Histone deacetylases (HDACs) are a class of Zn(2+) dependent metalloproteases that play an important role in tumorigenesis. Inhibition of HDACs may be a potential strategy for cancer therapy. This study designed and synthesized a series of novel N-hydroxybenzamide histone deacetylase inhibitors based on the structural features of suberoylanilide hydroxamic acid (SAHA), the first HDAC inhibitor ...

In this study, a series of mastoparan analogs were engineered based on the strategies of Ala and Lys scanning in relation to the sequences of classical mastoparans. Ten analog mastoparans, presenting from zero to six Lys residues in their sequences were synthesized and assayed for some typical biological activities for this group of peptide: mast cell degranulation, hemolysis, and antibiosis. I...

The catalytic activity of human cytidine deaminase APOBEC3B (A3B) has been correlated with kataegic mutational patterns within multiple cancer types. The molecular basis of how the N-terminal non-catalytic CD1 regulates the catalytic activity and consequently, biological function of A3B remains relatively unknown. Here, we report the crystal structure of a soluble human A3B-CD1 variant and deli...

BACKGROUND The 1α,25-dihydroxy-3-epi-vitamin-D3 (1α,25(OH)2-3-epi-D3), a natural metabolite of the seco-steroid vitamin D3, exerts its biological activity through binding to its cognate vitamin D nuclear receptor (VDR), a ligand dependent transcription regulator. In vivo action of 1α,25(OH)2-3-epi-D3 is tissue-specific and exhibits lowest calcemic effect compared to that induced by 1α,25(OH)2D3...

Biological processes occur in complex environments containing a myriad of potential interactors. Unfortunately, limitations on the sensitivity of biophysical techniques normally restrict structural investigations to purified systems, at concentrations that are orders of magnitude above endogenous levels. Dynamic nuclear polarization (DNP) can dramatically enhance the sensitivity of nuclear magn...

objectives: aim of the present work was to investigate the anti-inflammatory, analgesic and antiulcer effects of red seaweed porphyra vietnamensis (p. vietnamenis). materials and methods: aqueous (por) and alcoholic (pe) fractions were successfully isolated from p. vietnamenis. further biological investigations were performed using a classic test of paw edema induced by carrageenan, writhing in...

Dynamical wiring and rewiring in neural networks are carried out by activity-dependent growth and retraction of axons and dendrites, guided by gudance molecules, released by target cells. Experience-dependent structural changes in cortical microcurcuts lead to changes in activity, i.e. to changes in information encoded. Specific pattens of external stimulation can lead to creation of new synapt...