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Transcription Factor STAT3 as a Novel Molecular Target for Cancer Prevention
TLDR
Current literature is summarized, the potential importance of STAT3 as a novel target for cancer prevention and ofSTAT3 inhibitors as effective chemopreventive agents are discussed and the lag in developing effective STAT3 inhibitors is summarized. Expand
Small Molecule Inhibitors Targeting Activator Protein 1 (AP-1)
TLDR
Despite significant advances achieved in understanding AP-1 biology and function, medicinal chemistry efforts remain an urgent need to yield selective and efficaciousAP-1 inhibitors as a viable therapeutic strategy for human diseases. Expand
5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP.
TLDR
SAR analysis led to the identification of three more potent Epac antagonists (6b, 6g, and 6h), which may serve as valuable pharmacological probes for further elucidation of the physiological functions and mechanisms of Epac regulation. Expand
Intestinal microbiota-derived short-chain fatty acids regulation of immune cell IL-22 production and gut immunity
TLDR
It is shown that microbiota-derived short-chain fatty acids (SCFAs) promote IL-22 production by CD4+ T cells and ILCs through G-protein receptor 41 (GPR41) and inhibiting histone deacetylase (HDAC) and that SCFA supplementation enhances IL- 22 production, which protects intestines from inflammation. Expand
Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents.
TLDR
This review summarizes the current status of the structural diversity and evolution in medicinal chemistry of UA analogues and provides a detailed discussion of future direction for further research in the chemical modifications of UA. Expand
Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy.
TLDR
A small-molecule Bcl2-BH4 domain antagonist, BDA-366, that binds BH4 with high affinity and selectivity is identified that exhibits strong synergy against lung cancer in vivo. Expand
Fragment-based drug design and identification of HJC0123, a novel orally bioavailable STAT3 inhibitor for cancer therapy.
TLDR
The fragment-based drug design, systematic chemical synthesis and pharmacological evaluation of novel scaffolds as potent anticancer agents by utilizing six privileged fragments from known STAT3 inhibitors are reported, indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy. Expand
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
TLDR
The chemical design, synthesis, and pharmacological characterization of three different scaffolds (diarylsulfones, N,N-diarylamines, and arylsulfonamides) as highly potent and selective antagonists of EPAC2 are reported. Expand
Direct Activation of Bax Protein for Cancer Therapy
TLDR
Intriguingly, recent efforts demonstrate that Bax can serve as a promising direct target for small‐molecule drug discovery and several direct Bax activators have been identified to hold promise for cancer therapy with the advantages of specificity and the potential of overcoming chemo‐ and radioresistance. Expand
Biochemical and Pharmacological Characterizations of ESI-09 Based EPAC Inhibitors: Defining the ESI-09 “Therapeutic Window”
TLDR
It is demonstrated that ESI-09 indeed acts as an EPAC specific antagonist and does not significantly destabilize/denature proteins at pharmacological effective concentrations, which is further supported by NMR data showing that E SI-09 induces residue-dependent chemical shift changes at low concentrations, while preserving well dispersed peaks. Expand
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