J W Clader
J W Clader
characterized by loss of cholinergic neurons in regions of the brain that are known to be involved in learning and memory. Cholinergic therapy seeks to compensate for this loss by pharmacological enhancement of cholinergic transmission. The...
Structure-activity relationships and pharmacological profiles of new 5-HT(1) receptor agonists as antimigraine agents [0.03%]
新型5-HT₁受体激动剂的结构活性关系及其药理学特性研究（抗偏头痛药物）
M Perez,G W John
M Perez
The design of new generation drugs acting as 5-HT1 receptor agonists, in the field of acute treatment of migraine, is still very active. The reason is the need for safer medicines with improved response rates and a reduced rate of headache ...
Development of somatostatin receptor subtype selective agonists through combinatorial chemistry [0.03%]
采用组合化学合成选择性促生长抑素受体配体的方法研究
S P Rohrer,S C Berk
S P Rohrer
Non-peptide agonists of each of the five somatostatin receptors were identified from a combinatorial mixture library and three follow-up libraries. The initial library (20 x 20 x 79) was patterned after a lead structure which was identified...
A George
A George
The medical need for new drugs to treat CNS disorders and their commercial potential is not in question, however, CNS drugs may require different pharmacokinetic and pharmacological profiles to peripherally acting compounds. The role of mol...
Recent advances in protein kinase inhibition: current molecular scaffolds used for inhibitor synthesis [0.03%]
蛋白激酶抑制的最新进展：用于合成抑制剂的当前分子支架
D R Stover,N B Lydon,J J Nunes
D R Stover
Early efforts to discover and develop protein kinase inhibitors have focused largely on a small group of oncology targets such as the EGFR and PKC enzymes. More recently, hundreds of protein kinases have been identified at the genetic level...
HIV protease drug resistance and its impact on inhibitor design [0.03%]
人类免疫缺陷病毒蛋白酶的药物抗性和其对抑制剂设计的影响研究进展
P J Ala,J D Rodgers,C H Chang
P J Ala
The primary cause of resistance to the currently available HIV protease inhibitors is the accumulation of multiple mutations in the viral protease. So far more than 20 substitutions have been observed in the active site, dimer interface, su...
Editorial overview. The chemistry of drug design and lead optimization [0.03%]
综述评论。药物设计和先导化合物优化的化学研究
W J Greenlee,M Desai
W J Greenlee
R Krebs
R Krebs
A review of the literature published from late 1997 to the end of 1998 reveals a shift in paradigm of the discovery process and hence the productivity of pharmaceutical companies. Key factors are combined use in high-throughput screening sy...
The use of informatics and automation to remove bottlenecks in drug discovery [0.03%]
利用信息技术和自动化消除药物发现瓶颈
S Calvert,F P Stewart,K Swarna et al.
S Calvert et al.
Advances in molecular biology and genetics have furnished more targets than could be reasonably progressed, forcing the pharmaceutical industry to invest in increasing chemistry and screening throughput. Combinatorial chemistry, automation ...
J Antel
J Antel
During the past 15 years, the focus of the drug design community has undergone considerable change. After decades dedicated to studying traditional folk medicine and the biological activity of natural compounds as the major source of drugs,...