Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics

CS Swenson, G Mandava, DM Thomas… - Chemical …, 2024 - ACS Publications
The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …

Targeting intracellular protein–protein interactions with macrocyclic peptides

M Buyanova, D Pei - Trends in pharmacological sciences, 2022 - cell.com
Intracellular protein–protein interactions (PPIs) are challenging targets for traditional drug
modalities. Macrocyclic peptides (MPs) prove highly effective PPI inhibitors in vitro and can …

Membrane Permeability in a Large Macrocyclic Peptide Driven by a Saddle-Shaped Conformation

JH Faris, E Adaligil, N Popovych, S Ono… - Journal of the …, 2024 - ACS Publications
The effort to modulate challenging protein targets has stimulated interest in ligands that are
larger and more complex than typical small-molecule drugs. While combinatorial techniques …

Grb7, a critical mediator of EGFR/ErbB signaling, in cancer development and as a potential therapeutic target

PY Chu, YL Tai, TL Shen - Cells, 2019 - mdpi.com
The partner of activated epidermal growth factor receptor (EGFR), growth factor receptor
bound protein-7 (Grb7), a functionally multidomain adaptor protein, has been demonstrated …

Current development of bicyclic peptides

D Feng, L Liu, Y Shi, P Du, S Xu, Z Zhu, J Xu… - Chinese Chemical …, 2023 - Elsevier
Bicyclic peptides, a class of polypeptides with two loops within their structure, have emerged
as powerful tools in the development of new peptide drugs. They have the potential to bind …

Macrocycles and macrocyclization in anticancer drug discovery: Important pieces of the puzzle

C Zhang, F Liu, Y Zhang, C Song - European Journal of Medicinal …, 2024 - Elsevier
Increasing disease-related proteins have been identified as novel therapeutic targets.
Macrocycles are emerging as potential solutions, bridging the gap between conventional …

Miniproteins as a powerful modality in drug development

ZR Crook, NW Nairn, JM Olson - Trends in biochemical sciences, 2020 - cell.com
Miniproteins are a diverse group of protein scaffolds characterized by small (1–10 kDa) size,
stability, and versatility in drug-like roles. Coming largely from native sources, they have …

Peptide therapeutics in the management of metastatic cancers

D Bose, L Roy, S Chatterjee - RSC advances, 2022 - pubs.rsc.org
Cancer remains a leading health concern threatening lives of millions of patients worldwide.
Peptide-based drugs provide a valuable alternative to chemotherapeutics as they are highly …

Phosphotyrosine isosteres: past, present and future

RA Cerulli, JA Kritzer - Organic & biomolecular chemistry, 2020 - pubs.rsc.org
Tyrosine phosphorylation is a critical component of signal transduction for multicellular
organisms, particularly for pathways that regulate cell proliferation and differentiation. While …

Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors

RA Cerulli, L Shehaj, I Tosic, K Jiang, J Wang… - Bioorganic & medicinal …, 2020 - Elsevier
The signal transducer and activator of transcription 3 (STAT3) protein is constitutively
activated in several cancers. STAT3 activity can be blocked by inhibiting its Src Homology 2 …