作者: Luisa Fanzani , Federica Porta , Fiorella Meneghetti , Stefania Villa , Arianna Gelain
DOI: 10.2174/0929867322666150812150036
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摘要: Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance insurgence of drug resistance, which mostly triggered by lack compliance during lengthy treatment. Novel and more effective drugs against Mtb acting on new molecular targets are therefore demand order reduce treatment time address severe issue related progressive loss antibiotic efficacy. encodes for low weight tyrosine specific phosphatases (MPtpA MPtpB) that crucially involved pathogenesis. While MPtpA interferes with phagosome acidification blocking its maturation, MPtpB disrupts host signal transduction cascades, causing immune response subversion host. The important role played both MPtpB host–pathogen interaction makes them appealing targets TB drug discovery. Here, we provide an exhaustive review current knowledge MPtpA and characterization In particular, special emphasis placed all class inhibitors been developed studied date; binding mode, design strategies, biological activities, pharmacophore features well efforts overcome poor druggability of their target summarized detail.