Abstract: The present disclosure relates to monoclonal antibodies anti-FGFR4 and their use as medicaments and diagnostic agents. In particular, it relates to an antibody which specifically binds to the acid box domain of FGFR4 and to specific portions thereof. Nucleic acids coding for said antibody, vectors and host cells for their expression and production, antibody-drug conjugates and pharmaceutical compositions comprising said antibody are also within the scope of the present disclosure. The present disclosure also relates to antibodies anti-FGFR4 for use for detecting, killing, affecting or inhibiting development and/or differentiation of colon cancer stem cells.

Abstract: The present disclosure relates to monoclonal antibodies anti-FGFR4 and their use as medicaments and diagnostic agents. In particular, it relates to an antibody which specifically binds to the acid box domain of FGFR4 and to specific portions thereof. Nucleic acids coding for said antibody, vectors and host cells for their expression and production, antibody-drug conjugates and pharmaceutical compositions comprising said antibody are also within the scope of the present disclosure. The present disclosure also relates to antibodies anti-FGFR4 for use for detecting, killing, affecting or inhibiting development and/or differentiation of colon cancer stem cells.

Abstract: The present invention relates to antibody- or peptide-drug conjugate compounds where one or more cryptophycin derivatives (macrocyclic depsipeptide) are covalently attached by a self-immolative linker which binds to one or more tumor-associated antigens or cell-surface receptors. The linker contains a cleavage site for proteases and a dipeptide unit able to form a diketopiperazine. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders, such as immune or infective diseases.

Abstract: The present invention relates to an assay specific for histone deacetylases HDAC1 and/or 2 inhibitors which comprises: (i) incubating an HDAC1 and/or 2 enzymes(s) together with a protein that contains the SANT and ELM2 regions, found in MTA proteins such as MTA-2, MTA-1, MTA-3 and also found in CoREST, CoREST2, CoREST3 and MI-ER1, in a suitable assay buffer (ii) adding the potential HDAC inhibitor and a suitable substrate and incubating (iii) stopping the incubation and determining the effect the putative HDAC inhibitor has had on enzyme activity by comparison with standards.

Abstract: A method for identifying analytes which are histone deacetylase (HDAC) inhibitors is described. The method provides cells comprising a reporter gene operably linked to a transcription regulatory sequence, which includes nucleotide sequences responsive to a known HDAC inhibitor or subtype, stably integrated into the genome of the cells. A culture of the cells is incubated in medium which contains an analyte and the culture monitored for expression of the reporter gene. Analytes which have HDAC inhibitor activity induce expression of the reporter gene. In particular embodiments, the transcription regulatory region is a sequence of the p21WAF1/CIP1 transcription regulatory sequence which is responsive to a known HDAC inhibitor but not responsive to p53.