Abstract: A selection process is iterative and includes an initialization associating with a so-called current molecule a value of a predetermined molecule descriptor associated with the target molecular structure, and during each iteration of the selection process, the process includes evaluating, for each molecule of a database including a plurality of molecules each associated with a value of the descriptor, a so-called overall similarity measure between the value of the descriptor associated with the molecule and the value of the descriptor associated with the current molecule; selecting molecules from the database having an overall similarity measure greater than a predetermined threshold, the selected molecules being added to the reference subset; and updating the value of the descriptor associated with the current molecule from the values of the descriptors associated with at least some of the molecules belonging to the reference subset.

Abstract: A compound comprising a peptide moiety comprising, consisting essentially of, or consisting of, the peptide sequence of a tyrosine cluster YC of the BY-kinase of a Gram positive or Gram negative bacteria, or a fragment or an analogue thereof, and an adenine peptide analogue PNA(A), whereas the peptide moiety and the PNA are linked together. The compound is useful as an inhibitor of bacterial tyrosine kinase.

Abstract: Compounds that are capable of inhibiting the activity of one or more protein kinases are provided. The compounds are short, predominantly basic peptidic compounds comprising between about 5 and about 20 amino acids, and can optionally comprise an ATP mimetic moiety. The protein kinase inhibiting compounds can be used to inhibit the activity of one or more protein kinases in vitro or in vivo. Also provided are methods of inhibiting a protein kinase in a subject by administration of an effective amount of a protein kinase inhibiting compound and the use of the protein kinase inhibiting compounds, alone or in combination with other chemotherapeutic agents, in the treatment of protein kinase mediated diseases and disorders.

Abstract: Compounds that are capable of inhibiting the activity of one or more protein kinases are provided. The compounds are short, predominantly basic peptidic compounds comprising between about 5 and about 20 amino acids, and can optionally comprise an ATP mimetic moiety. The protein kinase inhibiting compounds can be used to inhibit the activity of one or more protein kinases in vitro or in vivo. Also provided are methods of inhibiting a protein kinase in a subject by administration of an effective amount of a protein kinase inhibiting compound and the use of the protein kinase inhibiting compounds, alone or in combination with other chemotherapeutic agents, in the treatment of protein kinase mediated diseases and disorders.

Abstract: A compound comprising a peptide moiety comprising, consisting essentially of, or consisting of, the peptide sequence of a tyrosine cluster YC of the BY-kinase of a Gram positive or Gram negative bacteria, or a fragment or an analogue thereof, and an adenine peptide analogue PNA(A), whereas the peptide moiety and the PNA are linked together. The compound is useful as an inhibitor of bacterial tyrosine kinase.

Abstract: Inhibitors of mammalian protein kinase C isoforms that comprise an inhibitor moiety, which is capable of inhibiting protein kinase activity, operatively associated with a peptide recognition element (PRE), which has an affinity for one or more PKC isoforms are provided. The targeted inhibitory molecules (TIMs) of the present invention are capable of inhibiting one or more PKC isoforms. The TIMs can be designed to target a specific PKC isoform by selection of a PRE component that is shown to preferentially target that PKC isoform. The TIMs are useful as therapeutic agents in the treatment of PKC-related diseases and disorders, such as cancer, psoriasis, angiogenesis, restenosis, atherosclerosis, cardiovascular disease, hypertension, diabetes, neurological disorders, rheumatoid arthritis, kidney disorders, inflammatory disorders and autoimmune disorders.

Abstract: Peptides having a sequence of general formula (I), or the retro form thereof, and having an affinity for one or more mammalian protein kinase C-alpha isoforms are provided: X—[(HY—HB)n-linker]m-(HB—HY)2—HB—(HY)m-Z (I) wherein: HY represents a block of 1 to 4 hydrophobic amino acid residues selected from the group of: Ala, Gly, He, Leu, Phe and Val; HB represents a block of 1 to 4 amino acid residues capable of forming hydrogen bonds selected from the group of: Arg, Asn, Asp, Glu, Gln, Lys and Ser; “linker” represents 1 to 4 Gly residues; n is 1, 2 or 3; m is 0 or 1; X represents the N-terminus of the peptide or a modified version thereof, and Z represents the C-terminus of the peptide or a modified version thereof. The peptides can be used as probes, screening agents, targeting agents, purification agents and diagnostic agents.

Abstract: Compounds that are capable of inhibiting the activity of one or more protein kinases are provided. The compounds are short, predominantly basic peptidic compounds comprising between about 5 and about 20 amino acids, and can optionally comprise an ATP mimetic moiety. The protein kinase inhibiting compounds can be used to inhibit the activity of one or more protein kinases in vitro or in vivo. Also provided are methods of inhibiting a protein kinase in a subject by administration of an effective amount of a protein kinase inhibiting compound and the use of the protein kinase inhibiting compounds, alone or in combination with other chemotherapeutic agents, in the treatment of protein kinase mediated diseases and disorders.