[HTML][HTML] Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

X Peng, Z Hu, L Zeng, M Zhang, C Xu, B Lu… - … Pharmaceutica Sinica B, 2024 - Elsevier
Epigenetic pathways play a critical role in the initiation, progression, and metastasis of
cancer. Over the past few decades, significant progress has been made in the development …

[HTML][HTML] The current status and future prospects for therapeutic targeting of KEAP1-NRF2 and β-TrCP-NRF2 interactions in cancer chemoresistance

R Srivastava, R Fernández-Ginés, JA Encinar… - Free Radical Biology …, 2022 - Elsevier
Drug resistance is one of the biggest challenges in cancer treatment and limits the potential
to cure patients. In many tumors, sustained activation of the protein NRF2 makes tumor cells …

Activation of human STING by a molecular glue-like compound

J Li, SM Canham, H Wu, M Henault, L Chen… - Nature chemical …, 2024 - nature.com
Stimulator of interferon genes (STING) is a dimeric transmembrane adapter protein that
plays a key role in the human innate immune response to infection and has been …

Biomimetic synthesis and chemical proteomics reveal the mechanism of action and functional targets of phloroglucinol meroterpenoids

AK Bracken, CE Gekko, NO Suss… - Journal of the …, 2024 - ACS Publications
Natural products perennially serve as prolific sources of drug leads and chemical probes,
fueling the development of numerous therapeutics. Despite their scarcity, natural products …

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Targeted protein degradation: principles and applications of the proteasome

Y Kim, EK Kim, Y Chey, MJ Song, HH Jang - Cells, 2023 - mdpi.com
The proteasome is a multi-catalytic protease complex that is involved in protein quality
control via three proteolytic activities (ie, caspase-, trypsin-, and chymotrypsin-like activities) …

FLT3-PROTACs for combating AML resistance: Analytical overview on chimeric agents developed, challenges, and future perspectives

HM Hesham, EME Dokla, EZ Elrazaz… - European Journal of …, 2024 - Elsevier
The urgent and unmet medical demand of acute myeloid leukemia (AML) patients has
driven the drug discovery process for expansion of the landscape of AML treatment. Despite …

Molecular glue degraders: exciting opportunities for novel drug discovery

T Lemaitre, M Cornu, F Schwalen, M Since… - Expert Opinion on …, 2024 - Taylor & Francis
ABSTRACT Introduction Molecular Glue Degraders (MGDs) is a concept that refers to a
class of compounds that facilitate the interaction between two proteins or molecules within a …

New insights into protein–protein interaction modulators in drug discovery and therapeutic advance

H Nada, Y Choi, S Kim, KS Jeong… - … and Targeted Therapy, 2024 - nature.com
Protein-protein interactions (PPIs) are fundamental to cellular signaling and transduction
which marks them as attractive therapeutic drug development targets. What were once …

Dual-site molecular glues for enhancing protein-protein interactions of the CDK12-DDB1 complex

Z Zhang, Y Li, J Yang, J Li, X Lin, T Liu, S Yang… - Nature …, 2024 - nature.com
Protein-protein interactions (PPIs) stabilization with molecular glues plays a crucial role in
drug discovery, albeit with significant challenges. In this study, we propose a dual-site …