Inhibitors of protein–protein interactions (PPIs): an analysis of scaffold choices and buried surface area

X Ran, JE Gestwicki - Current opinion in chemical biology, 2018 - Elsevier
Protein–protein interactions (PPI) were once considered 'undruggable', but clinical
successes, driven by advanced methods in drug discovery, have challenged that notion …

Rational design of peptide-based inhibitors disrupting protein-protein interactions

X Wang, D Ni, Y Liu, S Lu - Frontiers in chemistry, 2021 - frontiersin.org
Protein-protein interactions (PPIs) are well-established as a class of promising drug targets
for their implications in a wide range of biological processes. However, drug development …

Identification of a cellularly active SIRT6 allosteric activator

Z Huang, J Zhao, W Deng, Y Chen, J Shang… - Nature chemical …, 2018 - nature.com
SIRT6, a member of the SIRT deacetylase family, is responsible for deacetylation of histone
H3 N ε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac). As a tumor suppressor, SIRT6 has …

APC-activated long noncoding RNA inhibits colorectal carcinoma pathogenesis through reduction of exosome production

FW Wang, CH Cao, K Han, YX Zhao… - The Journal of …, 2019 - Am Soc Clin Investig
The adenomatous polyposis coli (APC) gene plays a pivotal role in the pathogenesis of
colorectal carcinoma (CRC) but remains a challenge for drug development. Long noncoding …

A duplex CRISPR-Cas9 ribonucleoprotein nanomedicine for colorectal cancer gene therapy

T Wan, Q Pan, C Liu, J Guo, B Li, X Yan, Y Cheng… - Nano Letters, 2021 - ACS Publications
Based on the high frequency of concurrent adenomatous polyposis coli (APC) and KRAS
mutations and their strong cooperative interaction in human colorectal cancer (CRC) …

Design of tracers in fluorescence polarization assay for extensive application in small molecule drug discovery

L Hua, D Wang, K Wang, Y Wang, J Gu… - Journal of Medicinal …, 2023 - ACS Publications
Development of fluorescence polarization (FP) assays, especially in a competitive manner,
is a potent and mature tool for measuring the binding affinities of small molecules. This …

[HTML][HTML] Peptide based therapeutics and their use for the treatment of neurodegenerative and other diseases

MH Baig, K Ahmad, M Saeed, AM Alharbi… - Biomedicine & …, 2018 - Elsevier
Bioactive peptides are actively involved in different biological functions and importantly
contribute to human health, and the use of peptides as therapeutics has a long successful …

Designing drugs and chemical probes with the dualsteric approach

J Zha, J He, C Wu, M Zhang, X Liu… - Chemical Society Reviews, 2023 - pubs.rsc.org
Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

Emerging roles of allosteric modulators in the regulation of protein‐protein interactions (PPIs): A new paradigm for PPI drug discovery

D Ni, S Lu, J Zhang - Medicinal research reviews, 2019 - Wiley Online Library
Protein‐protein interactions (PPIs) are closely implicated in various types of cellular activities
and are thus pivotal to health and disease states. Given their fundamental roles in a wide …

Discovery of hidden allosteric sites as novel targets for allosteric drug design

S Lu, M Ji, D Ni, J Zhang - Drug discovery today, 2018 - Elsevier
Highlights•Hidden allosteric sites provide valuable avenues for allosteric drug
discovery.•Hidden allosteric sites are invisible in the ligand-unbound crystal structures.• …