M. Bogyo

A broad cathepsin inhibitor blocks crystal-stimulated inflammasome-dependent and -independent inflammation, and gout arthritis

This study shows that broad-spectrum cathepsin inhibitors block crystal-induced inflammation and gout arthritis by inhibiting both inflammasome-dependent and -independent pathways that generate IL-1β.

Activity-Based Protein Profiling Identifies Klebsiella pneumoniae Serine Hydrolases with Potential Roles in Host-Pathogen Interactions

Polymer-tethered quenched fluorescent probes for enhanced imaging of tumor associated proteases

This paper develops polymer-tethered fluorescent probes for tumor-associated protease imaging, showing improved signal and tumor-to-background ratios compared to small molecule probes.

Mixed Alkyl/Aryl Phosphonates Identify Metabolic Serine Hydrolases as Antimalarial Targets

The paper identifies mixed alkyl/aryl phosphonates as anti-malarial compounds that inhibit serine hydrolases with low resistance potential.

Development of Oxadiazolone Activity-Based Probes Targeting FphE for Specific Detection of S. aureus Infections

The paper develops oxadiazolone-based probes targeting FphE to specifically detect S. aureus infections through covalent modification of the enzyme's active site.

Covalent macrocyclic proteasome inhibitors mitigate resistance in Plasmodium falciparum

This paper develops covalent macrocyclic proteasome inhibitors for Plasmodium falciparum that show reduced resistance compared to reversible inhibitors.

Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows

The paper describes a solid-phase synthesis method for creating macrocyclic peptides with fluorosulfate electrophiles, enabling chemoproteomic screening and target identification.

Chemoproteomic identification of a dipeptidyl peptidase 4 (DPP4) homolog in Bacteroides thetaiotaomicron important for envelope integrity and fitness

The paper identifies a DPP4 homolog in Bacteroides thetaiotaomicron important for envelope integrity and fitness, showing it is inhibited by diabetes drugs.

A screen of covalent inhibitors in Mycobacterium tuberculosis identifies serine hydrolases involved in lipid metabolism as potential therapeutic targets

Plasmodium berghei K13 Mutations Mediate In Vivo Artemisinin Resistance That is Reversed by Proteasome Inhibition

This study introduces K13 mutations into Plasmodium berghei to demonstrate their role in mediating artemisinin resistance in vivo, showing delayed parasite clearance and synergistic effects with proteasome inhibitors.

Toxoplasma gondii serine hydrolases regulate parasite lipid mobilization during growth and replication within the host

This study identifies serine hydrolases in Toxoplasma gondii that hydrolyze lipid esters, showing their role in lipid metabolism and potential as therapeutic targets.

Challenges for targeting SARS-CoV-2 proteases as a therapeutic strategy for COVID-19

This study evaluates compounds targeting SARS-CoV-2 proteases Mpro and PLpro, finding limited efficacy for Mpro due to off-target inhibition of host cathepsins and no viable hits for PLpro.

A chemiluminescent protease probe for rapid, sensitive, and inexpensive detection of live Mycobacterium tuberculosis

A chemiluminescent probe detects live Mycobacterium tuberculosis with high sensitivity and speed, enabling improved TB diagnostics and drug resistance monitoring.

Blocking palmitoylation of Toxoplasma gondii myosin light chain 1 disrupts glideosome composition but has little impact on parasite motility

This study shows that blocking palmitoylation of T. gondii TgMLC1 disrupts its association with TgGAP45 but does not significantly affect parasite motility.

Design of optical imaging probes by screening of diverse substrate libraries directly in disease tissue extracts

The paper develops fluorescent probes for cancer detection by screening peptide libraries in tissue extracts, identifying highly effective tumor-specific probes that outperform previous designs.

Multivariate 'AND-gate' substrate probes as enhanced contrast agents for fluorescence-guided surgery

This paper introduces multivariate AND-gate optical imaging probes that improve specificity and sensitivity for cancer margin detection during surgery by requiring sequential processing by multiple tumor-specific enzymes.

Structural basis for active-site probes targeting Staphylococcus aureus serine hydrolase virulence factors

The paper reports structures of Staphylococcus aureus serine hydrolases and their interactions with inhibitors, revealing functional insights and potential targets for therapeutic development.

The antimalarial natural product salinipostin A identifies essential α/β serine hydrolases involved in lipid metabolism in P. falciparum parasites

The study identifies essential α/β serine hydrolases in P. falciparum as targets of the antimalarial Salinipostin A, which disrupt lipid metabolism and inhibit parasite growth.

The clinical drug candidate ebselen attenuates inflammation and promotes microbiome recovery after antibiotic treatment for Clostridium difficile infection

This study shows ebselen reduces CDI recurrence and colitis in hamsters and promotes microbiome recovery without altering diversity in mice.

A phage display approach to identify highly selective covalent binders

The paper develops a phage display method to identify highly selective covalent binders, demonstrating its effectiveness with a cysteine protease inhibitor.

Leveraging peptide substrate libraries to design inhibitors of bacterial Lon protease

The paper uses peptide substrate libraries to determine the specificity of bacterial Lon protease and develops a potent inhibitor that affects Lon function in E. coli without toxicity to mammalian cells.

Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity reveals structural factors responsible for differences in amino acid preferences between peptide-based substrates and covalent inhibitors.

The paper characterizes P. falciparum DPAP3 specificity and identifies structural factors causing differences in amino acid preferences between peptide substrates and covalent inhibitors.