C. A. Fierke

Phage-Assisted, Active Site-Directed Ligand Evolution with a Genetically Encoded Nε-Butyryl-ʟ-Lysine to Identify a Cellularly Potent and Selective Inhibitor for the ENL YEATS Domain as an Anti-Leukemia Agent

This study develops a phage-assisted ligand evolution method to identify potent ENL inhibitors, finding a pentapeptide with sub-nanomolar affinity and anti-leukemia activity.

Mode of inhibition of RNase P by gambogic acid and juglone

This study identifies gambogic acid and juglone as inhibitors of PRORP1, with distinct mechanisms of action, and shows they also inhibit human mtRNase P.

Phage-Assisted, Active Site-Directed Ligand Evolution of a Potent and Selective Histone Deacetylase 8 Inhibitor

This paper develops PADLE, a phage-assisted method to evolve potent HDAC8 inhibitors, identifying two highly selective and potent inhibitors with sub-nanomolar Ki values.

Disease associated mutations in mitochondrial precursor tRNAs affect binding, m1R9 methylation and tRNA processing by mtRNase P

This study examines how disease-linked mutations in mitochondrial pre-tRNAs affect mtRNase P activity, revealing a link between tRNA processing defects and mitochondrial disease.

A Speedy Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

This study designs and synthesizes potent SARS-CoV-2 main protease inhibitors, with some showing IC50 values below 100 nM and high virus inhibition potency in cell assays.

Unexpected Specificity within Dynamic Transcriptional Protein-Protein Complexes

The paper investigates the molecular recognition of disordered activators by coactivators, revealing that specific contacts and coactivator plasticity drive specificity despite apparent nonspecific interactions.

Kinetic mechanism of human mitochondrial RNase P

This study investigates the kinetic mechanism of human mitochondrial RNase P, showing that MRPP1/2 enhances catalytic activity and substrate affinity, and facilitates MRPP3 recognition and cleavage efficiency.

Alzheimer’s Amyloid-Beta Intermediates Generated by Polymer-Nanodiscs

This study uses PMA-nanodiscs to study Aβ1-40 aggregation, showing they trap intermediates and reduce neurotoxicity of oligomers.

Cationic polymethacrylate-copolymer acts as an agonist for beta-amyloid and antagonist for amylin fibrillation

This study shows a cationic polymer promotes Aβ40 fibrillation and inhibits hIAPP aggregation through electrostatic interactions and structural restraint.