Albendazole is a member of the benzimidazole group of anthelmintics with broad-spectrum activity against gastro-intestinal roundworms including inhibited larval stages, tapeworms, liver flukes and lungworms in many species. In the […]
Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists
The vertebrate orexin neuropeptide–receptor system plays a pivotal role in the regulation of sleep and wake states as well as emotional states related to stress or reward. The neuropeptides orexin […]
Small-molecule modulators of the Sonic Hedgehog signaling pathway Shh pathway inhibition with non-naturally occurring small molecules Cell-based assays with reporter gene constructs have been widely used for discovering non-naturally occurring […]
The ADP-ribosyltranferase diphtheria toxin-like (ARTD) or poly-ADP-ribose polymerase (PARP) protein superfamily comprises 17 proteins that contain a common catalytic domain. Those that are catalytically active use β-NAD+ as an essential […]
Ya-tong-yi-li-wan (YTYLW) is a well-known traditional Chinese medicine (TCM) formula composed of ChanSu (toad venom), licorice root, realgar, and cinnabaris in the ratio of 24 : 24 : 6 : […]
Semi-synthetic glycopeptide antibiotics Oritavancin, telavancin and dalbavancin Early studies by Nagarajan et al. into the development of semi-synthetic glycopeptide antibiotics focused on utilizing vancomycin as a structural […]
Nanomaterials with easy surface functionalization and high biocompatibility have emerged as good candidates for theranostic applications. In particular the integration of multiple smart functions such as contrast agents (CA) and […]
The cathepsins comprise a family of lysosomal proteolytic enzymes. Eleven human cathepsins are cysteine proteases of the papain-like subfamily C1A and represent the best characterized group of cathepsins. Cysteine cathepsins […]
Epigenetic therapies from natural products in the clinic 1. Clinically approved natural product epigenetic modulators Despite an increasing number of synthetically-derived epigenetic modulators being taken into preclinical and clinical studies, […]
Xanthones with various substituents on the three-membered heterocyclic ring skeleton exhibit diverse biological activities, such as antihypertensive, antioxidative, antithrombotic and anticancer activities. Naturally existing xanthone analogues, including gentiakochianin, α-mangostin and […]