S. Ackloo

CACHE Challenge #1: targeting the WDR domain of LRRK2, a Parkinson's Disease associated protein.

The paper evaluates computational hit-finding methods for targeting the WDR domain of LRRK2, a Parkinson's disease protein, finding that diverse strategies yielded weakly potent compounds.

A resource to enable chemical biology and drug discovery of WDR Proteins

The paper develops a resource for discovering ligands for WDR proteins using experimental and computational methods, leading to the identification of drug-like ligands for 9 out of 20 targets.

Discovery and characterization of a chemical probe targeting the zinc-finger ubiquitin-binding domain of HDAC6

The paper identifies and characterizes a chemical probe, SGC-UBD253, that targets the HDAC6 UBD with selectivity, and a less active derivative as a negative control.

A host defense peptide mimetic, brilacidin, potentiates caspofungin antifungal activity against human pathogenic fungi

This study identifies brilacidin as a compound that enhances the antifungal activity of caspofungin against multiple human pathogenic fungi, including overcoming resistance mechanisms.

Pharmacological targeting of a PWWP domain demonstrates cooperative control of NSD2 localization

The paper develops a chemical probe, UNC6934, that targets the PWWP1 domain of NSD2, revealing cooperative control of NSD2 localization through chromatin reader domains.

Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

This study identifies a PRMT7 inhibitor and shows its effect on arginine methylation of stress proteins, linking PRMT7 to cellular stress response.

Design and characterisation of mutant and wild-type huntingtin proteins produced from a toolkit of scalable eukaryotic expression systems

This paper develops a toolkit for producing mutant and wild-type huntingtin proteins in eukaryotic systems to enable biochemical and structural studies of HD-related mutations.

A Chemical Toolbox for the Study of Bromodomains and Epigenetic Signaling

The paper presents a set of 25 chemical probes targeting human bromodomains and demonstrates their utility in studying muscle cell differentiation and triple negative breast cancer.