Medicinal Chemistry - Volume 7, Issue 5, 2011

Molecular medicine is the future of 21st century patient management. Molecular imaging can play pivotal roles in disease diagnosis, treatment efficacy assessment, drug discovery, and the understanding of fundamental biology. Positron emission tomography (PET) has been used in the clinic for decades and 18F-FDG has become indispensible in many facets of patient management, such as cancer staging and treatment moni Read More

The labeling of probes with fluorine-18 [18F, β(+); 96.7%] continues to play a considerably important role in the development of positron emission tomography (PET) as a modality for both clinical research and clinical diagnoses. This review summarizes the strategies and recent developments in the fluorine-18 labeling of probes for PET imaging. Problems and issues relating to the practical production of fluorine-18 currently in Read More

Positron Emission Tomography (PET) field and, in particular utilization of 68Ga radiometal is getting momentum. The development of new imaging agents for targeted, pre-targeted, non-targeted imaging and their clinical applications is accelerating worldwide. The pharmacopoeia monographs regarding generator produced 68Ga radionuclide and 68Ga-labeled somatostatin (SST) analogues are in progress. The number of com Read More

Development of targeted radionuclide therapy with 90Y labeled antibodies and peptides has gained momentum in the past decade due to the successes of 90Y-ibritumomab tiuxetan and 90Y-DOTA-Phe1-Tyr3-octreotide in treatment of cancer. 90Y is a pure β--emitter and cannot be imaged for patient-specific dosimetry which is essential for pre-therapeutic treatment planning and accurate absorbed dose estimation in individ Read More

The positron emitting isotope 89Zr is an ideal radionuclide for use in positron emission tomography (PET) imaging with monoclonal antibodies (mAbs). This article reviews the cyclotron physics of 89Zr production, and the chemical separation methods for isolating it from yttrium target material. 89Zr coordination with the bifunctional chelate desferrioxamine B is discussed, along with the common procedures for attachi Read More

Positron emission tomography (PET) is a powerful molecular imaging technology with the ability to image and monitor molecular events in vivo and in real time. With the increased application of PET radiopharmaceuticals for imaging physiological and pathological processes in vivo, there is a demand for versatile positron emitters with longer physical and biological half-lives. Traditional PET radionuclides, such as carbon-11 (11 Read More

The increasing use of positron emission tomography in preclinical and clinical settings has widened the demand for radiopharmaceuticals with high specificity that can image biological phenomena in vivo. While many PET tracers have been developed from small organic molecules labeled with carbon-11 or fluorine-18, the short half-lives of these radionuclides preclude their incorporation into radiotracers, which can be used to i Read More

Cancer is a diverse disease with decisive pathobiology involving complex mechanisms. Recent advancements through research continue to focus on identifying vital targets and discovering multi-model therapies. It is essential to understand the disease processes and exploring the possible therapeutic strategies to save the lives of patients; however, the key factor remains the early diagnosis of the disease. In cancer therap Read More

Non-steroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) specific inhibitors are antiinflammatory agents that have also shown to be useful in anticancer therapy. The effects of chebulagic acid (CA), a benzopyran tannin from Terminalia chebula having COX-2/5-LOX dual inhibitory properties, on the sensitivity of doxorubicin (Dox) in human hepatocellular carcinoma cell line HepG2 were studied in the prese Read More

Breast cancer is the most common cancer in women living in the Western world, even though it occurs worldwide. Cancer and cancer therapy induce multiple oral complications including dental and periodontal disease. Saliva is a complex and dynamic biologic fluid, which reflects both oral and systemic changes. While saliva is an easily accessible body fluid, there has been little effort to study its value in cancer diagnosis. Si Read More

Cancer cells exhibit many defects in cell communication that contribute to the loss of tissue homeostasis (excess cell proliferation, invasion, and metastasis). The process of cancer formation causes a disruption in cell homeostasis, affecting the ability to respond to extracellular signals, as well as triggering some intracellular events which alter gap junctional intercellular communication (GJIC). Previous research has shown that t Read More

Pharmacological inhibition of Hsp90 in tumor cells induces anticancer effects through the destabilization of several oncogenic signaling molecules. Although there were reports that Hsp90 inhibition compromises cellular integrity, how this affects the cell adhesion through extracellular matrix (ECM) and integrin signaling is not known. Using human neuroblastoma (IMR-32), cervical (HeLa) and breast (MCF-7) cancer cells, and m Read More

Src kinase mutations and/or overexpression have been implicated in the development of a number of human cancers including colon, breast, and lung cancers. Thus, designing potent and selective Src kinase inhibitors as anticancer agents is a subject of major interest. A series of 4-aryl substituted derivatives of 2-amino-7-dimethylamino-4H-chromene- 3-carbonitrile were synthesized using one-pot reaction of appropriat Read More

Aberrant methylation of tumor suppressor genes (TSG) is an important epigenetic event in cancer, including multiple myeloma (MM). Interleukin-6 (IL-6), which plays a significant role in the pathogenesis of MM, also regulates DNA methylation. However, attempts to bring IL-6 blockade to the clinic have had limited success. We hypothesize that IL-6 regulation of hypermethylation may be an important pathway leading to ration Read More

Tea is a popular, socially accepted, drink that is enjoyed by millions of people. A growing body of evidence suggests that moderate consumption of tea may protect against several forms of cancer. It is also known that bioactivation of precarcinogens and detoxification of ultimate carcinogens are carried out mainly by drug metabolizing enzymes such as cytochrome P450 (CYP). The present study investigates the effect of tea c Read More

Nano Drug Delivery, as a treatment method against brain tumors, is a progressing area in the field of precise targeted drug administration methodology. The unresolved problems related to chemotherapy, other invasive therapeutic procedures and various obstructions offered by biological barriers are circumvented by nanodrug delivery. Recent dramatic developments in nanotechnology have created a lot of nano Read More

Cancer represents a major cause of overall mortality, second to cardiovascular disorders. Cancer patients frequently encounter hypercoagulable states, with recurrent thromboembolic events due to the impact of cancer cells and chemotherapy/radiotherapy on the coagulation cascade. The expression of highly procoagulant proteins have been implicated to involve in tumor cell-induced thrombin generation, leading to platele Read More

Transcription factors are proteins that regulate gene expression by binding to specific DNA sequences within gene promoter regions. Specificity protein (Sp) family transcription factors play a critical role in various cellular processes and have been shown to be associated with tumorigenesis. The Sp family consists of several members that contain a highly conserved DNA-binding domain composed of three zinc fingers at the C Read More