Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

Proximity-inducing modalities: the past, present, and future

S Singh, W Tian, ZC Severance… - Chemical Society …, 2023 - pubs.rsc.org
Living systems use proximity to regulate biochemical processes. Inspired by this
phenomenon, bifunctional modalities that induce proximity have been developed to redirect …

Benchmarking methods for PROTAC ternary complex structure prediction

E Rovers, M Schapira - Journal of Chemical Information and …, 2024 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are bifunctional compounds that recruit an E3
ligase to a target protein to induce ubiquitination and degradation of the target. Rational …

Proteome-scale discovery of protein degradation and stabilization effectors

J Poirson, H Cho, A Dhillon, S Haider, AZ Imrit… - Nature, 2024 - nature.com
Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …

Beyond proteolysis-targeting chimeric molecules: designing heterobifunctional molecules based on functional effectors

L Hua, Q Zhang, X Zhu, R Wang, Q You… - Journal of Medicinal …, 2022 - ACS Publications
In recent years, with the successful development of proteolysis-targeting chimeric molecules
(PROTACs), the potential of heterobifunctional molecules to contribute to reenvisioning drug …

Clinical translation of targeted protein degraders

NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …

Therapeutic potential of targeting the SUMO pathway in cancer

A Kukkula, VK Ojala, LM Mendez, L Sistonen… - Cancers, 2021 - mdpi.com
Simple Summary The small ubiquitin-like modifier (SUMO) pathway regulates the hallmark
properties of cancer cells. Moreover, alterations in activity and in levels of SUMO machinery …

Recent advances in induced proximity modalities

CSC Ng, SM Banik - Current Opinion in Chemical Biology, 2022 - Elsevier
Challenging disease targets necessitate new approaches for therapeutic intervention.
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …

Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Q Li, L Zhou, S Qin, Z Huang, B Li, R Liu… - European Journal of …, 2023 - Elsevier
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …

Inter-crosslinking peptide augments 4-1BB receptor clustering for cancer immunotherapy

GT Lv, QH Chen, MD Wang, XW Ye, YX Liu, S Liu… - Nano Today, 2023 - Elsevier
1BB as a co-stimulatory receptor represents a next-generation therapeutic target in immune-
oncology, which has been targeted by agonist antibodies or embedded in CAR-T cell …