BIOMAT Database Logo BIOMAT Database Logo

Recent Advances in c-Jun N-Terminal Kinase (JNK) Inhibitors. 2021

Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Department of Oncology, Shunde Hospital, Southern Medical University (The First People's Hospital of Shunde), Foshan 528300, China.

c-Jun N-Terminal Kinases (JNKs), members of the Mitogen-Activated Protein Kinase (MAPK) signaling pathway, play a key role in the pathogenesis of many diseases including cancer, inflammation, Parkinson's disease, Alzheimer's disease, cardiovascular disease, obesity, and diabetes. Therefore, JNKs represent new and excellent target by therapeutic agents. Many JNK inhibitors based on different molecular scaffolds have been discovered in the past decade. However, only a few of them have advanced to clinical trials. The major obstacle for the development of JNK inhibitors as therapeutic agents is the JNKisoform selectivity. In this review, we describe the recent development of JNK inhibitors, including ATP competitive and ATP non-competitive (allosteric) inhibitors, bidentatebinding inhibitors and dual inhibitors, the challenges, and the future direction of JNK inhibitors as potential therapeutic agents.

UI MeSH Term Description Entries
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D048031 JNK Mitogen-Activated Protein Kinases A subgroup of mitogen-activated protein kinases that activate TRANSCRIPTION FACTOR AP-1 via the phosphorylation of C-JUN PROTEINS. They are components of intracellular signaling pathways that regulate CELL PROLIFERATION; APOPTOSIS; and CELL DIFFERENTIATION. jun N-Terminal Kinase,c-jun Amino-Terminal Kinase,c-jun N-Terminal Kinase,jun-NH2-Terminal Kinase,jun-NH2-Terminal Kinases,Amino-Terminal Kinase, c-jun,JNK Mitogen Activated Protein Kinases,Kinase, jun N-Terminal,N-Terminal Kinase, c-jun,N-Terminal Kinase, jun,c jun Amino Terminal Kinase,c jun N Terminal Kinase,jun N Terminal Kinase,jun NH2 Terminal Kinase,jun NH2 Terminal Kinases
D020935 MAP Kinase Signaling System An intracellular signaling system involving the mitogen-activated protein kinase cascades (three-membered protein kinase cascades). Various upstream activators, which act in response to extracellular stimuli, trigger the cascades by activating the first member of a cascade, MAP KINASE KINASE KINASES; (MAPKKKs). Activated MAPKKKs phosphorylate MITOGEN-ACTIVATED PROTEIN KINASE KINASES which in turn phosphorylate the MITOGEN-ACTIVATED PROTEIN KINASES; (MAPKs). The MAPKs then act on various downstream targets to affect gene expression. In mammals, there are several distinct MAP kinase pathways including the ERK (extracellular signal-regulated kinase) pathway, the SAPK/JNK (stress-activated protein kinase/c-jun kinase) pathway, and the p38 kinase pathway. There is some sharing of components among the pathways depending on which stimulus originates activation of the cascade. MAP Kinase Cascade,MAP Kinase Module,MAP Kinase Signaling Cascade,MAP Kinase Signaling Pathway,MAP Kinase Signaling Pathways,ERK Pathway,ERK Signal Tranduction Pathway,ERK1 and ERK2 Pathway,ERK1-2 Pathway,JNK Pathway,JNK Signaling Pathway,MAP Kinase Modules,MAP Kinase Signaling Cascades,MEK-ERK Pathway,p38 Kinase Pathway,p38 Kinase Signaling Pathway,Cascade, MAP Kinase,ERK Pathways,ERK1 2 Pathway,ERK1-2 Pathways,JNK Pathways,JNK Signaling Pathways,Kinase Cascade, MAP,Kinase Pathway, p38,Kinase Pathways, p38,MAP Kinase Cascades,MEK ERK Pathway,MEK-ERK Pathways,Module, MAP Kinase,Pathway, ERK,Pathway, ERK1-2,Pathway, JNK,Pathway, JNK Signaling,Pathway, MEK-ERK,Pathway, p38 Kinase,Pathways, ERK,Pathways, ERK1-2,Pathways, JNK,Pathways, JNK Signaling,Pathways, MEK-ERK,Pathways, p38 Kinase,Signaling Pathway, JNK,Signaling Pathways, JNK,p38 Kinase Pathways

Related Publications

Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
c-Jun N-terminal kinase (JNK) signaling: recent advances and challenges.
March 2010, Biochimica et biophysica acta,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Inhibitors of c-jun-N-terminal kinase (JNK).
July 2008, Mini reviews in medicinal chemistry,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Small molecule JNK (c-Jun N-terminal kinase) inhibitors.
April 2010, Journal of medicinal chemistry,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.
April 2015, ACS medicinal chemistry letters,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Novel Tryptanthrin Derivatives with Selectivity as c-Jun N-Terminal Kinase (JNK) 3 Inhibitors.
June 2023, Molecules (Basel, Switzerland),
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
June 2007, Bioorganic & medicinal chemistry letters,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Prolactin stimulates activation of c-jun N-terminal kinase (JNK).
October 2000, Molecular endocrinology (Baltimore, Md.),
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Alarmins and c-Jun N-Terminal Kinase (JNK) Signaling in Neuroinflammation.
October 2020, Cells,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors.
June 2009, Bioorganic & medicinal chemistry letters,
Gang Li, and Wenqing Qi, and Xiaoxun Li, and Jinwu Zhao, and Meihua Luo, and Jianjun Chen
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.
January 2014, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!