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 …
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 …
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
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 …
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 …
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 …
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 …
(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
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 …
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 …
Thienopyrimidines are an emerging class of fused pyrimidines due to their broad spectrum
of pharmacological properties, including antimicrobial, anti-inflammatory, antimalarial …
of pharmacological properties, including antimicrobial, anti-inflammatory, antimalarial …
Rare diseases and pyruvate kinase M2: a promising therapeutic connection
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 …
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 …
sustaining their phenotype of fast multiplication by continuously supplying energy and mass …