Advances in covalent kinase inhibitors

A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Gambogic acid as a candidate for cancer therapy: a review

Y Liu, Y Chen, L Lin, H Li - International Journal of Nanomedicine, 2020 - Taylor & Francis
Gambogic acid (GA), a kind of dry resin secreted by the Garcinia hanburyi tree, is a natural
active ingredient with various biological activities, such as anti-cancer, anti-inflammatory …

Molecular insight in the multifunctional activities of Withaferin A

WV Berghe, L Sabbe, M Kaileh, G Haegeman… - Biochemical …, 2012 - Elsevier
Herbal medicine which involves the use of plants for their medicinal value, dates as far back
as the origin of mankind and demonstrates an array of applications including cardiovascular …

Withaferin A inhibits NF-kappaB activation by targeting cysteine 179 in IKKβ

K Heyninck, M Lahtela-Kakkonen… - Biochemical …, 2014 - Elsevier
The transcription factor NF-κB is one of the main players involved in inflammatory responses
during which NF-κB becomes rapidly activated. However to maintain homeostasis, this NF …

Gambogic acid induces apoptosis in imatinib-resistant chronic myeloid leukemia cells via inducing proteasome inhibition and caspase-dependent Bcr-Abl …

X Shi, X Chen, X Li, X Lan, C Zhao, S Liu, H Huang… - Clinical Cancer …, 2014 - AACR
Purpose: Chronic myelogenous leukemia (CML) is characterized by the constitutive
activation of Bcr-Abl tyrosine kinase. Bcr-Abl-T315I is the predominant mutation that causes …

Chemistry and Biology of the Caged Garcinia Xanthones

O Chantarasriwong, A Batova… - … A European Journal, 2010 - Wiley Online Library
Natural products have been a great source of many small molecule drugs for various
diseases. In spite of recent advances in biochemical engineering and fermentation …

Role of pyroptosis in diabetic retinopathy and its therapeutic implications

A Al Mamun, AA Mimi, M Zaeem, Y Wu… - European journal of …, 2021 - Elsevier
Pyroptosis has recently been established as a term of programmed-inflammatory cell death.
Pyroptosis is mainly divided into two molecular signaling pathways, including caspase-1 …

A covalently bound inhibitor triggers EZH 2 degradation through CHIP‐mediated ubiquitination

X Wang, W Cao, J Zhang, M Yan, Q Xu, X Wu… - The EMBO …, 2017 - embopress.org
Enhancer of zeste homolog 2 (EZH 2) has been characterized as a critical oncogene and a
promising drug target in human malignant tumors. The current EZH 2 inhibitors strongly …

[HTML][HTML] Gambogic acid triggers vacuolization-associated cell death in cancer cells via disruption of thiol proteostasis

MJ Seo, DM Lee, IY Kim, D Lee, MK Choi, JY Lee… - Cell Death & …, 2019 - nature.com
Gambogic acid (GA), a xanthonoid extracted from the resin of the tree, Garcinia hanburyi,
was recently shown to exert anticancer activity in multiple studies, but the underlying action …

Gambogic acid is a novel anti-cancer agent that inhibits cell proliferation, angiogenesis and metastasis

X Wang, W Chen - Anti-Cancer Agents in Medicinal Chemistry …, 2012 - ingentaconnect.com
Gambogic acid (GA) is a caged xanthone that is derived from Garcinia hanburyi and
functions as a strong apoptotic inducer in many types of cancer cells. The distinct …