[HTML][HTML] Discovery of the 3-amino-1, 2, 4-triazine-based library as selective PDK1 inhibitors with therapeutic potential in highly aggressive pancreatic ductal …
D Carbone, M De Franco, C Pecoraro… - International Journal of …, 2023 - mdpi.com
Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly
involved in altered cancer cell metabolism, resulting in cancer aggressiveness and …
involved in altered cancer cell metabolism, resulting in cancer aggressiveness and …
1, 2, 4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation
C Pecoraro, M De Franco, D Carbone… - European Journal of …, 2023 - Elsevier
Among the different hallmarks of cancer, deregulation of cellular metabolism turned out to be
an essential mechanism in promoting cancer resistance and progression. The pyruvate …
an essential mechanism in promoting cancer resistance and progression. The pyruvate …
Identification of novel pyruvate dehydrogenase kinase 1 (PDK1) inhibitors by kinase activity-based high-throughput screening for anticancer therapeutics
W Zhang, X Hu, H Chakravarty, Z Yang… - ACS combinatorial …, 2018 - ACS Publications
Warburg effect, a preference of aerobic glycolysis for energy production even in the
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …
[HTML][HTML] Structural manipulations of marine natural products inspire a new library of 3-amino-1, 2, 4-triazine PDK inhibitors endowed with antitumor activity in …
D Carbone, M De Franco, C Pecoraro, D Bassani… - Marine Drugs, 2023 - mdpi.com
Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types of cancer,
characterized by late prognosis and drug resistance. Among the main factors sustaining …
characterized by late prognosis and drug resistance. Among the main factors sustaining …
Unexpected discovery of dichloroacetate derived adenosine triphosphate competitors targeting pyruvate dehydrogenase kinase to inhibit cancer proliferation
Pyruvate dehydrogenase kinases (PDKs) have recently emerged as an attractive target for
cancer therapy. Herein, we prepared a series of compounds derived from dichloroacetate …
cancer therapy. Herein, we prepared a series of compounds derived from dichloroacetate …
Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer
Pharmacologic inhibition of the oncogenic protein kinases using small molecules is a
promising strategy to combat several human malignancies. CDK1 is an example of such a …
promising strategy to combat several human malignancies. CDK1 is an example of such a …
Development of the first generation of disulfide-based subtype-selective and potent covalent pyruvate dehydrogenase kinase 1 (PDK1) inhibitors
Y Liu, Z Xie, D Zhao, J Zhu, F Mao, S Tang… - Journal of medicinal …, 2017 - ACS Publications
Pyruvate dehydrogenase kinases (PDKs) are overexpressed in most cancer cells and are
responsible for aberrant glucose metabolism. We previously described bis (4-morpholinyl …
responsible for aberrant glucose metabolism. We previously described bis (4-morpholinyl …
Rational design of mitochondria-targeted pyruvate dehydrogenase kinase 1 inhibitors with improved selectivity and antiproliferative activity
Herein, triphenylphosphonium cation moieties were incorporated into a
dichloroacetophenone derivative, leading to the discovery of novel mitochondria-targeted …
dichloroacetophenone derivative, leading to the discovery of novel mitochondria-targeted …
Targeting pyruvate dehydrogenase kinase signaling in the development of effective cancer therapy
Pyruvate is irreversibly decarboxylated to acetyl coenzyme A by mitochondrial pyruvate
dehydrogenase complex (PDC). Decarboxylation of pyruvate is considered a crucial step in …
dehydrogenase complex (PDC). Decarboxylation of pyruvate is considered a crucial step in …
Discovery of novel pyruvate dehydrogenase kinase 4 inhibitors for potential oral treatment of metabolic diseases
D Lee, HS Pagire, SH Pagire, EJ Bae… - Journal of Medicinal …, 2019 - ACS Publications
Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases
including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of …
including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of …