[HTML][HTML] PDK1 inhibitor BX795 improves cisplatin and radio-efficacy in oral squamous cell carcinoma by downregulating the PDK1/CD47/Akt-mediated glycolysis …

S Pai, VK Yadav, KT Kuo, NW Pikatan, CS Lin… - International journal of …, 2021 - mdpi.com
Background: Oral squamous cell carcinoma (OSCC) has a high prevalence and predicted
global mortality rate of 67.1%, necessitating better therapeutic strategies. Moreover, the …

[HTML][HTML] Targeting PDK1 with dichloroacetophenone to inhibit acute myeloid leukemia (AML) cell growth

L Qin, Y Tian, Z Yu, D Shi, J Wang, C Zhang, R Peng… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Abstract Pyruvate dehydrogenase kinase-1 (PDK1), a key metabolic enzyme involved in
aerobic glycolysis, is highly expressed in many solid tumors. Small molecule compound …

Dkk1 involvement and its potential as a biomarker in pancreatic ductal adenocarcinoma

E Igbinigie, F Guo, SW Jiang, C Kelley, J Li - Clinica chimica acta, 2019 - Elsevier
Abstract Dickkopf-1 (Dkk1)'s dysregulation has been implicated in the pathogenesis of a
variety of cancers. It is part of the Dkk family of proteins that includes Dkk2, Dkk3 and Dkk4 …

Investigation of inhibitory potential of quercetin to the pyruvate dehydrogenase kinase 3: Towards implications in anticancer therapy

R Dahiya, T Mohammad, S Roy, S Anwar… - International journal of …, 2019 - Elsevier
Abstract Pyruvate dehydrogenase kinase 3 (PDK3) is a mitochondrial protein, has recently
been considered as a potential pharmacological target for varying types of cancer. Here, we …

Design, synthesis, and pharmacological evaluation of isoindoline analogues as new HPK1 inhibitors

C Xie, B Liu, Z Song, Y Yang, M Dai… - Journal of Medicinal …, 2023 - ACS Publications
Hematopoietic progenitor kinase 1 (HPK1) is an important negative regulator in T-cell
receptor signaling and as a promising key target for immunotherapy. Herein, based on the …

2-Anilino-4-(1-methyl-1H-pyrazol-4-yl) pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation

BS Fanta, L Mekonnen, SKC Basnet, T Teo… - Bioorganic & Medicinal …, 2023 - Elsevier
Deregulation of cyclin-dependent kinase 2 (CDK2) and its activating partners, cyclins A and
E, is associated with the pathogenesis of a myriad of human cancers and with resistance to …

PDK1 promotes tumor growth and metastasis in a spontaneous breast cancer model

J Du, M Yang, S Chen, D Li, Z Chang, Z Dong - Oncogene, 2016 - nature.com
Because malignant cells have altered, usually accelerated, energy consumption, targeting
metabolic signaling represents a prevailing strategy for tumor therapy. Phosphoinositide …

Discovery of novel KRAS-PDEδ inhibitors by fragment-based drug design

L Chen, C Zhuang, J Lu, Y Jiang… - Journal of Medicinal …, 2018 - ACS Publications
Targeting KRAS-PDEδ protein–protein interactions with small molecules represents a
promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ …

Tailored first-line and second-line CDK4-targeting treatment combinations in mouse models of pancreatic cancer

A Chou, D Froio, AM Nagrial, A Parkin, KJ Murphy… - Gut, 2018 - gut.bmj.com
Objective Extensive molecular heterogeneity of pancreatic ductal adenocarcinoma (PDA),
few effective therapies and high mortality make this disease a prime model for advancing …

PDK1 and PKB/Akt: ideal targets for development of new strategies to structure‐based drug design

T Harris - IUBMB life, 2003 - Wiley Online Library
Growth factor binding events to receptor tyrosine kinases result in activation of
phosphatidylinositol 3‐kinase (PI3K), and activated PI3K generates the membrane‐bound …