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 …

Novel sulfonamides unveiled as potent anti-lung cancer agents via tumor pyruvate kinase M2 activation

R Das, DR Chatterjee, S Kapoor, H Vyas… - RSC Medicinal …, 2024 - pubs.rsc.org
This rational pursuit led to the identification of a novel sulfonamide derivative as a potent anti-
lung cancer (LC) compound. Considering these results, we synthesized 38 novel …

Design and efficient synthesis of new 4-amino-substituted 2-(4-Bromobenzyl)-5, 6, 7, 8-tetrahydrobenzo [4, 5] thieno [2, 3-d] pyrimidines of anticancer interest and their …

S Arora, S Thakur, VR Kaki, R Kumar - Synthesis, 2025 - thieme-connect.com
Thienopyrimidines are an emerging class of fused pyrimidines due to their broad spectrum
of pharmacological properties, including antimicrobial, anti-inflammatory, antimalarial …

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 …

Polyphyllin II Induces Apoptosis in Fibrosarcoma Cells via Activating Pyruvate Kinase M2

J Wu, Z Ding, M Zhong, J **, Y He… - Chemical Research in …, 2024 - ACS Publications
Aerobic glycolysis is a metabolic reprogramming of tumor cells that is essential for
sustaining their phenotype of fast multiplication by continuously supplying energy and mass …