Novel p21-activated kinase 4 (PAK4) allosteric modulators overcome drug resistance and stemness in pancreatic ductal adenocarcinoma

A Aboukameel, I Muqbil, W Senapedis, E Baloglu… - Molecular cancer …, 2017 - AACR
Abstract The p21-activated kinase 4 (PAK4) is a key downstream effector of the Rho family
GTPases and is found to be overexpressed in pancreatic ductal adenocarcinoma (PDAC) …

Reprogramming energy metabolism with synthesized PDK inhibitors based on dichloroacetate derivatives and targeted delivery systems for enhanced cancer therapy

W She, T Liu, H Li, Z Wang, Z Guo… - Journal of Medicinal …, 2023 - ACS Publications
In many types of cancers, pyruvate dehydrogenase kinase (PDK) is abnormally
overexpressed and has become a promising target for cancer therapy. However, few highly …

Identification of high-affinity inhibitors of pyruvate dehydrogenase kinase-3: towards therapeutic management of cancer

T Mohammad, K Arif, MF Alajmi, A Hussain… - Journal of …, 2021 - Taylor & Francis
Abstract Pyruvate dehydrogenase kinase 3 (PDK3) is a multifunctional enzyme that plays a
central role in the cancer metabolic switch by blocking pyruvate catabolism in the TCA cycle …

[HTML][HTML] New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells

M Tandon, J Johnson, Z Li, S Xu, P Wipf, QJ Wang - PloS one, 2013 - journals.plos.org
The emergence of protein kinase D (PKD) as a potential therapeutic target for several
diseases including cancer has triggered the search for potent, selective, and cell-permeable …

Urolithin A, a novel natural compound to target PI3K/AKT/mTOR pathway in pancreatic cancer

TM Totiger, S Srinivasan, VR Jala, P Lamichhane… - Molecular cancer …, 2019 - AACR
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive malignancy and is highly
resistant to standard treatment regimens. Targeted therapies against KRAS, a mutation …

Inhibition of pyruvate dehydrogenase kinase as a therapeutic strategy against cancer

S Sradhanjali, MM Reddy - Current topics in medicinal …, 2018 - ingentaconnect.com
Cancer cells alter their metabolism to support the uninterrupted supply of biosynthetic
molecules required for continuous proliferation. Glucose metabolism is frequently …

JX06 selectively inhibits pyruvate dehydrogenase kinase PDK1 by a covalent cysteine modification

W Sun, Z Xie, Y Liu, D Zhao, Z Wu, D Zhang, H Lv… - Cancer research, 2015 - AACR
Pyruvate dehydrogenase kinase PDK1 is a metabolic enzyme responsible for switching
glucose metabolism from mitochondrial oxidation to aerobic glycolysis in cancer cells, a …

Combined MEK and PI3K inhibition in a mouse model of pancreatic cancer

B Alagesan, G Contino, AR Guimaraes… - Clinical cancer …, 2015 - AACR
Purpose: Improved therapeutic approaches are needed for the treatment of pancreatic
ductal adenocarcinoma (PDAC). As dual MEK and PI3K inhibition is presently being used in …

[HTML][HTML] Inhibition of KRAS, MEK and PI3K demonstrate synergistic anti-tumor effects in pancreatic ductal adenocarcinoma cell lines

Y Ma, B Schulz, N Trakooljul, M Al Ammar, A Sekora… - Cancers, 2022 - mdpi.com
Simple Summary Small molecule inhibitors and targeted therapy are considered to have
significant potential for pancreatic ductal adenocarcinoma therapies. Preclinical studies of …

Role of protein kinase D signaling in pancreatic cancer

S Guha, S Tanasanvimon, J Sinnett-Smith… - Biochemical …, 2010 - Elsevier
Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal cancers with dismal
survival rates. Its intransigence to conventional therapy renders PDAC an aggressive …