Abstract:
:Over the last three decades, neoplasms have become the largest cause of human mortality due to both high tumor incidence and mortality. Chemotherapy is one of the main therapies employed to treat neoplasms. Although classical genotoxic drugs, such as cyclophosphamide, 5-FU, cisplatin and doxorubicin have been applied in clinical settings and have achieved very good treatment efficacy, many cancer patients died of tumor metastasis, drug toxicity or drug resistance due to tumor heterogeneity. Targeted molecular treatments based on the genes, receptors, and kinases expressed by a tumor make individualized treatment possible. Protein kinases catalyze the phosphorylation of proteins and are involved in multiple cellular processes. In many cancers, mutation or abnormal expression of protein kinases is correlated with tumorigenesis, metastasis and resistance to chemotherapy. Tumor-related protein kinases have become important molecular targets and biomarkers. The use of protein kinases as tumor biomarkers primarily focuses on tyrosine and serine/threonine kinases. Many tumor drugs targeting protein kinases, such as monoclonal antibody and tyrosine kinase inhibitors (TKIs), are widely utilized in clinic. Additional drugs aimed at combating drug resistance and metastasis should be developed targeting protein kinases. In this review, we summarize several important protein kinases involved in cancer and analyze why these kinases can be used as biomarkers or targets for cancer diagnosis and/or treatment. Furthermore, numerous drugs targeting protein kinases as well as their development and activity are discussed.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Quan C,Xiao J,Liu L,Duan Q,Yuan P,Zhu Fdoi
10.2174/1381612823666170720113216subject
Has Abstractpub_date
2017-11-16 00:00:00pages
4209-4225issue
29eissn
1381-6128issn
1873-4286pii
CPD-EPUB-84888journal_volume
23pub_type
杂志文章,评审abstract::Cumulative scientific evidence gathered over the past ten years has confirmed the role of platelet GP IIb/IIIa inhibitors in reducing ischemic complications of patients undergoing percutaneous coronary intervention (PCI). Recently, mortality data available on more than 20,000 patients enrolled in randomized clinical t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043453306
更新日期:2004-01-01 00:00:00
abstract::Senescence is defined as an irreversible growth arrest that is characterised by a changed morphology, gene expression pattern and chromatin structure as well as an activated DNA damage response. Senescence has a dual role for tumour development-it acts as a tumour suppressor to prevent the proliferation of seriously d...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210789941874
更新日期:2010-01-01 00:00:00
abstract::Marine plants, animals and microorganisms display steady growth in the ocean and are abundant carbohydrate resources. Specifically, natural polysaccharides obtained from brown algae have been drawing increasing attention owing to their great potential in pharmaceutical applications. This review describes the structura...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190618143952
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Vaginal infections caused by non-albicans species have become common in women of all age groups. The resistance of species such as Candida parapsilosis to the various antifungal agents is a risk factor attributed to these types of infections, which instigates the search for new sources of active compounds in...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200317131041
更新日期:2020-01-01 00:00:00
abstract::Fusion proteins have been well-studied and widely applied in biopharmaceutics. Albumin fusion proteins are simple to construct, easy to purify, and stable to formulate. One main application of fusion protein is to extend the plasma half-life of therapeutic proteins and peptides. Albiglutide for diabetes treatment is t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150302120047
更新日期:2015-01-01 00:00:00
abstract::The liver acts as a host to many functions hence raising the possibility that any one may be compromised by a single gene defect. Inherited or de novo mutations in these genes may result in relatively mild diseases or be so devastating that death within the first weeks or months of life is inevitable. Some diseases ca...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211797247541
更新日期:2011-01-01 00:00:00
abstract::Serotonin (5-HT) is one of the main transmitters in the nervous system. Serotonergic neurons in the raphe nuclei in the brainstem innervate most parts of the central nervous system including motoneurons in the spinal cord and brainstem. This review will focus on the modulatory role that 5-HT exerts on motoneurons and ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990341
更新日期:2013-01-01 00:00:00
abstract::The receptor for urokinase plasminogen activator (uPAR) is required in hematopoietic stem/progenitor cells (HSC, HPC) mobilization in the mouse. Indeed, uPAR Ko mice are deficient both in retention and mobilization of HSC and HPC, because uPAR causes their retention in the BM through its interaction with the α4β1 inte...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161211796718206
更新日期:2011-01-01 00:00:00
abstract:BACKGROUND:Human brain is amongst the most complex organs in human body, and delivery of therapeutic agents across the brain is a tedious task. Existence of blood brain barrier (BBB) protects the brain from invasion of undesirable substances; therefore it hinders the transport of various drugs used for the treatment of...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200417141600
更新日期:2020-01-01 00:00:00
abstract::The apoptosis inducing factor (AIF) was first discovered as a caspase-independent apoptosis effector that promoted cell death upon release from the mitochondria (triggered by pro-apoptotic stimuli) and relocalization into the nucleus, where it promotes chromatin condensation and DNA fragmentation. AIF is a mammalian m...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319140012
更新日期:2013-01-01 00:00:00
abstract::The drug discovery process in general is a very resource intensive undertaking that has existed for a very long time. In the last two decades, performing molecular simulations that determine the level of interaction between a protein and ligand have been refined to the point where they are now an essential part of the...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160414142530
更新日期:2016-01-01 00:00:00
abstract::We estimated the frequency of detection of different human papillomavirus (HPV) types in women with atypical squamous cells of undetermined significance (ASCUS) or low-grade squamous intraepithelial lesion (LSIL) cytology in a population-based primary screening programme. 247 liquid-based cytology (LBC) samples with A...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:
更新日期:2013-01-01 00:00:00
