Design, synthesis and biological activity evaluation of novel covalent S-acylation inhibitors

Article Chemistry, Medicinal

Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma

Jifeng Qi et al.

Summary: PI3K delta inhibitors with a new chemical structure show superior efficacy and mechanism in the treatment of hepatocellular carcinoma.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Oncology

E2F1-induced microRNA-224-5p expression is associated with hepatocellular carcinoma cell migration, invasion and epithelial-mesenchymal transition via MREG

An Li et al.

Summary: miR-224-5p is downregulated in hepatocellular carcinoma and inhibits cell migration, invasion, and EMT. E2F1 regulates the expression of miR-224-5p and promotes cancer cell migration, invasion, and EMT. miR-224-5p exerts its function by targeting MREG.

ONCOLOGY LETTERS (2022)

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Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Novel Evodiamine Derivatives as Potential Antihepatocellular Carcinoma Agents

Fang Lei et al.

Summary: In this study, 23 disubstituted derivatives of Evodiamine were synthesized and their structure-activity relationship was investigated. Compounds F-3 and F-4 exhibited significant in vitro antiproliferative activity and possessed the ability to inhibit tumor cell invasion, arrest the cell cycle, and induce apoptosis. Compound F-4 also showed potential in inhibiting the progression of liver fibrosis and tumor growth.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Artemisinin inhibits NRas palmitoylation by targeting the protein acyltransferase ZDHHC6

Nan Qiu et al.

Summary: Protein S-palmitoylation is crucial in cancer cells, and artemisinin, a clinically approved antimalarial drug, has been found to inhibit a specific palmitoyl transferase, reducing palmitoylation of oncogenic proteins and disrupting cell proliferation signaling cascades.

CELL CHEMICAL BIOLOGY (2022)

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Review Biochemistry & Molecular Biology

Inhibitors of DHHC family proteins

Tong Lan et al.

Summary: Protein S-acylation is a dynamically regulated post-translational protein lipidation process, with DHHC proteins being recognized as critical regulators of S-acylation-mediated cellular processes. The increasing demand for chemical inhibitors of DHHC proteins has led to focus on inhibitors such as 2-bromopalmitate and N-cyanomethyl-N-myracrylamide. Advances in structure elucidation, mechanistic interrogation, and novel inhibitor design around DHHC proteins are expected to spark innovative strategies for modulating these critical proteins in living systems.

CURRENT OPINION IN CHEMICAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology

Development of an Acrylamide-Based Inhibitor of Protein S-Acylation

Saara-Anne Azizi et al.

Summary: Protein S-acylation is a dynamic lipid post-translational modification that can modulate the localization and activity of target proteins. A new broad-spectrum DHHC family inhibitor called cyano-myracrylamide (CMA) was synthesized and characterized, showing potent inhibition of DHHC family proteins with decreased toxicity and avoidance of inhibiting the S-acylation eraser enzymes. CMA provides an improved chemical scaffold for understanding the complexities of DHHC-mediated cell signaling by protein S-acylation.

ACS CHEMICAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology

High-Throughput Enzyme Assay for Screening Inhibitors of the ZDHHC3/7/20 Acyltransferases

Jun Young Hong et al.

Summary: Researchers have developed a ZDHHC3/7/20 high-throughput assay based on the Acyl-cLIP method to accelerate the screening of improved ZDHHC inhibitors for treating cancer and autoimmune diseases.

ACS CHEMICAL BIOLOGY (2021)

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Article Cell Biology

Potential Role of S-Palmitoylation in Cancer Stem Cells of Lung Adenocarcinoma

Yitong Zhang et al.

Summary: The study suggests that S-palmitoylation of INCENP mediated by ZDHHC5 may be a potential mechanism to regulate cancer stem cells in lung adenocarcinoma (LUAD).

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology