Critical assessment of LC3/GABARAP ligands used for degrader development and ligandability of LC3/GABARAP binding pockets
Recent successes in developing small molecule degraders that act through the ubiquitin
system have spurred efforts to extend this technology to other mechanisms, including the …
system have spurred efforts to extend this technology to other mechanisms, including the …
Development and Discovery of a Selective Degrader of Casein Kinases 1 δ/ε
A Haag, V Němec, P Janovská… - Journal of medicinal …, 2025 - ACS Publications
Members of the casein kinase 1 (CK1) family have emerged as key regulators of cellular
signaling and as potential drug targets. Functional annotation of the 7 human isoforms …
signaling and as potential drug targets. Functional annotation of the 7 human isoforms …
[HTML][HTML] Single-plate kinome screening in live-cells to enable highly cost-efficient kinase inhibitor profiling
MP Schwalm, S Knapp - SLAS Discovery, 2025 - Elsevier
Cancer research, cancer treatment, and the field of chemical biology are examples which
heavily rely on the discovery of selective kinase inhibitors. While determining on-target …
heavily rely on the discovery of selective kinase inhibitors. While determining on-target …
Functional characterization of pathway inhibitors for the ubiquitin-proteasome system (UPS) as tool compounds for CRBN and VHL-mediated targeted protein …
MP Schwalm, A Menge, L Elson, FA Greco… - ACS Chemical …, 2025 - ACS Publications
Small molecule degraders such as PROteolysis TArgeting Chimeras (PROTACs) and
molecular glues are new modalities for drug development and important tools for target …
molecular glues are new modalities for drug development and important tools for target …
Type-II kinase inhibitors that target Parkinson's Disease-associated LRRK2
ND Raig, KJ Surridge, M Sanz-Murillo, V Dederer… - bioRxiv, 2024 - biorxiv.org
Aberrant increases in kinase activity of leucine-rich repeat kinase 2 (LRRK2) are associated
with Parkinson's disease (PD). Numerous LRRK2-selective type-I kinase inhibitors have …
with Parkinson's disease (PD). Numerous LRRK2-selective type-I kinase inhibitors have …
[PDF][PDF] MASTER'S DISSERTATION TITLE
NA Ankamah - 2024 - libstore.ugent.be
The advent of TPD has advanced the field of drug discovery, making it possible to degrade
heretofore undruggable targets. PROTACs have extensively been applied to various targets …
heretofore undruggable targets. PROTACs have extensively been applied to various targets …