Natural products against key Mycobacterium tuberculosis enzymatic targets: Emerging opportunities for drug discovery

Virtual screening and crystallographic studies reveal an unexpected γ-lactone derivative active against MptpB as a potential antitubercular agent

“…MptpB is a mycobacterial extracellular protein, essential for the in vivo viability of Mtb within the host cell. This enzyme shares only about 6% sequence similarity with human phosphatases, thus Interestingly, 1 shares its characteristic core lactone moiety with a natural MptpB inhibitor extracted from Aspergillus terreus SCSIO 41008 [27,28]; this finding contributes to validate this scaffold as a starting point for further developments. Taken together, these results validate the reliability of the VS protocol and highlight the crucial role of crystallographic analyses to unambiguously define the structure of the hit compound, allowing the discovery of a new, unexpected scaffold for the inhibition of MptpB, in the framework of the search for novel anti-TB therapies.…”

Insights on the Modulation of SIRT5 Activity: A Challenging Balance

“…The first part of the following two sections is dedicated to natural products (NPs), which represent an invaluable source of structurally unique bioactive compounds, and a paramount source of new drug candidates [ 17 , 18 , 19 , 20 , 21 ]. Semisynthetic and synthetic derivatives are described in the second part of both sections.…”

GlmU inhibitor from the roots of Euphorbia ebracteolata as an anti-tuberculosis agent

“…With the help of automatic purication system, 18 chromatographic fractions of E. ebracteolata (Fr. [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] were prepared for inhibitory activity assay against GlmU acetyltransferase (Fig. 1c).…”