ArticleJournal of medicinal chemistry2015
Targeting Mycobacterium tuberculosis Biotin Protein Ligase (MtBPL) with Nucleoside-Based Bisubstrate Adenylation Inhibitors.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 44 citations in OpenAlex.
- Synthesis of New DltA Inhibitors and Their Application as Adjuvant Antibiotics to Re-Sensitize Methicillin-ResistantMolecules (Basel, Switzerland) · 2025Article
- Co-crystal structure of Helicobacter pylori biotin protein ligase with biotinyl-5-ATP.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Design and synthesis of a library of C2-substituted sulfamidoadenosines to probe bacterial permeability.Bioorganic & medicinal chemistry letters · 2024Article
- The implication of Mycobacterium tuberculosis-mediated metabolism of targeted xenobiotics.Nature reviews. Chemistry · 2023Review
- Structural Study of Potent Triazole-Based Inhibitors ofACS medicinal chemistry letters · 2023Article
- Biotin-dependent cell envelope remodelling is required for Mycobacterium abscessus survival in lung infection.Nature microbiology · 2023Article
- Synthesis and Anticancer and Antiviral Activities of C-2'-Branched Arabinonucleosides.International journal of molecular sciences · 2022Article
- In Vitro Scolicidal Activity of the Sesquiterpenes Isofuranodiene, α-Bisabolol and Farnesol onMolecules (Basel, Switzerland) · 2020Article
- Advanced Resistance Studies Identify Two Discrete Mechanisms inAntibiotics (Basel, Switzerland) · 2020Article
- The Biotin Biosynthetic Pathway in Mycobacterium tuberculosis is a Validated Target for the Development of Antibacterial Agents.Current medicinal chemistry · 2020Review
- A Novel Lipoate-Protein Ligase, Mhp-LplJ, Is Required for Lipoic Acid Metabolism inFrontiers in microbiology · 2020Article
- A single regulator NrtR controls bacterial NADeLife · 2019Article
- Targeting adenylate-forming enzymes with designed sulfonyladenosine inhibitors.The Journal of antibiotics · 2019Review
- In Vitro and In Vivo Effectiveness of Carvacrol, Thymol and Linalool againstMolecules (Basel, Switzerland) · 2019Article
- Active Essential Oils and Their Components in Use against Neglected Diseases and Arboviruses.Oxidative medicine and cellular longevity · 2019Review
- Novel 5'-Norcarbocyclic Pyrimidine Derivatives as Antibacterial Agents.Molecules (Basel, Switzerland) · 2018Article
- Avoiding Antibiotic Inactivation in Mycobacterium tuberculosis by Rv3406 through Strategic Nucleoside Modification.ACS infectious diseases · 2018Article
- Targeting protein biotinylation enhances tuberculosis chemotherapy.Science translational medicine · 2018Article
- Trypanosoma brucei Inhibition by Essential Oils from Medicinal and Aromatic Plants Traditionally Used in Cameroon (Azadirachta indica, Aframomum melegueta, Aframomum daniellii, Clausena anisata, Dichrostachys cinerea and Echinops giganteus).International journal of environmental research and public health · 2017Article
- New Series of BPL Inhibitors To Probe the Ribose-Binding Pocket ofACS medicinal chemistry letters · 2016Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
Mycobacterium tuberculosis (Mtb), responsible for both latent and symptomatic tuberculosis (TB), remains the second leading cause of mortality among infectious diseases worldwide. Mycobacterial biotin protein ligase (MtBPL) is an essential enzyme in Mtb and regulates lipid metabolism through the post-translational biotinylation of acyl coenzyme A carboxylases. We report the synthesis and evaluation of a systematic series of potent nucleoside-based inhibitors of MtBPL that contain modifications to the ribofuranosyl ring of the nucleoside. All compounds were characterized by isothermal titration calorimetry (ITC) and shown to bind potently with K(D)s ≤ 2 nM. Additionally, we obtained high-resolution cocrystal structures for a majority of the compounds. Despite fairly uniform biochemical potency, the whole-cell Mtb activity varied greatly with minimum inhibitory concentrations (MIC) ranging from 0.78 to >100 μM. Cellular accumulation studies showed a nearly 10-fold enhancement in accumulation of a C-2'-α analogue over the corresponding C-2'-β analogue, consistent with their differential whole-cell activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.