ArticleCell chemical biology2020
A Preclinical Candidate Targeting Mycobacterium tuberculosis KasA.
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Article in Cell chemical biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed.
- Identification of chemical features for improved outer membrane permeation in mycobacteria using machine learning.Nature microbiology · 2026Article
- Targeting KasA: isosakuranetin derivatives as promising scaffolds for novel anti-tuberculosis agents against drug-resistantFrontiers in bioinformatics · 2026Article
- The Biosynthetic Pathway of Mycolic Acids: Dual-Function Targets for Tuberculosis Therapeutics and Green Steroid Drugs Biomanufacturing.Pharmaceutics · 2025Review
- Human pluripotent stem cell-derived skin organoids enabled pathophysiological model of Mycobacterium tuberculosis infection.Nature communications · 2025Article
- Targeting Mycolic Acid Biosynthesis with Cyclic Sulfamates: A New Strategy againstACS infectious diseases · 2025Article
- Mycobacterium tuberculosis FAS-II pathway targeted integrative deep learning based identification of potential anti-tubercular agents.Journal of computer-aided molecular design · 2025Article
- A computational approach to mycolic acid biosynthesis disruption in mycobacterium tuberculosis via molluscan metabolites as KasA inhibitors.Scientific reports · 2025Article
- The KasA inhibitor JSF-3285 improves the sterilizing activity of bedaquiline-pretomanid-containing regimens in a mouse model of tuberculosis.Antimicrobial agents and chemotherapy · 2025Article
- Evolution of Small Molecule Inhibitors ofJournal of medicinal chemistry · 2025Article
- Identification of chemical features that influence mycomembrane permeation and antitubercular activity.bioRxiv : the preprint server for biology · 2025Article
- Progress of anti-tuberculosis drug targets and novel therapeutic strategies.Frontiers in microbiology · 2025Review
- Synthesis, Molecular Docking, Molecular Dynamic Simulation Studies, and Antitubercular Activity Evaluation of Substituted Benzimidazole Derivatives.Advances in pharmacological and pharmaceutical sciences · 2024Article
- Review
- Target Identification in Anti-Tuberculosis Drug Discovery.International journal of molecular sciences · 2023Review
- Article
- Indole: A promising scaffold for the discovery and development of potential anti-tubercular agents.Current research in pharmacology and drug discovery · 2022Review
- Anti-tuberculosis drug developmentFrontiers in microbiology · 2022Review
- Review
- An Outline of the Latest Crystallographic Studies on Inhibitor-Enzyme Complexes for the Design and Development of New Therapeutics against Tuberculosis.Molecules (Basel, Switzerland) · 2021Review
- Targeting Mycobacterium tuberculosis response to environmental cues for the development of effective antitubercular drugs.PLoS biology · 2021Article
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Authors and funding
25 authors.
Daigo InoyamaDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Divya AwasthiDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Glenn C CapodagliDepartment of Microbiology, Biochemistry and Molecular Genetics, New Jersey Medical School, Rutgers, The State University of New Jersey, Newark, USA.
Kholiswa TsotetsiDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Paridhi SukhejaDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Matthew ZimmermanPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Shao-Gang LiDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Ravindra JadhavDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Riccardo RussoDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Xin WangDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Courtney GradyDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Todd RichmannDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Riju ShresthaDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Liping LiDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Yong-Mo AhnDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Hsin Pin Ho LiangPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Marizel MinaPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Steven ParkPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
David S PerlinPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Nancy ConnellDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
Véronique DartoisPublic Health Research Institute, Rutgers University - New Jersey Medical School, Newark, NJ, USA.
David AllandDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA. Electronic address: allandda@njms.rutgers.edu.
Matthew B NeiditchDepartment of Microbiology, Biochemistry and Molecular Genetics, New Jersey Medical School, Rutgers, The State University of New Jersey, Newark, USA. Electronic address: neiditmb@njms.rutgers.edu.
Pradeep KumarDivision of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA. Electronic address: kumarp3@njms.rutgers.edu.
Joel S FreundlichDepartment of Pharmacology, Physiology, and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ, USA; Division of Infectious Disease, Department of Medicine and the Ruy V. Lourenco Center for the Study of Emerging and Re-emerging Pathogens, Rutgers University - New Jersey Medical School, Newark, NJ, USA. Electronic address: freundjs@rutgers.edu.
Funding
Therapeutics for drug-resistant bacteria: aryl myxopyronins and arylalkylcarboxamido phloroglucinolsU19AI142731 · NIAID · HACKENSACK UNIVERSITY MEDICAL CENTER · PI ALLAND, DAVID · 2019 to 2023
$33.9MTherapeutics for drug resistant-bacteria: Arylpropionyl-phloroglucinolsU19AI109713 · NIAID · RBHS-NEW JERSEY MEDICAL SCHOOL · PI FREUNDLICH, JOEL STEPHEN · 2014 to 2018
$26.9MDiscovery and Validation of Drug Targets in Vulnerable PopulationsR33AI111647 · NIAID · RBHS-NEW JERSEY MEDICAL SCHOOL · PI ALLAND, DAVID · 2016 to 2018
$1.5MA QTRAP 6500 LC-MS/MS System from SCIEX for high accuracy drug content analysisS10OD023524 · OD · RBHS-NEW JERSEY MEDICAL SCHOOL · PI DARTOIS, VERONIQUE · 2017 to 2017
$526kDiscovery and validation of drug targets in vulnerable pathways of MtbR21AI111647 · NIAID · RBHS-NEW JERSEY MEDICAL SCHOOL · PI ALLAND, DAVID · 2014 to 2015
$437kNIAID NIH HHS R21 AI111647NIAID NIH HHS R33 AI111647NIAID NIH HHS U19 AI109713NIAID NIH HHS U19 AI142731NIH HHS S10 OD023524
Abstract
Published Mycobacterium tuberculosis β-ketoacyl-ACP synthase KasA inhibitors lack sufficient potency and/or pharmacokinetic properties. A structure-based approach was used to optimize existing KasA inhibitor DG167. This afforded indazole JSF-3285 with a 30-fold increase in mouse plasma exposure. Biochemical, genetic, and X-ray studies confirmed JSF-3285 targets KasA. JSF-3285 offers substantial activity in an acute mouse model of infection and in the corresponding chronic infection model, with efficacious reductions in colony-forming units at doses as low as 5 mg/kg once daily orally and improvement of the efficacy of front-line drugs isoniazid or rifampicin. JSF-3285 is a promising preclinical candidate for tuberculosis.
Indexed as
3-Oxoacyl-(Acyl-Carrier-Protein) SynthaseAnimalsAntitubercular AgentsBacterial ProteinsDrug DiscoveryEnzyme InhibitorsFemaleHumansMiceModels, MolecularMycobacterium tuberculosisTuberculosis3-Oxoacyl-(Acyl-Carrier-Protein) SynthaseAntitubercular AgentsBacterial ProteinsEnzyme InhibitorsantitubercularJSF-3285KasAMycobacterium tuberculosispharmacokineticsstructure-based design
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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.