Molecular glues: enhanced protein-protein interactions and cell proteome editing

EG Weagel, JM Foulks, A Siddiqui… - Medicinal Chemistry …, 2022 - Springer
The druggable genome is limited by structural features that can be targeted by small
molecules in disease-relevant proteins. While orthosteric and allosteric protein modulators …

Lactate and lactylation: Behind the development of tumors

E Dai, W Wang, Y Li, D Ye, Y Li - Cancer Letters, 2024 - Elsevier
There is growing evidence that lactate can have a wide range of biological impacts in
addition to being a waste product of metabolism. Because of the Warburg effect, tumors …

S-lactoyl modification of KEAP1 by a reactive glycolytic metabolite activates NRF2 signaling

Y Ko, M Hong, S Lee, M Kumar… - Proceedings of the …, 2023 - National Acad Sciences
KEAP1 (Kelch-like ECH-associated protein), a cytoplasmic repressor of the oxidative stress
responsive transcription factor Nuclear factor erythroid 2-related factor 2 (NRF2), senses the …

Discovery of novel sesquiterpene lactone derivatives as potent PKM2 activators for the treatment of ulcerative colitis

P Wang, H Yang, W Lin, J Zhou, Y Liu… - Journal of Medicinal …, 2023 - ACS Publications
The pyruvate kinase M2 (PKM2) can significantly affect the differentiation of Th17 and Treg
cells; thus, it is considered a promising target for UC therapy. Herein, five series of …

Anti-tumor effects of novel alkannin derivatives with potent selectivity on comprehensive analysis

Z Dai, F Gao, Z Zhang, M Lu, Y Luo, T Zhang, B Shang… - Phytomedicine, 2023 - Elsevier
Background Therapeutic approaches based on glycolysis and energy metabolism of tumor
cells are new promising strategies for the treatment of cancer. Currently, researches on the …

Integration with Transcriptomic and Metabolomic Analyses Reveals the In Vitro Cytotoxic Mechanisms of Chinese Poplar Propolis by Triggering the Glucose …

Y Guo, Z Liu, Q Wu, Z Li, J Yang, H Xuan - Nutrients, 2023 - mdpi.com
Natural products serve as a valuable reservoir of anticancer agents. Chinese poplar propolis
(CP) has exhibited remarkable antitumor activities, yet its precise mechanisms of action …

Rare diseases and pyruvate kinase M2: a promising therapeutic connection

S Kapoor, V Kalmegh, H Kumar, A Mandoli… - Drug Discovery …, 2024 - Elsevier
Abstract Pyruvate kinase M2 (PKM2) is a key glycolytic enzyme that regulates proliferating
cell metabolism. The role of PKM2 in common diseases has been well established, but its …

GalaxySagittarius-AF: Predicting Targets for Drug-Like Compounds in the Extended Human 3D Proteome

S Kwon, N Jung, J Yang, C Seok - Journal of Molecular Biology, 2024 - Elsevier
In recent years, advancements in deep learning techniques have significantly expanded the
structural coverage of the human proteome. GalaxySagittarius-AF translates these …

Design, Synthesis and Biological Evaluation of Quinoline-8-Sulfonamides as Inhibitors of the Tumor Cell-Specific M2 Isoform of Pyruvate Kinase: Preliminary Study

K Marciniec, Z Rzepka, E Chrobak, S Boryczka… - Molecules, 2023 - mdpi.com
Cancer cells need to carefully regulate their metabolism to keep them growing and dividing
under the influence of different nutrients and oxygen levels. Muscle isoform 2 of pyruvate …

Development of isoselenazolium chlorides as selective pyruvate kinase isoform M2 inhibitors

P Dimitrijevs, M Makrecka-Kuka, A Bogucka… - European Journal of …, 2023 - Elsevier
Alterations in cancer metabolic pathways open up an opportunity for targeted and effective
elimination of tumor cells. Pyruvate kinase M2 (PKM2) is predominantly expressed in …