Human deoxyribonucleic acid topoisomerases: molecular targets of anticancer drugs.
نویسنده
چکیده
Mammalian cells contain two distinct types of topoisomerases. They have been mechanistically classified into a type I (topo I) and type II (topo II) enzyme. Anticancer drugs which target topo I include camptothecin, irinotecan, topotecan, and 9-aminocamptothecin. Anticancer drugs which target topo II include etoposide, mitoxantrone, teniposide, and doxorubicin. Much experimental work has indicated that cells with high topoisomerase are drug sensitive, and cells with low topoisomerase are drug resistant. These data suggest that patients whose tumors have abundant topoisomerase might be predicted to respond to topo targeted anticancer drugs. In order to test this hypothesis, immunohistochemical stains have been developed which can recognize the topoisomerases in formalin-fixed, paraffin-embedded, human tissue sections. This may make it feasible to correlate topoisomerase expression in human cancers with clinical response to chemotherapy.
منابع مشابه
Molecular dynamics simulation and docking studies on the binding properties of several anticancer drugs to human serum albumin
Disposition and transportation of anticancer drugs by human serum albumin (HSA) affects their bioavailability, distribution and elimination. In this study, the interaction of a set of anticancer drugs with HSA was investigated by molecular dynamics and molecular docking simulations. The drugs' activities were analyzed according to their docking scores, binding sites and structural descriptors. ...
متن کاملStudy of Human Albumin Protein Interaction with Fluorouracil Anticancer Drug Using Molecular Docking Method
Introduction: Drugs are mainly delivered to the target tissues by plasma proteins, such as human serum albumin, in the human body. Practical information about the thermodynamic parameters of drugs and their stability can be obtained using simulation methods, such as molecular docking. Material & Methods: This study, investigated the molecular docking of human serum albumin with fluorouracil an...
متن کاملNatural Compounds as Anticancer Agents Targeting DNA Topoisomerases
DNA topoisomerases are important cellular enzymes found in almost all types of living cells (eukaryotic and prokaryotic). These enzymes are essential for various DNA metabolic processes e.g. replication, transcription, recombination, chromosomal decatenation etc. These enzymes are important molecular drug targets and inhibitors of these enzymes are widely used as effective anticancer and antiba...
متن کاملA high-throughput fluorescence anisotropy-based assay for human topoisomerase II β-catalyzed ATP-dependent supercoiled DNA relaxation.
Because of their essentiality for DNA replication, transcription, and repair, type II topoisomerases are targets for antibacterial and anticancer drugs. There are two type II topoisomerases in humans, topoisomerase IIα (TOP2A) and topoisomerase IIβ (TOP2B), and two in bacteria, gyrase and topoisomerase IV. Inhibition of one or both of the human type II topoisomerases by antibacterial compounds ...
متن کاملInhibitors of topoisomerases as anticancer drugs: problems and prospects.
DNA topoisomerases, which solve topological problems associated with various DNA transactions, are the targets of many therapeutic agents. Various topoisomerase inhibitors especially, topo-poisons, camptothecin (topo-I) and etoposide (topo-II) are some of the drugs that are used in the current treatment protocols, particularly for the treatment of leukemia (AML, ALL etc). However, tumor resista...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Annals of clinical and laboratory science
دوره 27 6 شماره
صفحات -
تاریخ انتشار 1997