent allowing affinity concentration followed by subsequent simultaneous release-functionalization.

Bioconjugates with a controlled degree of conjugation, their process of preparation, and the reagents for their preparation

This invention pertains to protein-drug conjugates that may be used in the treatment of cancers and to pharmaceutical compositions containing the same. The protein-drug conjugate has the following formula (I), wherein: L is a cysteine-containing protein residue linked through one or more of the cysteine groups of the protein, Ris selected from the group consisting of arylene, arylene-heteroarylene, heteroarylene-arylene and heteroarylene, n is an integer from 0 to 5, p and q are independently 0 or 1, R, Rand Z are spacers, u is 0 or 1 and T is a cleavable unit sensitive to hydrolases, k is 1 or 2 and D is a cytotoxic drug residue selected from dolastatin residues, which may be identical to or different from each other when k is 2, m is the mean payload-to-protein ratio (PPR) of the conjugate, which ranges from 0.1 to 16. 

Protein-drug conjugates and their use in the treatment of cancers

The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

3-aryl propiolonitrile compounds for thiol labeling

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Strasbourg, France

Oleksandr Koniev