Volume 17 Issue 7, July 2021

YAP is a major downstream effector of the Hippo intracellular signaling pathway, with key roles in organ development, regeneration, and cancer biology. A small molecule that targets Annexin (ANX) acts through YAP to promote rapid epidermal tissue expansion.

Heme-containing proteins support a broad range of cellular functions. A new crystal structure explains how an integral-membrane heme lyase attaches the hydrophobic heme to soluble proteins.

Over the past two decades, inhibitors of the polycomb repressor complex (PRC) have been driven from bench to bedside. New chemical compounds targeting the RING1B in polycomb repressor complex 1 (PRC1) add important tools to regulate polycomb functions.

This Review summarizes the recent technical advances in probing RNA secondary structures and discusses their connection with RNA regulatory functions in various biological processes and future directions in RNA structure-probing methods.

Annexin A2 (ANXA2) is identified as the target of a pharmacological YAP activator and as a druggable component of the Hippo pathway.

A substrate-biased activity-based probe technology was developed to enable relatively facile identification of proteases responsible for specific proteolytic events in complex biological milieu, revealing that urokinase regulates CDCP1 proteolysis.

Fragment screening and medicinal chemistry optimization led to development of a small-molecule inhibitor of RING1B–BMI1 E3 ligase, blocking the H2A ubiquitination activity of the Polycomb repressive complex 1 and inducing differentiation in leukemia cells.

A genome-mining approach targeted to enzyme domains that co-occur in a single protein (CO-ED) facilitates the discovery and characterization of an oxazolone synthetase involved in the biosynthesis of a series of oxazolone-containing natural products.

The structure of the heme lyase CcmF, an integral membrane protein, reveals a cavity opening toward the extracellular side to receive heme groups from the chaperone CcmE and a surface groove for guiding the substrate protein during heme attachment.

Liquid glycan arrays (LiGAs), presented on M13 bacteriophage surface proteins through bioorthogonal chemistry, link surface glycans to genetic barcodes in phage DNA, enabling lectin–glycan interaction profiling by DNA sequencing.

Engineering of a blue light-inducible AraC dimerization system in E. coli permits light-dependent, rather than arabinose-based, regulation of gene expression from standard P_BAD promoters, enabling temporal and spatial control of bacterial systems.

Degradation-tuning RNAs (dtRNAs) have the capacity to increase and decrease RNA stability in vivo and in vitro. Appending these modules to transcripts allows fine tuning of circuit dynamics, CRISPR interference and paper-based viral diagnostics.