[Design of Acetylcholinesterase Inhibitor for Alzheimer’s Disease Therapy: From Multi-Binding Site Inhibitors to Multi-Target Directed Ligands].

[Design of acetylcholinesterase inhibitor for Alzheimer’s disease therapy: from multi-binding site inhibitors to multi-target directed ligands].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Mar; 47(3): 313-21
Yang WC, Sun Q, Yu NX, Zhu XL, Yang GF

Alzheimer’s disease (AD) is a complex neurodegenerative disorder which seriously causes the dementia in elderly people and afflicts millions of people worldwide. Drug discovery for Alzheimer’s disease therapy has been a hot research area and a big challenge, in which development of acetylcholinesterase (AChE) inhibitors design was the most active and some AChE inhibitors are commercially available for AD medication already. However, practical using of commercial AChE inhibitors showed their limited usefulness and related adverse effects. Thus, it is extremely urgent to find novel AChE inhibitors with higher potency and less adverse effects. Based on the accurate crystallographic studies about AChE, strategies for multi-binding site AChE inhibitors have been formed, followed by design of the multi-target directed ligands. In this review, the structures and binding modes of commercial AChE inhibitors were briefly discussed, together with the development of AChE inhibitor design for AD therapy: from multi-binding site inhibitors to multi-target directed ligands.
HubMed – drug


[The application of small molecule bioactive probes in the identification of cellular targets].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Mar; 47(3): 299-306
Zhang J, Zhou HC

Identification of the cellular targets of bioactive compounds is a major challenge and a key issue in chemical biology and drug discovery. As an important technology in functional proteomics, small molecule probes play a pivotal role in the identification of cellular targets of bioactive compounds. This review is intended to introduce the application principles and structural design philosophy of chemical probes for the purpose of mechanistic study. Recent cases of successful application were also discussed to further demonstrate the principles and significance ofbioactive small molecule-based probes.
HubMed – drug


[Research progress of graphene-based materials in the application to biomedicine].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Mar; 47(3): 291-8
Jiang H, Wang XM, Wang CS

Graphene is a kind of atomic crystal with two-dimensional polycyclic aromatic hydrocarbons planes, which is of great concern in various fields. This paper reviews the latest development of graphene-based materials in biomedical research fields in the recent years, including in vitro and in vivo toxicity, drug loading, targeting controlled release, as well as photodynamic therapy. These researches validate that the graphene-based materials indicate promising prospects in the application to biomedicine.
HubMed – drug


[Progress in the study of some important natural bioactive cyclopeptides].

Filed under: Drug and Alcohol Rehabilitation

Yao Xue Xue Bao. 2012 Mar; 47(3): 271-9
Xu WY, Zhao SM, Zeng GZ, He WJ, Xu HM, Tan NH

Natural cyclopeptides are hot spots in chemical and pharmaceutical fields because of the wide spreading bio-resources, complex molecular structures and various bioactivities. Bio-producers of cyclopeptides distribute over almost every kingdom from bacteria to plants and animals. Many cyclopeptides contain non-coded amino acids and non-pepditic bonds. Most exciting characteristic of cyclopeptides is a range of interesting bioactivities such as antibiotics gramicidin-S (2), vancomycin (3) and daptomycin (4), immunosuppressive cyclosporin-A (1) and astin-C (8), and anti-tumor aplidine (5), RA-V (6) and RA-VII (7). Compounds 1-4 are being used in clinics; compounds 5-8 are in the stages of clinical trial or as a candidate for drug research. In this review, the progress in chemical and bioactive studies on these important natural bioactive cyclopeptides 1-8 are introduced, mainly including discovery, bioactivity, mechanism, QSAR and synthesis.
HubMed – drug


Meth Addiction, Drug-Related Crimes Plague an Indian Reservation

Filed under: Drug and Alcohol Rehabilitation

With tattoos peaking above his coat collar, he spoke calmly about his journey to recovery and his drive to be a good father. Looking back, he says he wasted most of his life on drugs. “I've never been off of parole,” he said.
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