@article {44424,
	title = {Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life},
	journal = {European Journal of Medicinal Chemistry},
	volume = {152},
	year = {2018},
	month = {MAY},
	pages = {358-369},
	abstract = {Non-natural antimicrobial peptides are ideal as next-generation antibiotics because of their ability to circumvent the problems of drug resistance and in vivo instability. We report novel all-alpha- and alpha,gamma-mixed Tat peptide analogues as potential antibacterial and anti-TB agents. These peptides have broad spectrum antibacterial activities against Gram-positive (MICs 0.61 +/- 0.03 to 1.35 +/- 0.21 mu M with the peptide gamma TatM4) and Gram-negative (MICs 0.71 +/- 0.005 to 1.26 +/- 0.02 M with gamma TatM4) bacteria and are also effective against active and dormant forms of Mycobacterium tuberculosis, including strains that are resistant to rifampicin and isoniazid. The introduction of the non-natural amino acids of the study in the Tat peptide analogues results in increased resistance to degradation by proteolysis, significantly increasing their half-life. The peptides appear to inhibit bacteria by a membrane disruption mechanism, and have only a low cytotoxic effect on mammalian cells. (C) 2018 Elsevier Masson SAS. All rights reserved.},
	doi = {10.1016/j.ejmech.2018.04.039},
	author = {Bhosle, Govind S. and Nawale, Laxman and Yeware, Amar M. and Sarkar, Dhiman and Fernandes, Moneesha}
}
