Abstract:
:Thromboembolic diseases such as deep vein thrombosis (DVT), pulmonary embolism (PE), myocardial infarction (MI) and ischemic strokes are mainly responsible for people's morbidity and mortality and have severely affected the people's quality of life all over the world. According to WHO statistics, an average of 17 million people are killed by the thromboembolic diseases each year globally. Therefore, the prevention and treatment of thromboembolic diseases have received widespread attention in recent years. Based on thrombotic mechanism, anti-thrombotic drugs are mainly divided into anticoagulants, antiplatelet agents and direct thrombolytic drugs. In particular, anticoagulants such as vitamin K antagonists (VKAs), unfractionated heparin (UFH), and low-molecular-weight heparins (LMWHs) have become the main therapies for pre-treatment of thromboembolic disorders. However, the limitations of traditional anticoagulants such as slow onset of action, dose-adjusted requirement, drug-drug and drug-food interactions have restricted their improvement in the clinical treatment. The mechanism of the thromboembolic disorders has indicated that coagulation factor Xa (fXa) plays a pivotal role in the blood coagulation cascade. Thus, selective inhibition of fXa by diminishing the amplified generation of thrombin without affecting the pre-existing thrombin levels can provide better antithrombotic effect, thereby causing less impairment of primary hemostasis. In this paper, we mainly introduce the recent advances of fXa inhibitors, with focus on their biological activity and structure-activity relationship (SAR) information. In particular, the inspirations from the structures of the fXa inhibitors and their future direction are highlighted.
journal_name
Curr Drug Targetsjournal_title
Current drug targetsauthors
Guo L,Ma Sdoi
10.2174/1389450116666150518095533subject
Has Abstractpub_date
2015-01-01 00:00:00pages
1207-32issue
11eissn
1389-4501issn
1873-5592pii
CDT-EPUB-67385journal_volume
16pub_type
杂志文章,评审abstract::Osteoporosis causes bone loss, and makes bone to susceptible to fracture. The main cause of osteoporosis is estrogen deficiency. Estrogen, calcitonin, calcium, vitamin D and antioxidants can be used to prevent osteoporosis. For the treatment of osteoporosis, the potential biological activities of traditional medicines...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/13894501113149990205
更新日期:2013-12-01 00:00:00
abstract::Pancreatic ductal adenocarcinoma (referred here as pancreatic cancer) is a lethal disease with the worst prognosis among all solid tumors. Surgical resection represents the only hope for cure but it is possible only in patients that present with local disease (about 20% of cases). Whether dismal prognosis of pancreati...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945012800564103
更新日期:2012-06-01 00:00:00
abstract::Infiltrating inflammatory cells into the kidney mediate the initiation and progression of damage by direct cytotoxicity, the secretion of soluble factors such as cytokines and proteases, or by the subsequent induction of further immune response. Before leukocytes can exert their effects on renal damage or repair, they...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945006775270213
更新日期:2006-01-01 00:00:00
abstract::Enzymes are proteins that act as biological catalysts to speed up cellular biochemical processes. According to their main Enzyme Commission (EC) numbers, enzymes are divided into six categories: EC-1: oxidoreductase; EC-2: transferase; EC-3: hydrolase; EC-4: lyase; EC-5: isomerase and EC-6: synthetase. Different enzym...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450119666181002143355
更新日期:2019-01-01 00:00:00
abstract::It has been well recognized that inflammatory responses are part of pathogenesis for various disorders such as autoimmune diseases. For example, multiple sclerosis (MS) is an inflammatory demyelinating disease of central nervous system that is presumably caused by activated T cells specific for myelin antigens. Rheuma...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010790980321
更新日期:2010-04-01 00:00:00
abstract::The understanding of the neurobiological processes leading to major depressive disorder (MDD) is an active field of research in the scientific community. For years, the alteration of monoamine neurotransmission, in particular serotonin (5-HT), has been considered the most significant pathophysiological mechanism of th...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/13894501113149990154
更新日期:2013-05-01 00:00:00
abstract::Recently, a significant number of breast cancer (BC) patients have been diagnosed at an early stage. It is therefore critical to accurately predict the risk of recurrence and distant metastasis for better management of BC in this setting. Clinicopathologic patterns, particularly lymph node status, tumor size, and horm...
