[HTML][HTML] Cyclic peptides as therapeutic agents and biochemical tools

SH Joo - Biomolecules & therapeutics, 2012 - ncbi.nlm.nih.gov
There are many cyclic peptides with diverse biological activities, such as antibacterial
activity, immunosuppressive activity, and anti-tumor activity, and so on. Encouraged by …

β-Hairpin peptidomimetics: design, structures and biological activities

JA Robinson - Accounts of chemical research, 2008 - ACS Publications
The folded 3D structures of peptides and proteins provide excellent starting points for the
design of synthetic molecules that mimic key epitopes (or surface patches) involved in …

[HTML][HTML] HIV-1 integrase binds the viral RNA genome and is essential during virion morphogenesis

JJ Kessl, SB Kutluay, D Townsend, S Rebensburg… - Cell, 2016 - cell.com
While an essential role of HIV-1 integrase (IN) for integration of viral cDNA into human
chromosome is established, studies with IN mutants and allosteric IN inhibitors (ALLINIs) …

Simultaneous recognition of HIV-1 TAR RNA bulge and loop sequences by cyclic peptide mimics of Tat protein

A Davidson, TC Leeper… - Proceedings of the …, 2009 - National Acad Sciences
The interaction of the HIV-1 transactivator protein Tat with its transactivation response (TAR)
RNA is an essential step in viral replication and therefore an attractive target for developing …

Defining RNA–small molecule affinity landscapes enables design of a small molecule inhibitor of an oncogenic noncoding RNA

SP Velagapudi, Y Luo, T Tran, HS Haniff… - ACS Central …, 2017 - ACS Publications
RNA drug targets are pervasive in cells, but methods to design small molecules that target
them are sparse. Herein, we report a general approach to score the affinity and selectivity of …

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 …

The design, structures and therapeutic potential of protein epitope mimetics

JA Robinson, S DeMarco, F Gombert, K Moehle… - Drug discovery today, 2008 - Elsevier
Using a biologically relevant peptide or protein structure as a starting point for lead
identification represents one of the most powerful approaches in modern drug discovery …

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 …

Inhibition of both HIV-1 reverse transcription and gene expression by a cyclic peptide that binds the Tat-transactivating response element (TAR) RNA

MS Lalonde, MA Lobritz, A Ratcliff… - PLoS …, 2011 - journals.plos.org
The RNA response element TAR plays a critical role in HIV replication by providing a
binding site for the recruitment of the viral transactivator protein Tat. Using a structure-guided …

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 …