Current Medicinal Chemistry - Volume 7, Issue 12, 2000

Calpain is unique among the cysteine protease family of enzymes in that it combines thiol protease activity with calmodulin-like activity. Despite its wide spread distribution the exact physiological function(s) of calpain is yet to be deciphered. The enzyme is however, implicated in a number of pathophysiological conditions. Due to the potential of calpain as a therapeutic target a number of inhibitors have been described for the Read More

DNA topoisomerases are essential for the survival of prokaryotic and eukaryotic organisms. Topoisomerases inhibitors, due to their capacity to induce DNA breaking, can exhibit interesting antitumor properties. While there are many potent antitumor agents which target topoisomerase II, relatively few families of specific topoisomerase I inhibitors have been identified.The present review describes a new family of topoisom Read More

Initiation, progression, and completion of the cell cycle are regulated by various cyclin-dependent kinases (CDKs), which are thus critical for cell growth. Tumour development is closely associated with genetic alteration and deregulation of CDKs and their regulators, suggesting that inhibitors of CDKs may be useful anti-cancer therapeutics. Indeed, early results suggest that transformed and normal cells differ in their requirem Read More

Crisis periods in development are critical periods of cell death that have long been suggested as “epigenetic crises” which are central to normal and abnormal embryogenesis. Under in-vitro culture conditions, there are similar crisis periods or Hayflick limits of culture senescence. Epigenetic modulations from CpG methylation coupled to DNA replication provide an alternate timing mechanism to the telomere/telomerase biolo Read More

Radical induced oxidative damage is extremely harmful to tissues and organs due to molecular modifications brought to polyunsaturated membrane lipids, proteins and nucleic acids. Oxidative stress is believed to be one of the pathophysiological mechanisms that operate in neurodegenerative disorders such as cerebral ischemias, amyotrophic lateral sclerosis, Parkinson's and Alzheimer's diseases.Nitrones o Read More

Developments in the field of adenosine receptor (AR) agonists of the past years are presented and discussed. Four different AR subtypes, A1, A2A, A2B, and A3, have been cloned from different species including the human receptors. Recombinant ARs expressed in permanent mammalian cell lines have found wide application in the screening of new ligands. Considerable differences are observed among data from different lab Read More

The metallocene dihalides are a relatively new class of small, hydrophobic organometallic anticancer agents that exhibit antitumour properties against numerous cell lines including leukemias P388 and L1210, colon 38 and Lewis lung carcinomas, B16 melanoma, solid and fluid Ehrlich ascites tumours and several human colon and lung carcinomas transplanted into athymic mice. Titanocene dichloride 1 has been the most wide Read More

20-Hydroxyecdysone (20E) is an insect molting hormone that is also widely spread in various plants. Many chromatographic methods can be used to identify and/or determine 20E content in samples of biological origin and various spectroscopic methods serve to identify its structural elements. We have utilized X-ray crystallography to reveal the stereostructures of 20E. Our data demonstrates that 20E exists in two different crys Read More