Inhibition of glycolysis and glutaminolysis: an emerging drug discovery approach to combat cancer
Cancer cells have a very different metabolism from that of normal cells from which they are
derived. Their metabolism is elevated, which allows them to sustain higher proliferative rate …
derived. Their metabolism is elevated, which allows them to sustain higher proliferative rate …
Recent advances of IDH1 mutant inhibitor in cancer therapy
W Tian, W Zhang, Y Wang, R Jin, Y Wang… - Frontiers in …, 2022 - frontiersin.org
Isocitrate dehydrogenase (IDH) is the key metabolic enzyme that catalyzes the conversion of
isocitrate to α-ketoglutarate (α-KG). Two main types of IDH1 and IDH2 are present in …
isocitrate to α-ketoglutarate (α-KG). Two main types of IDH1 and IDH2 are present in …
Molecular mechanisms mediating relapse following ivosidenib monotherapy in IDH1-mutant relapsed or refractory AML
S Choe, H Wang, CD DiNardo, EM Stein… - Blood …, 2020 - ashpublications.org
Abstract Isocitrate dehydrogenase (IDH) 1 and 2 mutations result in overproduction of D-2-
hydroxyglutarate (2-HG) and impaired cellular differentiation. Ivosidenib, a targeted mutant …
hydroxyglutarate (2-HG) and impaired cellular differentiation. Ivosidenib, a targeted mutant …
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma
QX Wang, PY Zhang, QQ Li, ZJ Tong, JZ Wu… - European Journal of …, 2023 - Elsevier
Glioma is one of the most common types of brain tumors, and its high recurrence and
mortality rates threaten human health. In 2008, the frequent isocitrate dehydrogenase 1 …
mortality rates threaten human health. In 2008, the frequent isocitrate dehydrogenase 1 …
Discovery and optimization of quinolinone derivatives as potent, selective, and orally bioavailable mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors
J Lin, W Lu, JA Caravella, AM Campbell… - Journal of medicinal …, 2019 - ACS Publications
Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently
identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small molecules …
identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small molecules …
Beyond brooding on oncometabolic havoc in IDH-mutant gliomas and AML: current and future therapeutic strategies
Isocitrate dehydrogenases 1 and 2 (IDH1, 2), the key Krebs cycle enzymes that generate
NADPH reducing equivalents, undergo heterozygous mutations in> 70% of low-to mid …
NADPH reducing equivalents, undergo heterozygous mutations in> 70% of low-to mid …
Disabling uncompetitive inhibition of oncogenic IDH mutations drives acquired resistance
Mutations in IDH genes occur frequently in acute myeloid leukemia (AML) and other human
cancers to generate the oncometabolite R-2HG. Allosteric inhibition of mutant IDH …
cancers to generate the oncometabolite R-2HG. Allosteric inhibition of mutant IDH …
Stereo-and regioselective 1, 3-dipolar cycloaddition of the stable ninhydrin-derived azomethine ylide to cyclopropenes: Trapping of unstable cyclopropene …
AS Filatov, S Wang, OV Khoroshilova… - The Journal of …, 2019 - ACS Publications
A stereo-and regioselective 1, 3-dipolar cycloaddition of the stable ninhydrin-derived
azomethine ylide [2-(3, 4-dihydro-2 H-pyrrolium-1-yl)-1-oxo-1 H-inden-3-olate, DHPO] to …
azomethine ylide [2-(3, 4-dihydro-2 H-pyrrolium-1-yl)-1-oxo-1 H-inden-3-olate, DHPO] to …
Asymmetric construction of 3-azabicyclo [3.1. 0] hexane skeleton with five contiguous stereogenic centers by Cu-catalyzed 1, 3-dipolar cycloaddition of trisubstituted …
H Deng, WL Yang, F Tian, W Tang, WP Deng - Organic letters, 2018 - ACS Publications
A highly diastereo-and enantioselective desymmetrization of prochiral cyclopropenes via a
Cu (CH3CN) 4BF4/Ph-Phosferrox complex catalyzed 1, 3-dipolar cycloaddition of …
Cu (CH3CN) 4BF4/Ph-Phosferrox complex catalyzed 1, 3-dipolar cycloaddition of …
[HTML][HTML] The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer
Y Liu, W Xu, M Li, Y Yang, D Sun, L Chen, H Li… - … Pharmaceutica Sinica B, 2023 - Elsevier
Reprogramming of energy metabolism is one of the basic characteristics of cancer and has
been proved to be an important cancer treatment strategy. Isocitrate dehydrogenases (IDHs) …
been proved to be an important cancer treatment strategy. Isocitrate dehydrogenases (IDHs) …