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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
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
ent-Kaurane-based regio- and stereoselective inverse electron demand hetero-Diels-Alder reactions: synthesis of dihydropyran-fused diterpenoids.
TLDR
Efficient cross-HDA cycloadditions of this enone with various vinyl ethers or vinyl sulfides were achieved in a regio- and stereoselective manner, thus providing access to novel dihydropyran-fused diterpenoids as potential anticancer agents to overcome chemoresistance. Expand
Regio- and Stereospecific Synthesis of Oridonin D-Ring Aziridinated Analogues for the Treatment of Triple-Negative Breast Cancer via Mediated Irreversible Covalent Warheads.
Covalent drug discovery has undergone a resurgence in recent years due to comprehensive optimization of the structure-activity relationship (SAR) and the structure-reactivity relationship (SRR) forExpand
Enhanced effects of novel oridonin analog CYD0682 for hepatic fibrosis.
TLDR
In comparison with oridonin, its novel derivative CYD0682 may act as a more potent antihepatic fibrosis agent. Expand
Enhanced anti-fibrogenic effects of novel oridonin derivative CYD0692 in hepatic stellate cells
TLDR
The results indicated that pretreatment with CYD0692 blocked TGFβ1-induced FN expression, thereby decreasing the downstream factors of TGF β1 signaling, such as Phospho-Smad2/3 and phospho-ERK. Expand
BH4 domain of Bcl-2 as a novel target for cancer therapy.
TLDR
The proof-of-concept studies support the hypothesis that targeting the BH4 domain of Bcl-2 holds promise to offer a novel anticancer therapy through the induction of apoptosis and an increased potential to overcome therapeutic resistance. Expand
Modulation of Bax and mTOR for Cancer Therapeutics.
TLDR
The refinement of the Bax agonist SMBA1 to generate CYD-2-11, which has characteristics of a suitable clinical lead compound and provides preclinical evidence for a pharmacologic combination of Bax activation and mTOR inhibition as a rational strategy to improve lung cancer treatment. Expand
Discovery and development of natural product oridonin-inspired anticancer agents.
  • Ye Ding, C. Ding, +6 authors Jia Zhou
  • Chemistry, Medicine
  • European journal of medicinal chemistry
  • 21 October 2016
TLDR
This review summarizes the recent advances in medicinal chemistry on the explorations of novel oridonin analogues as potential anticancer therapeutics, and provides a detailed discussion of future directions for the development and progression of this class of molecules into the clinic. Expand
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