Constraining cyclic peptides to mimic protein structure motifs

TA Hill, NE Shepherd, F Diness… - Angewandte Chemie …, 2014 - Wiley Online Library
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

Recent advances in developing small molecules targeting RNA

L Guan, MD Disney - ACS chemical biology, 2012 - ACS Publications
RNAs are underexploited targets for small molecule drugs or chemical probes of function.
This may be due, in part, to a fundamental lack of understanding of the types of small …

Discovery of selective bioactive small molecules by targeting an RNA dynamic ensemble

AC Stelzer, AT Frank, JD Kratz, MD Swanson… - Nature chemical …, 2011 - nature.com
Current approaches used to identify protein-binding small molecules are not suited for
identifying small molecules that can bind emerging RNA drug targets. By docking small …

Structural mechanism for HIV-1 TAR loop recognition by Tat and the super elongation complex

U Schulze-Gahmen, JH Hurley - Proceedings of the …, 2018 - National Acad Sciences
Promoter-proximal pausing by RNA polymerase II (Pol II) is a key regulatory step in human
immunodeficiency virus-1 (HIV-1) transcription and thus in the reversal of HIV latency. By …

Using genome sequence to enable the design of medicines and chemical probes

AJ Angelbello, JL Chen, JL Childs-Disney… - Chemical …, 2018 - ACS Publications
Rapid progress in genome sequencing technology has put us firmly into a postgenomic era.
A key challenge in biomedical research is harnessing genome sequence to fulfill the …

Deep structural insights into RNA‐binding disordered protein regions

A Zeke, E Schad, T Horvath… - Wiley …, 2022 - Wiley Online Library
Recent efforts to identify RNA binding proteins in various organisms and cellular contexts
have yielded a large collection of proteins that are capable of RNA binding in the absence of …

A macrocyclic peptide ligand binds the oncogenic MicroRNA-21 precursor and suppresses dicer processing

MD Shortridge, MJ Walker, T Pavelitz… - ACS chemical …, 2017 - ACS Publications
MicroRNAs (miRNAs) help orchestrate cellular growth and survival through post-
transcriptional mechanisms. The dysregulation of miRNA biogenesis can lead to cellular …

An ultra-high affinity ligand of HIV-1 TAR reveals the RNA structure recognized by P-TEFb

MD Shortridge, PT Wille, AN Jones… - Nucleic acids …, 2019 - academic.oup.com
The HIV-1 trans-activator protein Tat binds the trans-activation response element (TAR) to
facilitate recruitment of the super elongation complex (SEC) to enhance transcription of the …

Methods to enable the design of bioactive small molecules targeting RNA

MD Disney, I Yildirim, JL Childs-Disney - Organic & biomolecular …, 2014 - pubs.rsc.org
RNA is an immensely important target for small molecule therapeutics or chemical probes of
function. However, methods that identify, annotate, and optimize RNA-small molecule …

[HTML][HTML] Insights into HIV-1 proviral transcription from integrative structure and dynamics of the Tat: AFF4: P-TEFb: TAR complex

U Schulze-Gahmen, I Echeverria, G Stjepanovic, Y Bai… - Elife, 2016 - elifesciences.org
HIV-1 Tat hijacks the human superelongation complex (SEC) to promote proviral
transcription. Here we report the 5.9 Å structure of HIV-1 TAR in complex with HIV-1 Tat and …