Harnessing the anti-cancer natural product nimbolide for targeted protein degradation
Nimbolide, a terpenoid natural product derived from the Neem tree, impairs cancer
pathogenicity; however, the direct targets and mechanisms by which nimbolide exerts its …
pathogenicity; however, the direct targets and mechanisms by which nimbolide exerts its …
Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function
The translation of functionally active natural products into fully synthetic small-molecule
mimetics has remained an important process in medicinal chemistry. We recently discovered …
mimetics has remained an important process in medicinal chemistry. We recently discovered …
A nimbolide-based kinase degrader preferentially degrades oncogenic BCR-ABL
Targeted protein degradation (TPD) and proteolysis-targeting chimeras (PROTACs) have
arisen as powerful therapeutic modalities for degrading specific proteins in a proteasome …
arisen as powerful therapeutic modalities for degrading specific proteins in a proteasome …
Nimbolide, a neem limonoid, is a promising candidate for the anticancer drug arsenal
Nimbolide, a major limonoid constituent of Azadirachta indica, commonly known as neem,
has attracted increasing research attention owing to its wide spectrum of pharmacological …
has attracted increasing research attention owing to its wide spectrum of pharmacological …
Covalent ligand discovery against druggable hotspots targeted by anti-cancer natural products
Many natural products that show therapeutic activities are often difficult to synthesize or
isolate and have unknown targets, hindering their development as drugs. Identifying …
isolate and have unknown targets, hindering their development as drugs. Identifying …
Nimbolide, a neem limonoid abrogates canonical NF-κB and Wnt signaling to induce caspase-dependent apoptosis in human hepatocarcinoma (HepG2) cells
K Kavitha, RV Priyadarsini, P Anitha… - European journal of …, 2012 - Elsevier
Nuclear factor kappa B (NF-κB), an oncogenic signaling factor plays a critical role in the
development and progression of various cancers. The objective of this study was to …
development and progression of various cancers. The objective of this study was to …
[HTML][HTML] Chemical proteomics identifies druggable vulnerabilities in a genetically defined cancer
The transcription factor NRF2 is a master regulator of the cellular antioxidant response, and
it is often genetically activated in non-small-cell lung cancers (NSCLCs) by, for instance …
it is often genetically activated in non-small-cell lung cancers (NSCLCs) by, for instance …
Covalent ligand screening uncovers a RNF4 E3 ligase recruiter for targeted protein degradation applications
Targeted protein degradation has arisen as a powerful strategy for drug discovery allowing
the targeting of undruggable proteins for proteasomal degradation. This approach most …
the targeting of undruggable proteins for proteasomal degradation. This approach most …
Application of mass spectrometry profiling to establish brusatol as an inhibitor of global protein synthesis
S Vartanian, TP Ma, J Lee, PM Haverty… - Molecular & Cellular …, 2016 - ASBMB
The KEAP1/Nrf2 pathway senses and responds to changes in intracellular oxidative stress.
Mutations that result in constitutive activation of Nrf2 are present in several human tumors …
Mutations that result in constitutive activation of Nrf2 are present in several human tumors …
Harnessing the E3 ligase KEAP1 for targeted protein degradation
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …