Mini Reviews in Medicinal Chemistry - Volume 8, Issue 6, 2008

The tetracyclic indolo[3,2-b]quinoline ring system constitutes an important structural moiety in natural products exhibiting numerous biological activities. In particular, indolo [3, 2-b]quinoline, commonly known as linear quindoline is of particular interest, because of its rigid structure and scope of derivatization. Although the core linear quindoline skeleton shows little or no activity in several biological systems, introduction Read More

The plasma membrane redox (PMR) system is important for cell metabolism and survival; it is also crucial for blood coagulation and thrombosis. This review will give an update on the PMR system, with a particular regard to platelets, and on the role of antioxidant vitamins belonging to this system.

Tamoxifen, a selective estrogen receptor modulator (SERM), has been used for many decades as the “gold standard” adjuvant treatment for patients with hormone-receptor-positive early breast cancer. This drug, when administered for 5 years, reduces the risk for recurrence, contralateral breast cancer (BC) and death. The optimal duration of tamoxifen in the adjuvant setting has not been established yet, but i Read More

Saponins are plant glycosides with favorable anti-tumorigenic properties. Several saponins inhibit tumor cell growth by cell cycle arrest and apoptosis with IC50 values of up to 0.2 μM. We discuss diverse groups of saponins (dioscins, saikosaponins, julibrosides, soy saponins, ginseng saponins and avicins) investigated in relation to tumor therapy and focus on cellular and systemic mechanisms of tumor cell growth inhi Read More

An intermolecular disulfide bond serves as a thioredoxin-dependent redox-sensing switch for the regulation of the enzymatic activity of 3-mercaptopyruvate sulfurtransferase (MST, EC.2.8.1.2). A cysteine residue on the surface of each subunit was oxidized to form an intersubunit disulfide bond so as to decrease MST activity, and thioredoxin-specific conversion of a dimer to a monomer increased MST activity. Furth Read More

Toll-like receptor 9 has been the focus of considerable research attention for the ability to modulate its activity, and subsequent innate immune responses, through DNA-based immunotherapeutics. Nucleic acids are attractive as therapeutics for their low cost, chemical stability and ease of production. While the ability for TLR9 to be differentially regulated by nucleic acids of varying sequences and structures offers flexibility f Read More

The mode of action of retinoids in relation to their activity in the adult central nervous system and the potential of synthetic retinoid analogues is reviewed. Investigation into the activity of such molecules will further our understanding of the retinoid pathway during nervous system development and in various neurological disease states.

Rho GTPases, which control processes such as cell proliferation and cytoskeleton remodeling, are often hyperexpressed in tumors. Several members, such as RhoA/B/C, must be isoprenylated to interact with their effectors. Statins, by inhibiting the synthesis of prenyl groups, may affect RhoA/B/C activity and represent a promising tool in anticancer therapy.

Endothelial Lipase (EL) is a newly identified member of the triacylglycerol lipase family. Recent studies suggested that EL may be an important determinant of HDL-metabolism and inflammation acting at the level of the vessel wall. The aim of this review is to summarize important facts derived from experimental approaches and from epidemiologic human studies to provide a comprehensive view on the role of EL in infl Read More

The Src family of non-transmembrane protein kinases is comprised of eleven homologous members in mammals. Together, these kinases regulate a wide variety of cellular processes including cell survival, proliferation, differentiation, and motility. One member of this family, Lck, plays a pivotal role in T-cell signaling. Inhibition of Lck with small molecules has significant potential for therapeutic immunosuppression and treatment Read More