Structural manipulations of marine natural products inspire a new library of 3-amino-1, 2, 4-triazine PDK inhibitors endowed with antitumor activity in pancreatic ductal …
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 …
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 …
Discovery of the 3-amino-1, 2, 4-triazine-based library as selective PDK1 inhibitors with therapeutic potential in highly aggressive pancreatic ductal adenocarcinoma
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 …
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 …
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 …
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 …
central role in the cancer metabolic switch by blocking pyruvate catabolism in the TCA cycle …
Discovery of 3, 6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico …
A Sabt, WM Eldehna, T Al-Warhi… - Journal of Enzyme …, 2020 - Taylor & Francis
Human health in the current medical era is facing numerous challenges, especially cancer.
So, the therapeutic arsenal for cancer should be unremittingly enriched with novel small …
So, the therapeutic arsenal for cancer should be unremittingly enriched with novel small …
Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold
An efficient synthesis of substituted pyrido [2, 3-d] pyrimidines was carried out and evaluated
for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2) …
for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2) …
Targeting the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual …
L Gan, Y Yang, Z Liang, M Zhang, Y He… - European Journal of …, 2024 - Elsevier
Proliferating cancer cells are characterized by the Warburg effect, a metabolic alteration in
which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation …
which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation …
Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors
NJ O'Brien, M Brzozowski, MJ Buskes… - Bioorganic & medicinal …, 2014 - Elsevier
PDK1, a biological target that has attracted a large amount of attention recently, is
responsible for the positive regulation of the PI3K/Akt pathway that is often activated in a …
responsible for the positive regulation of the PI3K/Akt pathway that is often activated in a …
相关搜索
- structural manipulations pdk inhibitors
- antitumor activity pdk inhibitors
- structural manipulations antitumor activity
- pyruvate dehydrogenase pdk inhibitors
- anticancer activity pancreatic cancer
- pharmacological evaluation pdk inhibitors
- cdk1 inhibitors pancreatic cancer
- virtual screening pdk inhibitors
- cdk1 inhibitors anticancer activity