[HTML][HTML] Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket
SC Tso, X Qi, WJ Gui, CY Wu, JL Chuang… - Journal of Biological …, 2014 - ASBMB
Pyruvate dehydrogenase kinase isoforms (PDKs 1–4) negatively regulate activity of the
mitochondrial pyruvate dehydrogenase complex by reversible phosphorylation. PDK …
mitochondrial pyruvate dehydrogenase complex by reversible phosphorylation. PDK …
Development of isatin-thiazolo [3, 2-a] benzimidazole hybrids as novel CDK2 inhibitors with potent in vitro apoptotic anti-proliferative activity: Synthesis, biological and …
In the current medical era, human health is experiencing numerous challenges, particularly
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …
[HTML][HTML] Differential inhibition of PDKs by phenylbutyrate and enhancement of pyruvate dehydrogenase complex activity by combination with dichloroacetate
R Ferriero, C Iannuzzi, G Manco… - Journal of inherited …, 2015 - Springer
Pyruvate dehydrogenase complex (PDHC) is a key enzyme in metabolism linking glycolysis
to tricarboxylic acid cycle and its activity is tightly regulated by phosphorylation catalyzed by …
to tricarboxylic acid cycle and its activity is tightly regulated by phosphorylation catalyzed by …
Design, synthesis, and biological evaluation of 4-methyl quinazoline derivatives as anticancer agents simultaneously targeting phosphoinositide 3-kinases and …
K Zhang, F Lai, S Lin, M Ji, J Zhang… - Journal of Medicinal …, 2019 - ACS Publications
Polypharmacology is a promising paradigm in modern drug discovery. Herein, we have
discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid …
discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid …
Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase
X Ning, H Qi, R Li, Y Li, Y Jin, MA McNutt, J Liu… - European journal of …, 2017 - Elsevier
Abstract Pyruvate kinase M2 (PKM2) is a rate-limiting enzyme of the glycolytic pathway
which is highly expressed in cancer cells. Cancer cells rely heavily on PKM2 for anabolic …
which is highly expressed in cancer cells. Cancer cells rely heavily on PKM2 for anabolic …
Therapeutic targeting of the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis in cancer
PW Stacpoole - JNCI: Journal of the National Cancer Institute, 2017 - academic.oup.com
The mitochondrial pyruvate dehydrogenase complex (PDC) irreversibly decarboxylates
pyruvate to acetyl coenzyme A, thereby linking glycolysis to the tricarboxylic acid cycle and …
pyruvate to acetyl coenzyme A, thereby linking glycolysis to the tricarboxylic acid cycle and …
Identification of novel PI3Kδ inhibitors by docking, ADMET prediction and molecular dynamics simulations
YY Liu, XY Feng, WQ Jia, Z Jing, WR Xu… - … biology and chemistry, 2019 - Elsevier
Abstract Background Phosphoinositide-3-kinase Delta (PI3Kδ) plays a key role in B-cell
signal transduction and inhibition of PI3Kδ is confirmed to have clinical benefit in certain …
signal transduction and inhibition of PI3Kδ is confirmed to have clinical benefit in certain …
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review
Y Wang, M Tortorella - European Journal of Medicinal Chemistry, 2022 - Elsevier
Aberrant activation of the phosphoinositide 3-kinase (PI3K) signaling network is a key event
in many human cancers and therefore enormous efforts have been made in the …
in many human cancers and therefore enormous efforts have been made in the …
[HTML][HTML] In Silico Identification and In Vitro and In Vivo Validation of Anti-Psychotic Drug Fluspirilene as a Potential CDK2 Inhibitor and a Candidate Anti-Cancer …
Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related deaths
worldwide. Surgical resection and conventional chemotherapy and radiotherapy ultimately …
worldwide. Surgical resection and conventional chemotherapy and radiotherapy ultimately …
Molecular overlay-guided design of new CDK2 inhibitor thiazepinopurines: Synthesis, anticancer, and mechanistic investigations
Adopting the molecular overlay approach, three novel sets of thiazepinopurines with
expected cytotoxicity and CDK2 inhibition potential were designed and synthesized. This …
expected cytotoxicity and CDK2 inhibition potential were designed and synthesized. This …