A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.

Zhang; Zhong-Yin

He; Yantao

Zeng; Li-Fan

Indiana University Research and Technology Corporation

Tyrosine phosphatase inhibitors and uses thereof to modulate the activity of enzymes involved in the pathology of Mycobacterium tuberculosis

Peptide sequence capable of initiating delayed hypersensitivity reactions of different intensity in the presence of living bacteria as opposed to dead bacteria of the Mycobacterium tuberculosis complex. The sequence is characterized in that it comprises no more than 0.5% by weight of tyrosine, phenylalanine, methionine, histidine, arginine and cysteine amino acids. The invention also concerns the diagnostic and therapeutic applications of a peptide or protein comprising said sequence.

Institut Pasteur

Peptide sequence capable of inducing a delayed-type hypersensitivity reaction in the presence of living bacteria of the Mycobacterium tuberculosis complex and its applications

The present invention provides mutant Mycobacterium strains harboring a modified tyrosine phosphatase gene (mptpA or mptpB) wherein the mutant Mycobacterium strain is incapable of expressing the active tyrosine phosphatase. The invention provides a method for developing the said mutant strain from either Mycobacterium tuberculosis or Mycobacterium bovis. The mptpA or mptpB gene may be modified by replacing the internal sequences with an antibiotic resistance marker gene, which disrupts the expression of the active gene. The invention further provides a recombinant vector comprising the modified mptpA or mptpB which may be used to develop the mutant strains of mycobacteria. The invention provides a method to assess the role of tyrosine phosphatases MptpA and MptpB in the virulence and pathogenesis of Mycobacterium which can be used as potential targets for developing anti-tubercular drug.

tuberculosis/tyrosine

Tyrosine phosphatase inhibitors and uses thereof to modulate the activity of enzymes involved in the pathology of Mycobacterium tuberculosis

Peptide sequence capable of inducing a delayed-type hypersensitivity reaction in the presence of living bacteria of the Mycobacterium tuberculosis complex and its applications

Mutants of mycobacteria and process thereof

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