Exploring Decaprenylphosphoryl-β-d-Ribose 2′-Epimerase 1 (DprE1): A Target for Anti-tubercular Drugs

Yadav, Mange Ram; Murumkar, Prashant R.; Ghuge, Rahul B.; Barot, Rahul R.; Chauhan, Monica

doi:10.1007/978-3-031-15955-8_24

Cited by 3 publications

(2 citation statements)

References 69 publications

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“…40 Decaprenol-1-phosphoribose (DPR) production involves multiple enzymatic steps catalyzed by UbiA, PrsA, and DprE1/DprE2. 41 The addition of arabinofuranosyl residues to the AG backbone is catalyzed by arabinofuranosyl transferase (AftA) and Emb proteins (EmbA and EmbB). 5 AG was linked to the PG layer by Lcp1.…”

Section: Potential Targetsmentioning

confidence: 99%

“…Galactose residues are added to the PG linkage by galactofuranosyltransferases (GlfT1 and GlfT2), whereas arabinose residues are provided by decaprenylphosphoryl- d -arabinose (Araf) . Decaprenol-1-phosphoribose (DPR) production involves multiple enzymatic steps catalyzed by UbiA, PrsA, and DprE1/DprE2 . The addition of arabinofuranosyl residues to the AG backbone is catalyzed by arabinofuranosyl transferase (AftA) and Emb proteins (EmbA and EmbB) .…”

Section: Arabinogalactan Biosynthesis and Potential Targetsmentioning

confidence: 99%

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Revolutionizing Tuberculosis Treatment: Uncovering New Drugs and Breakthrough Inhibitors to Combat Drug-Resistant Mycobacterium tuberculosis

Verma,

Naik,

Kumar

et al. 2023

ACS Infect. Dis.

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Tuberculosis (TB) is a global health threat that causes significant mortality. This review explores chemotherapeutics that target essential processes in Mycobacterium tuberculosis, such as DNA replication, protein synthesis, cell wall formation, energy metabolism, and proteolysis. We emphasize the need for new drugs to treat drug-resistant strains and shorten the treatment duration. Emerging targets and promising inhibitors were identified by examining the intricate biology of TB. This review provides an overview of recent developments in the search for anti-TB drugs with a focus on newly validated targets and inhibitors. We aimed to contribute to efforts to combat TB and improve therapeutic outcomes.

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Section: Potential Targetsmentioning

confidence: 99%

Section: Arabinogalactan Biosynthesis and Potential Targetsmentioning

confidence: 99%

Revolutionizing Tuberculosis Treatment: Uncovering New Drugs and Breakthrough Inhibitors to Combat Drug-Resistant Mycobacterium tuberculosis

Verma,

Naik,

Kumar

et al. 2023

ACS Infect. Dis.

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Design, synthesis, biological evaluation and molecular dynamics of some novel 3-phenylpyrazolo[1,5- a ]pyrimidine-2,7(1 H ,4 H )-dione based compounds as anti-tubercular agents

Chauhan,

Prajapati,

Mirza

et al. 2023

Journal of Biomolecular Structure and Dynamics

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Polymorphism and whole-molecule disorder of an antitubercular 8- nitrobenzothiazinone

Seidel,

Goddard,

Schlegel

et al. 2024

Preprint

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8-Nitrobenzo-1,3-thiazin-4-ones (BTZs) are a promising class of antitubercular agents with a novel mechanism of action, viz. suicide inhibition of decaprenylphosphoryl-β-d-ribose 2’-epimerase (DprE1), an enzyme crucial for cell wall synthesis in the pathogen Mycobacterium tuberculosis. 8-Nitro-2-(piperidin-1-yl)-6-(trifluoromethyl)-4H-benzo-1,3-thiazin-4-one (1) is a chemically simplified analogue of the anti-tuberculosis phase 2 clinical drug candidate BTZ-043. Structural elucidation of 1 in the solid-state has been carried out by X-ray crystallography and two polymorphic forms of 1 have been revealed. 1-I crystallizes in the triclinic system (space group P-1, Z = 6) with one molecule exhibiting whole-molecule disorder with a preferred orientation. The crystal structure of 1-II belongs to the tetragonal system (space group P43, Z = 4) and exhibits positional disorder in several parts of the molecule.

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Exploring Decaprenylphosphoryl-β-d-Ribose 2′-Epimerase 1 (DprE1): A Target for Anti-tubercular Drugs

Cited by 3 publications

References 69 publications

Revolutionizing Tuberculosis Treatment: Uncovering New Drugs and Breakthrough Inhibitors to Combat Drug-Resistant Mycobacterium tuberculosis

Revolutionizing Tuberculosis Treatment: Uncovering New Drugs and Breakthrough Inhibitors to Combat Drug-Resistant Mycobacterium tuberculosis

Design, synthesis, biological evaluation and molecular dynamics of some novel 3-phenylpyrazolo[1,5- a ]pyrimidine-2,7(1 H ,4 H )-dione based compounds as anti-tubercular agents

Polymorphism and whole-molecule disorder of an antitubercular 8- nitrobenzothiazinone

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