Current Topics in Medicinal Chemistry - Volume 15, Issue 8, 2015

Kruppel-like factor 5 (KLF5) belongs to a family of zinc-finger-containing transcription factors which are involved in regulating expression of a wide range of genes, thereby affecting diverse cellular functions. The activities of KLF5 are regulated by multiple signaling pathways including Wnt, Ras, TGFβ, Hippo, Notch, retinoid acid receptor, and hormone receptors. The expression of KLF5 is frequently abnormal in human cancers an Read More

In recent years, there has been an increased effort in the development of therapies which target an epigenetic mode of action. Among thes e efforts include progress in the development of inhibitors of EZH2 (Enhancer of Zeste Homolog 2), a key epigenetic target with strong disease implications to cancer. Over the last 3+ years, multiple reports describing small molecule inhibitors of EZH2 have been described, includ Read More

Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded as a potential target for anticancer therapy. As a suppressor pathway, autophagy prevents tumor initi Read More

The mitochondrion’s negatively charged membrane potential has been well documented to drive the accumulation of membrane permeable delocalized lipophilic cations (DLC). DLC attachments to known bioactive compounds can direct organelle localization and improve drug exposure to targets within the mitochondria. Due to the mitochondria’s essential function and its regulation of cell death, DLC targeted therapies are Read More

Due to ever-increasing failure rates, high cost, unsatisfactory safety profile, and limited efficacy associated with anticancer drug development, the repositioning of established non-cancer drugs for new oncology indications has emerged as an increasingly attractive approach to addressing the unmet cancer-related medical need. With the rapid development of bioinformatics, chemoinformatics as well as high-performance com Read More

Lysine acetylation is a pivotal mechanism in chromatin processes and the regulation of gene transcription. The acetylated lysine residues of histones are exclusively recognized by bromodomains (BRDs) known as epigenetic reader. Proteins containing BRDs undergo a post-translational modification (PTM) with development of cellular signaling and disease biology. The bromo and extra-terminal (BET) proteins are the seco Read More

Positron emission tomography (PET) is one of the most rapidly growing areas of medical imaging for cancer research. The principal goal of PET imaging is to visualize, characterize, and measure biological processes at the molecular and cellular levels in living subjects using non-invasive procedures. Taking advantage of the traditional diagnostic imaging techniques, PET imaging introduces positron-emitting probes to dete Read More