Advancing targeted protein degradation for cancer therapy
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
Expanding chemical probe space: quality criteria for covalent and degrader probes
IV Hartung, J Rudolph, MM Mader… - Journal of Medicinal …, 2023 - ACS Publications
Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
VG Klein, AG Bond, C Craigon… - Journal of medicinal …, 2021 - ACS Publications
Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Förster resonance energy transfer (FRET) and applications thereof
FRET is a nonradiative process of energy transfer that is based on the dipole–dipole
interactions between molecules that are fluorescent. Transfer of energy takes place rapidly …
interactions between molecules that are fluorescent. Transfer of energy takes place rapidly …
Aptamer-based targeted protein degradation
The selective removal of misfolded, aggregated, or aberrantly overexpressed protein plays
an essential role in maintaining protein-dominated biological processes. In parallel, the …
an essential role in maintaining protein-dominated biological processes. In parallel, the …
PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery
N Guedeney, M Cornu, F Schwalen, C Kieffer… - Drug Discovery …, 2023 - Elsevier
Abstract Target Protein Degradation TPD is a new avenue and revolutionary for therapeutics
because redefining the principles of classical drug discovery and guided by event-based …
because redefining the principles of classical drug discovery and guided by event-based …
Delivering on the promise of protein degraders
MN O'Brien Laramy, S Luthra, MF Brown… - Nature Reviews Drug …, 2023 - nature.com
Over the past 3 years, the first bivalent protein degraders intentionally designed for targeted
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …
Targeted protein degradation: advances, challenges, and prospects for computational methods
The therapeutic approach of targeted protein degradation (TPD) is gaining momentum due
to its potentially superior effects compared with protein inhibition. Recent advancements in …
to its potentially superior effects compared with protein inhibition. Recent advancements in …
[HTML][HTML] Piperlongumine conjugates induce targeted protein degradation
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that degrade target
proteins through recruiting E3 ligases. However, their application is limited in part because …
proteins through recruiting E3 ligases. However, their application is limited in part because …
Identification and characterization of a novel indoleamine 2, 3-dioxygenase 1 protein degrader for glioblastoma
Indoleamine 2, 3-dioxygenase 1 (IDO1) is a potent immunosuppressive enzyme that inhibits
the antitumor immune response through both tryptophan metabolism and non-enzymatic …
the antitumor immune response through both tryptophan metabolism and non-enzymatic …