abstract::Medicinal inorganic chemistry plays an important role in exploring the properties of metal ions for the designing of new drugs. The field has been stimulated by the success of cis-platin, the world best selling anticancer drug and platinum complexes with reduced toxicity, oral activity and activity against resistant t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160906143249
更新日期:2016-01-01 00:00:00
abstract::Aneuploidy is a pathological condition that affects 35% of human spontaneous abortions and 0.3% of livebirths. In spite of the increasing knowledge about molecular mechanisms of meiosis and chromosome segregation, maternal age remains the only ascertained aetiological factor. Genetically modified mouse models have bee...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206776389859
更新日期:2006-01-01 00:00:00
abstract::Gene delivery, a process of introducing foreign functional nucleic acids into target cells, has proven to be a very promising tool for inducing specific gene expression in host cells. Many different technologies have been developed for efficient gene delivery. Among them, electroporation has been adopted in gene deliv...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666151027152121
更新日期:2015-01-01 00:00:00
abstract::G protein receptor kinase 2 (GRK2) has been for years mainly considered the negative regulator of the cardiac β adrenergic signaling. However GRK2 is a ubiquitous molecule and its kinase activity and scaffold properties brought to several investigations which have evidenced its involvement in pathophysiology of extra-...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161212799040493
更新日期:2012-01-01 00:00:00
abstract::Stability of a dosage form is its ability to preserve its quality attributes within preset limits. The time span over which these attributes remain within specifications is the shelf-life of the drug product. Stability is a very complex feature and is influenced not only by the stability of the drug substance but also...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160726094236
更新日期:2016-01-01 00:00:00
abstract::Cystic fibrosis is caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene that lead to abnormalities in transepithelial ion transport in the airways of affected patients. Lung disease is the major contributor to morbidity and mortality in patients with cystic fibrosis but recommende...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212799315984
更新日期:2012-01-01 00:00:00
abstract::Macrophages are professional scavengers of apoptotic and necrotic cells, and hence constantly take up self antigens. Paradoxically, macrophages are also professional antigen-presenting cells, which would seem to invite autoimmune disorders. Moreover, macrophages are effector cells in the tissue-destruction phase of au...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033392026
更新日期:2003-01-01 00:00:00
abstract:BACKGROUND:Primary aldosteronism is the most common causes of secondary hypertension. Patients suffering from this clinical syndrome have an increased cardiovascular risk and target organ damage. Mineralocorticoid receptor antagonists are the optimal pharmaceutical option for the management of such patients. OBJECTIVE...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190311130138
更新日期:2018-01-01 00:00:00
abstract::Emerging evidence has shown that microRNAs (miRNAs) can act as oncogenes in the initiation and progression of leukemia and lymphoma. Aberrant expression of oncogenic miRNAs, including miR-155, miR-17-92, miR-21, miR-125b, miR-93, miR-143-p3, miR-196b, and miR-223 promotes leukemogenesis through increasing the leukemic...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140128211724
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:Tissue engineering (TE) is a promising solution for orthopaedic diseases such as bone or cartilage defects and bone metastasis. Cell culture in vitro and scaffold fabrication are two main parts of TE, but these two methods both have their own limitations. The static cell culture medium is unable to achieve m...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190301142833
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Medical treatments are used either alone or in combination with assisted reproductive techniques for treatment of infertile patients with hypergonadotropic hypogonadism. A wide range of treatment options such as gonadotropins, aromatase inhibitors (AIs), selective estrogen receptor modulators (SERMs) and the...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666201102110456
更新日期:2020-11-01 00:00:00
abstract:: ...
journal_title:Current pharmaceutical design
pub_type: 社论
doi:10.2174/1381612825999190515120510
更新日期:2019-01-01 00:00:00
abstract::Gestational diabetes mellitus is a common metabolic complication of pregnancy. Universal guidelines on gestational diabetes have been impeded by the long-term controversies on its definition and screening strategies. The prevalence of gestational diabetes is rising all over the world, is significantly influenced by et...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666201106092423
更新日期:2020-01-01 00:00:00
abstract::Stem cell therapy heralds a new chapter in cardiovascular regenerative medicine. Cardiovascular implants are often used in both surgery and interventional cardiology. Cardiovascular stents are utilized in percutaneous coronary interventions (PCI), and are classified as either bare metal stents (BMS) or drug-eluting st...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210794455058
更新日期:2010-01-01 00:00:00
abstract::Since identifying a transmissible agent responsible for tumorigenesis in chickens, the v-Src oncogene, significant progress has been made in determining the functions of its cellular homologue. c-Src is the product of the SRC gene and has been found both over-expressed and highly activated in a number of human cancers...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612053507576
更新日期:2005-01-01 00:00:00
abstract::Recent progresses in the development of fluorescent technologies become a reliable device for drug discovery research. The fluorescence tools offer attractive options for an opportunity to visualize the effects of drug candidates in the cells. The fluorescent tools, such as fluorescent protein, are regularly used in a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789207006
更新日期:2009-01-01 00:00:00
abstract::Low density lipoproteins (LDL) and high density lipoproteins (HDL) are independent risk factors for coronary heart disease (CHD); decreasing LDL-cholesterol (LDL-C) levels with statin therapy represents the primary goal in the management of cardiovascular disease. However, despite the efficacy of statins in reducing c...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990298
更新日期:2013-01-01 00:00:00
abstract::Nucleoside reverse transcriptase inhibitors (NRTIs) are components of most current antiretroviral (ARV) regimens. Side effects arising from mitochondrial toxicity (MtT) induced by these drugs is a common reason why patients treated with NRTI change or discontinue therapy. These toxicities can be difficult to reverse, ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210793563482
更新日期:2010-10-01 00:00:00