Small‐molecule inhibitors of PDK1

C Peifer, DR Alessi - ChemMedChem: Chemistry Enabling …, 2008 - Wiley Online Library
Signal transduction of many growth factors and oncogenes is mediated by 3‐
phosphoinositide‐dependent protein kinase‐1 (PDK1), a master regulator of a number of …

Molecular interaction studies on ellagic acid for its anticancer potential targeting pyruvate dehydrogenase kinase 3

R Dahiya, T Mohammad, P Gupta, A Haque… - RSC …, 2019 - pubs.rsc.org
Pyruvate dehydrogenase kinase 3 (PDK3) plays a central role in the cancer metabolic
switch through the reversible phosphorylation of pyruvate dehydrogenase complex thereby …

Computational study on new natural compound inhibitors of pyruvate dehydrogenase kinases

X Zhou, S Yu, J Su, L Sun - International Journal of Molecular Sciences, 2016 - mdpi.com
Pyruvate dehydrogenase kinases (PDKs) are key enzymes in glucose metabolism,
negatively regulating pyruvate dehyrogenase complex (PDC) activity through …

Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1)

ST Murphy, G Alton, S Bailey, SM Baxi… - Journal of medicinal …, 2011 - ACS Publications
Analogues substituted with various amines at the 6-position of the pyrazine ring on (4-amino-
7-isopropyl-7H-pyrrolo [2, 3-d] pyrimidin-5-yl) pyrazin-2-ylmethanone were discovered as …

Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening

EV Bobkova, MJ Weber, Z Xu, YL Zhang, J Jung… - Journal of Biological …, 2010 - ASBMB
The phosphoinositide 3-kinase/AKT signaling pathway plays a key role in cancer cell
growth, survival, and angiogenesis. Phosphoinositide-dependent protein kinase-1 (PDK1) …

Reprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2, 5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds

AK Farag, AHE Hassan, BS Ahn, KD Park… - Journal of enzyme …, 2020 - Taylor & Francis
Hybridization of reported weakly active antiproliferative hit 5-amino-4-pyrimidinol derivative
with 2-anilino-4-phenoxypyrimidines suggests a series of 2, 5-diamino-4-pyrimidinol …

[HTML][HTML] VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent …

JD Moore, A Staniszewska, T Shaw, J D'Alessandro… - Oncotarget, 2014 - ncbi.nlm.nih.gov
VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase
kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells …

CDKN2A-inactivated pancreatic ductal adenocarcinoma exhibits therapeutic sensitivity to paclitaxel: a bioinformatics study

JC Lin, TP Liu, PM Yang - Journal of Clinical Medicine, 2020 - mdpi.com
The mutation of cyclin dependent kinase inhibitor 2A (CDKN2A) is frequently found in
pancreatic ductal adenocarcinoma (PDAC). However, its prognostic and therapeutic roles in …

The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6‐Indolylpyridone‐3‐Carbonitrile derivatives

MM Saleh, T El-Moselhy, E El-Bastawissy… - European Journal of …, 2023 - Elsevier
MAPK pathway sparkles with RTK activation, passes through subsequent downstream RAS-
RAF-MEK-ERK signaling cascades, with consequent direct and indirect CDK4/6 signaling …

Is there a CDKN2A-centric network in pancreatic ductal adenocarcinoma?

C Wu, P Yang, B Liu, Y Tang - OncoTargets and therapy, 2020 - Taylor & Francis
Pancreatic cancer has a high mortality rate and its incidence has risen rapidly in recent
years. Meanwhile, the diagnosis and treatment of this cancer remain challenging. Pancreatic …