Arnab K. Chatterjee
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Design, Synthesis, and Biological Evaluation of Tetrazol-2-yl-acetamides as Novel Antitubercular Agents Open
A focused small-molecule library was screened against extracellular Mycobacterium tuberculosis (Mtb) across four distinct carbon sources that mimic different metabolic states of the pathogen. This screen identified a novel tetrazol-2-yl-ac…
View article: Covalent Probes Reveal Small-Molecule Binding Pockets in Structured RNA and Enable Bioactive Compound Design
Covalent Probes Reveal Small-Molecule Binding Pockets in Structured RNA and Enable Bioactive Compound Design Open
The SARS-CoV-2 frameshift stimulation element (FSE) is a critical RNA structure that is essential for viral replication and represents a promising target for antiviral intervention. Here, Chemical Cross-Linking and Isolation by Pull-down (…
View article: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites
A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
Improved Bicyclic Pyrrolidine Analogues Inhibit <i>Toxoplasma gondii</i> Growth In Vitro and Cure Infection In Vivo Open
Inhibition of phenylalanine tRNA synthetase (PheRS) by bicyclic pyrrolidines provides a potent and specific inhibition of parasite growth. Herein, we describe novel bicyclic pyrrolidines designed to explore structure-activity relationships…
Fubylation as a Druggable Ubiquitin-Like Conjugation System Controlling Hippo Pathway Activity Open
The functionally and evolutionarily conserved Hippo-YAP signaling pathway plays a critical role in regulating cellular proliferation, organ size control, and regeneration. Accordingly, activators of YAP-driven transcription hold therapeuti…
View article: Adapting a LAMP Plasmodium vivax Malaria Diagnostic for Use in Low Resource Settings
Adapting a LAMP Plasmodium vivax Malaria Diagnostic for Use in Low Resource Settings Open
Malaria caused by the P. vivax parasite can be difficult to diagnose due to dormant phases and genetic variants. Regions such as Sub-Saharan Africa, South America, and Southeast Asia experience diagnostic accessibility issues due to the ‘g…
View article: Bunyaviral Cap-Snatching Endonuclease Activity and Inhibition with Baloxavir-like Inhibitors in the Context of Full-Length L Proteins
Bunyaviral Cap-Snatching Endonuclease Activity and Inhibition with Baloxavir-like Inhibitors in the Context of Full-Length L Proteins Open
The Bunyavirales order includes a range of zoonotic viruses, which can cause severe disease in humans. The viral replication machinery is a logical target for the development of direct-acting antivirals. Inhibition of the cap-snatching end…
Advanced Characterization of Liposomal Vitamin C: TEM, Cryo-EM, and Caco-2 Bioavailability Studies Open
A vital nutrient, vitamin C (ascorbic acid) offers numerous physiological advantages, such as immune system support, collagen synthesis and antioxidant protection. However, its bioavailability is limited due to degradation in the gastroint…
High-Throughput Repurposing Screen Reveals Compounds with Activity against <i>Toxoplasma gondii</i> Bradyzoites Open
Toxoplasma gondii causes widespread chronic infections that are not cured by current treatments due to the inability to affect semidormant bradyzoite stages within tissue cysts. To identify compounds to eliminate chronic infection, we deve…
Novel isoxazole thiophene-containing compounds active against Mycobacterium tuberculosis Open
Screening of the ChemDiv molecular library in cholesterol media against Mycobacterium tuberculosis (Mtb) H37Rv strain identified a novel isoxazole thiophene hit as a putative Rv1625c/Cya activator with a promising in vitro activity and goo…
Cryo-EM reveals conformational variability in the SARS-CoV-2 spike protein RBD induced by two broadly neutralizing monoclonal antibodies Open
Antibody binding to the SARS-CoV-2 spike undergoes intermediate conformational states, revealing dynamic antibody binding mechanisms.
Synthesis and Structure-Activity Relationship of Covalent Inhibitors of SARS-CoV-2 Papain-Like Protease with Antiviral Potency Open
The papain-like protease (PLpro) is a highly conserved domain encoded by the coronavirus (CoV) genome and it plays an essential role in the replication and maturation of the virus in addition to weakening host immune response. Due to the v…
High Throughput Repurposing Screen Reveals Compounds with Activity Against Toxoplasma gondii Bradyzoites Open
Toxoplasma gondii causes widespread chronic infections that are not cured by current treatments due to inability to affect semi-dormant bradyzoite stages within tissue cysts. To identify compounds to eliminate chronic infection, we develop…
View article: Identification of mCMQ069, a novel antimalarial with potential for a single-dose cure and/or 28-day chemoprevention
Identification of mCMQ069, a novel antimalarial with potential for a single-dose cure and/or 28-day chemoprevention Open
In efforts towards eliminating malaria, a discovery program was initiated to identify a novel antimalarial using KAF156 as a starting point. Following the most recent TCP/TPP guidelines, we have identified mCMQ069 with a predicted single o…
View article: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites
A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites
A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: Pharmacological expansion of type 2 alveolar epithelial cells promotes regenerative lower airway repair
Pharmacological expansion of type 2 alveolar epithelial cells promotes regenerative lower airway repair Open
Type 2 alveolar epithelial cells (AEC2s) are stem cells in the adult lung that contribute to lower airway repair. Agents that promote the selective expansion of these cells might stimulate regeneration of the compromised alveolar epitheliu…
View article: Formulation and characterization of Liposomal glutathione as a key component in mitigation of Kwashiorkor disease in children with malnutrition
Formulation and characterization of Liposomal glutathione as a key component in mitigation of Kwashiorkor disease in children with malnutrition Open
Background. Kwashiorkor disease is due to deficiency of protein in malnutrition condition. Malnutrition is one of the major drawbacks among the Indian children. In India, the impact of undernutrition among impoverished children is dispropo…
Bicyclic pyrrolidine inhibitors of <i>Toxoplasma gondii</i> phenylalanine t-RNA synthetase with antiparasitic potency <i>in vitro</i> and brain exposure Open
Previous studies have shown that bicyclic azetidines are potent and selective inhibitors of apicomplexan phenylalanine tRNA synthetase (PheRS), leading to parasite growth inhibition in vitro and in vivo , including in models of Toxoplasma …
A small molecule MST1/2 inhibitor accelerates murine liver regeneration with improved survival in models of steatohepatitis Open
Dysfunctional liver regeneration following surgical resection remains a major cause of postoperative mortality and has no therapeutic options. Without targeted therapies, the current treatment paradigm relies on supportive therapy until ho…
A Prodrug Strategy to Reposition Atovaquone as a Long-Acting Injectable for Malaria Chemoprotection Open
Recent malaria drug discovery approaches have been extensively focused on the development of oral, smallmolecule inhibitors for disease treatment whereas parenteral routes of administration have been avoided due to limitations in deploying…
View article: Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead Open
There remains a need to develop novel SARS-CoV-2 therapeutic options that improve upon existing therapies by an increased robustness of response, fewer safety liabilities, and global-ready accessibility. Functionally critical viral main pr…