Current Medicinal Chemistry - Volume 9, Issue 24, 2002

One challenge associated with the clinical use of protein therapeutics destined for chronic administration is the potential for the development of unwanted anti-drug immune reactions. The molecular basis for this reactivity is the binding of peptide fragments (epitopes) derived from the breakdown of the protein drug to the HLA receptors expressed by the patient's immune cells. If these epitopes are recognized as “foreig Read More

Cytokines are powerful molecules that the body's immune cells secrete in response to an offending agent. Their main function is to direct the immune response into the most effective pathway that will eventually result in elimination of the offender. The last decade was marked by an enormous and ever growing interest that led to discovery of numerous cytokine molecules and their amazing influence on the body im Read More

The most important natural sources of new leads are plant extracts, bacterial broths, animal venoms and peptides isolated from living organisms. However, only the three first have been used extensively in the development of new therapeutic agents. This is probably due to the low pharmacological profile exhibited by peptides, that requires a lengthy transformation to make them suitable as new leads. In contrast, bi Read More

Diabetes mellitus refers to a spectrum of syndromes characterized by abnormally high levels of glucose in blood. These syndromes are associated with an absolute (Type 1 diabetes) or relative (Type 2 diabetes) deficiency of insulin, coupled with varying degrees of peripheral resistance to the actions of insulin. Clinical studies have shown that controlling hyperglycemia significantly reduces the appearance and progression of th Read More

Design and synthesis of metabolically stable peptide analogs that can either mimic or block the bioactivity of natural peptides or enzymes is an important constituent of bioorganic and medicinal chemistry research. Isosteric replacement of a scissile peptide bond represents a viable and popular approach in the rational design of peptidomimetics. Peptidomimetics find applications as drugs, in protein engineering and so on Read More

The decision of stressed cells to die or to survive is made by integrating signals at different levels through multiple check points. However, initiation and continued progression toward cell death by apoptosis in cancer cells may be blocked by mutation of the tumor suppressor p53 or overexpression of members of the bcl-2 family of proteins. The existence of such mechanisms indicates that cancer cells lose the contr Read More