Katherine Deigan Warner

TL;DR: In this article, the authors discuss principles for discovering small-molecule drugs that target RNA and argue that the overarching challenge is to identify appropriate target structures - namely, in disease-causing RNAs that have high information content and, consequently, appropriate ligand-binding pockets.

TL;DR: The cocrystal structure of Spinach bound to its cognate exogenous chromophore is solved, showing that Spinach activates the small molecule by immobilizing it between a base triple, a G-quadruplex and an unpaired G.

TL;DR: The asymmetric dimer interface of Corn could form the basis for the development of mutants that only fluoresce as heterodimers, and may be useful in analyzing RNA co-expression or association, or in designing self-assembling RNA nanostructures.

TL;DR: Crystallographic studies show that, despite having micromolar Kds, four different fragments bind the TPP riboswitch site-specifically, occupying the pocket that recognizes the aminopyrimidine of TPP, suggesting that off-pathway conformations of RNAs can be targeted for drug development.

TL;DR: This chapter describes the methods for co-crystallization and structure determination of fragment-bound TPP riboswitch structures and focuses on considerations for screening crystallization conditions across multiple crystal forms and guidance for building the fragment into the refined crystallographic model.