Search results for "cancer therapy"
showing 10 items of 101 documents
Small molecule DNA-PK inhibitors as potential cancer therapy: a patent review (2010–present)
2021
Introduction: DNA-dependent protein kinase (DNA-PK) plays a crucial role in the repair of DSBs via non-homologous end joining (NHEJ). Several DNA-PK inhibitors are being investigated for potential anticancer treatment in clinical trials.Area covered: This review aims to give an overview of patents published since 2010 by analyzing the patent space and structure features of scaffolds used in those patents. It also discusses the recent clinical developments and provides perspectives on future challenges and directions in this field.Expert opinion: As a key component of the DNA damage response (DDR) pathway, DNA-PK appears to be a viable drug target for anticancer therapy. The clinical investi…
Principal component analysis on molecular descriptors as an alternative point of view in the search of new Hsp90 inhibitors
2009
Inhibiting a protein that regulates multiple signal transduction pathways in cancer cells is an attractive goal for cancer therapy. Heat shock protein 90 (Hsp90) is one of the most promising molecular targets for such an approach. In fact, Hsp90 is a ubiquitous molecular chaperone protein that is involved in folding, activating and assembling of many key mediators of signal transduction, cellular growth, differentiation, stress-response and apoptothic pathways. With the aim to analyze which molecular descriptors have the higher importance in the binding interactions of these classes, we first performed molecular docking experiments on the 187 Hsp90 inhibitors included in the BindingDB, a pu…
Hypoxia: Importance in tumor biology, noninvasive measurement by imaging, and value of its measurement in the management of cancer therapy
2006
The Cancer Imaging Program of the National Cancer Institute convened a workshop to assess the current status of hypoxia imaging, to assess what is known about the biology of hypoxia as it relates to cancer and cancer therapy, and to define clinical scenarios in which in vivo hypoxia imaging could prove valuable.Hypoxia, or low oxygenation, has emerged as an important factor in tumor biology and response to cancer treatment. It has been correlated with angiogenesis, tumor aggressiveness, local recurrence, and metastasis, and it appears to be a prognostic factor for several cancers, including those of the cervix, head and neck, prostate, pancreas, and brain. The relationship between tumor oxy…
Gefitinib in lung cancer therapy. Clinical results, predictive markers of response and future perspectives.
2009
Over the past few years, epidermal growth factor receptor has emerged as one of the most important targets in tumorgenesis and several drugs targeting signal transduction pathways have been developed. The first among these agents to be approved for the treatment of NSCLC was gefitinib, a potent, selective and reversible inhibitor of HER1/EGFR tyrosine kinase activity. The review summarizes its clinical development and the new therapeutic options, with particular focus on predictive markers of susceptibility to this drug.
Identification of chemosensitizers by drug repurposing to enhance the efficacy of cancer therapy
2020
Abstract The progressively rising drug resistance has driven the development of chemosensitizers, which aim to enhance the current chemotherapeutic efficacy through either quantitatively increasing intracellular drug concentration by inhibiting drug efflux, vesicle sequestration, and metabolic inactivation or qualitatively exerting concomitant effects on cellular regulation to promote apoptosis. Given the high failure rates and costs during standard drug development, drug repurposing represents an effective and economic approach for chemosensitizer identification. By applying drug repurposing, a wide range of existing clinic drugs including anticardiovascular agents, immunosuppressants, ant…
Relevance of Multidrug Resistance Proteins on the Clinical Efficacy of Cancer Therapy
2005
Variations in drug uptake and efflux, as well as changes in intracellular drug entrapment and distribution may represent important resistance mechanisms to cancer therapy. A variety of ATP binding cassette transporters (ABC) localised in multiple cell membranes is implied in those phenomena, representing a mechanism of protection of cells against xenobiotics. Many cancer cell lines over express some ABC transporters, especially p-glycoprotein, MRP1 and BCRP. This over expression is related to worse cancer treatment outcome and, in some cases, reduced overall survival of cancer patients. This paper reviews the location and physiological role of the three transporters mentioned and also descr…
Management of chemotherapy extravasation: ESMO–EONS Clinical Practice Guidelines
2012
Extravasation is the process by which any liquid (fluid or drug) accidentally leaks into the surrounding tissue. In terms of cancer therapy, extravasation refers to the inadvertent infiltration of chemotherapy into the subcutaneous or subdermal tissues surrounding the intravenous or intra-arterial administration site. Extravasated drugs are classified according to their potential for causing damage as ‘vesicant’, ‘irritant’ and ‘nonvesicant’ (Table 1). Some vesicant drugs are further classified into two groups: DNA binding and non-DNA binding. Allwood et al. (2002) divided the drugs into vesicants, exfoliants, irritants, inflammitants and neutrals.
Targeting epigenetics in cancer: therapeutic potential of flavonoids
2021
Irrespective of sex and age, cancer is the leading cause of mortality around the globe. Therapeutic incompliance, unwanted effects, and economic burdens imparted by cancer treatments, are primary health challenges. The heritable features in gene expression that are propagated through cell division and contribute to cellular identity without a change in DNA sequence are considered epigenetic characteristics and agents that could interfere with these features and are regarded as potential therapeutic targets. The genetic modification accounts for the recurrence and uncontrolled changes in the physiology of cancer cells. This review focuses on plant-derived flavonoids as a therapeutic tool for…
Highly Homogeneous Biotinylated Carbon Nanodots: Red-Emitting Nanoheaters as Theranostic Agents toward Precision Cancer Medicine
2019
Very recent red-emissive carbon nanodots (CDs) have shown potential as near-infrared converting tools to produce local heat useful in cancer theranostics. Besides, CDs seem very appealing for clinical applications combining hyperthermia, imaging, and drug delivery in a single platform capable of selectively targeting cancer cells. However, CDs still suffer from dramatic dot-to-dot variability issues such that a rational design of their structural, optical, and chemical characteristics for medical applications has been impossible so far. Herein, we report for the first time a simple and highly controllable layer-by-layer synthesis of biotin-decorated CDs with monodisperse size distribution, …
NUTRITION AND CANCER
1969
The last decades have seen the identification of a number of drugs targeting oncogene pathways, therefore contributing to moving the cancer therapy field toward precision medicine. However, existing and acquired resistance to targeted therapies represent major obstacles against their long-term effectiveness. In fact, the initial efficacy of targeted therapies is often limited to a portion of the patient population and is frequently followed by the acquisition of drug-resistant disease.