A tetrameric N-acetyl galactosaminyl (GalNAc) peptidomimetic was constructed by N-acetylation of repeating proline-based hydroxamic acid units, followed by a convergent 'click chemistry' coupling. This novel glycopeptidomimetic was determined to effectively antagonize the interaction between a transmembrane hepatic lectin and GalNAc on the cellular level.

A new Plasmodium falciparum histone deacetylase1 (PfHDAC1) homology model was built based on the highest sequence identity available template human histone deacetylase 2 structure. The generated model was carefully evaluated for stereochemical accuracy, folding correctness and overall structure quality. All evaluations were acceptable and consistent. Docking a group of hydroxamic acid histone d...

BACKGROUND AND OBJECTIVES Chromatin structure and thereby transcription is controlled by the level of acetylation of histones, which is determined by the balance between histone acetyl transferase (HAT) activity and histone deacetylase (HDAC) activity. HDAC inhibitors are a class of compounds able to regulate gene expression by modulating chromatin structure. There are two major classes of HDAC...

Simple hydroxamic acids (XHA) are hydrophilic organic compoundswith the general formula RCONHOH that can act as O,O donor ligands with high affinities for hard cations such as Fe3+, Np4+ and Pu4+ with which they form 5-membered chelate rings (Muri et al.,2002; Desaraju & Winston,1986; Carrott et al.,2007). They have a wide range of applications in many fields, including as enzyme inhibitors, so...