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Showing results 1 to 6 of 6

Journal Article

Bifunctional small molecules that induce nuclear localization and targeted transcriptional regulation

Authors : Gibson, William J. (2023)

The aberrant localization of proteins in cells is a key factor in the development of various diseases, including cancer and neurodegenerative disease. To better understand and potentially manipulate protein localization for therapeutic purposes, we engineered bifunctional compounds that bind to proteins in separate cellular compartments. We show these compounds induce nuclear import of cytosolic cargoes, using nuclear-localized BRD4 as a “carrier” for co-...

Journal Article

Probing Bioactive Chemical Space to Discover RNA-Targeted Small Molecules

Authors : wicks, sarah L. (2023)

The use of small molecules to modulate RNA structure and function has become invaluable for studying the many roles of RNA in biological processes1 as well as discovering effective therapeutic treatments.2-5 Early on, the promise of RNA as a ‘druggable’ target was demonstrated by the identification of several RNA-targeting small molecule classes such as aminoglycosides.6, 7 These ligands bound highly abundant and structured ribosomal RNA (r...

Journal Article

Small Molecule Screen Identifies Non-Catalytic USP3 Chemical Handle

Authors : K. Mann, Mandeep (2023)

Zinc-finger ubiquitin binding domains (ZnF-UBDs) are non-catalytic domains mostly found in deubiquitylases (DUBs). They represent an underexplored opportunity for the development of deubiquitylase-targeting chimeras (DUBTACs) to pharmacologically induce the deubiquitination of target proteins. We have previously shown that ZnF-UBDs are ligandable domains. Here, a focused small molecule library screen against a panel of eleven ZnF-UBDs led to the identification of 5...

Journal article

Targeting Troponin C with Small Molecules Containing Diphenyl Moieties: Calcium Sensitivity Effects on Striated Muscle and Structure Activity Relationship

Authors : Hantz, Eric R. (2023)

Despite large investments from academia and industry, heart failure, which results from a disruption of the contractile apparatus, remains a leading cause of death. Cardiac muscle contraction is a calcium-dependent mechanism, which is regulated by the troponin protein complex (cTn) and specifically by the N-terminal domain of its calcium binding subunit (cNTnC). There is an increasing need for the development of small molecules that increase...

Journal Article

USING SMALL MOLECULES TO TURN AN RNA APTAMER INTO SENSORS FOR INORGANIC TARGETS WITHOUT IN VITRO SELECTION

Authors : aggarwal, Tushar (2023)

Aptamers are structured nucleic acid sequences that selectively bind a molecular target with high affinity. Aptamer sequences can be found in nature as gene regulation elements located in the untranslated regions of mRNAs,1 or discovered in the laboratory by in vitro selection (also known as SELEX: systematic evolution of ligands by exponential enrichment) from a random pool of nucleic acids.2,3 Some in vitroselected aptamers can bind ...

Journal article

VHL ligand binding increases intracellular level of VHL

Authors : Frost, Julianty (2021)

The von–Hippel Lindau (VHL) protein is a tumour suppressor protein frequently mutated in the VHL disease, which functions as substrate recognition subunit of a Cul2 E3 ubiquitin ligase (CRL2VHL). CRL2VHL plays an important role in oxygen sensing, by binding and targeting Hypoxia Inducible Factor-alpha subunits (HIF-alpha) for ubiquitination and degradation. VHL is also commonly hijacked by heterobifunctional degrader molecules known as...