journal_title:Current drug targets
pub_type: 杂志文章
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更新日期:2020-01-01 00:00:00
abstract:AIMS:The aim of this study is to provide an overview of several emerging anti-diabetic molecules. BACKGROUND:Diabetes is a complex metabolic disorder involving the dysregulation of glucose homeostasis at various levels. Insulin, which is produced by β-pancreatic cells, is a chief regulator of glucose metabolism, regul...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450120666191031104653
更新日期:2020-01-01 00:00:00
abstract::Hepatitis C virus (HCV), a member of the Flaviviridae family, has been recognised to be responsible for both parenterally transmitted and sporadic non-A and non-B hepatitis affecting 1-3% of the world population. HCV is a positive stranded RNA virus encoding a single polyprotein which contains at least ten unique stru...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450023347650
更新日期:2002-08-01 00:00:00
abstract::Thrombomodulin (TM) is a type 1 membrane bound glycoprotein that has a C-type lectin domain at its Nterminus, 6 copies of the epidermal growth factor-like (EGF) motif and serine/threonine rich domain carrying a glycosoaminoglycan external to the membrane. TM binds thrombin changing thrombin's substrate specificity fro...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945012799424606
更新日期:2012-03-01 00:00:00
abstract::Post-translational modification represents an important mechanism to regulate protein function in cardiac cells. Ubiquitin (Ub) and ubiquitin-like proteins (UBLs) are a family of protein modifiers that share a certain extent of sequence and structure similarity. Conjugation of Ub or UBLs to target proteins is dynamica...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666151209114608
更新日期:2018-01-01 00:00:00
abstract::The aim of the present article is to review the indications, the monitoring and the complications of sedation in the post-anaesthesia care unit (PACU). In this setting, sedation is often an unwanted side effect of anaesthetic drugs that delay discharge, however it could be specifically indicated. Such indications incl...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945005774574542
更新日期:2005-11-01 00:00:00
abstract::The HIV-1 transactivator Tat protein plays a key role in AIDS pathogenesis. Besides the Tat role as activator of HIV-1 transcription, it exerts several important functions on infected and uninfected cells. In fact, HIV-1 Tat is released by infected cells and is taken up by neighboring cells. In this way it regulates e...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150825110658
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Global death rate due to cardiovascular diseases (CVDs) is highest as compared to other ailments. Principal risk factor associated with CVDs is hypertension. Major classes of current antihypertensive (AHT) therapies include angiotensin converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARBs)...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666160711163119
更新日期:2017-01-01 00:00:00
abstract::The production of reactive oxygen species is a normal part of cell physiology, but many internal and external stimuli are able to trigger the production of excess levels of oxidants that are potentially damaging. The threat of oxidative damage is particularly significant to DNA, as damaged bases can interfere with rep...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150126111055
更新日期:2016-01-01 00:00:00
abstract::Terpenoids represent a large and diverse class of naturally occurring compounds found in a variety of fruits, vegetables and medicinal plants. Structurally some of the terpenoids are similar to human hormones. A diet rich in terpenoids is inversely related with the risk of chronic diseases including cancers. Breast an...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010791170842
更新日期:2010-06-01 00:00:00
abstract::Colorectal cancer (CRC) is one of the most common cancers worldwide. In developed countries, its mortality remains high, yet the prevalence has established owing to effective screening programs; however due to the westernization of lifestyle, the incidences in many other countries have increased. Although the treatmen...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450120666191112141901
更新日期:2020-01-01 00:00:00
abstract::Aldose reductase (AR) enzymatically transforms cytosolic glucose into sorbitol, a molecule that poorly penetrates cell membranes and is sometimes slowly metabolized. Hyperglycemia can cause intracellular accumulation of sorbitol and its metabolite, fructose, which can create osmotic swelling and cell dysfunction. Driv...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008783431781
更新日期:2008-01-01 00:00:00
abstract::The contribution of proteases to developmental, physiological and pathological processes has been well accepted. Cleavage of matrix proteins is a key requirement for cell migration and remodeling of the extracellular environment. The constant process of matrix turnover is dependent on the delicate balance between degr...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008785909365
更新日期:2008-10-01 00:00:00
abstract::Alzheimer's, a degenerative cause of the brain cells, is called as a progressive neurodegenerative disease and appears to have a heterogeneous etiology with main emphasis on amyloid-cascade and hyperphosphorylated tau-cascade hypotheses, that are directly linked with macromolecules called enzymes such as β- & γ-secret...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450119666180820104723
更新日期:2019-01-01 00:00:00
abstract::Atherosclerosis is associated with the increased trans-sialidase activity, which can be detected in the blood plasma of atherosclerosis patients. The likely involvement in the disease pathogenesis made this activity an interesting research subject and the enzyme that may perform such activity was isolated and characte...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450120666190308111619
更新日期:2019-01-01 00:00:00
abstract::The incidence and mortality of malignant tumors are on the rise, which has become the second leading cause of death in the world. At present, anti-tumor drugs are one of the most common methods for treating cancer. In recent years, with the in-depth study of tumor biology and related disciplines, it has been gradually...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450120666190402145325
更新日期:2019-01-01 00:00:00
abstract::Rituximab has demonstrated a major effect in B-cell lymphoma and in a wide range of autoimmune disorders. Unfortunately, the blood-brain-barrier excludes the disorders restricted to the central nervous system (CNS) from the action of rituximab. The progressive phase of multiple sclerosis (MS) is a prototypical CNS aut...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666141029234644
更新日期:2014-01-01 00:00:00
abstract::Treatment of chronic myeloid leukemia (CML) with interferon-alpha (IFN-α) was introduced in the early 1980s. Several clinical trials showed a survival advantage for patients treated with IFN-α compared to conventional chemotherapy. Some patients achieved longstanding complete cytogenetic remissions (i.e. >2 log tumor ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011794815301
更新日期:2011-03-01 00:00:00
abstract::Oxysterols are pleiotropic messengers interacting with multiple receptor systems. One of the cognate receptors for oxysterols is EBI2, a G protein-coupled receptor highly expressed in the cells of the immune system. Here we discuss the receptor's role in the adapted immunity and inflammation as well as the receptor's ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666160217123042
更新日期:2016-01-01 00:00:00
abstract::The Wnt signaling pathway has important functions in development, tissue homeostasis, and regeneration. Deregulation of canonical Wnt/beta-catenin signaling is frequently found in various human cancers, particularly in colorectal cancer, and non-canonical Wnt signaling pathways also have been implicated in neoplasia. ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008784911769
更新日期:2008-07-01 00:00:00
abstract:BACKGROUND:Nanotechnology deals with the manufacturing of materials at the atomic and molecular scale. According to the National Nanotechnology Initiative, nanotechnology denotes those structures which are nearly in 1-100 nm size regime in at least one dimension. OBJECTIVE:Nanotechnology in drug delivery has been evid...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450119666180131105822
更新日期:2018-01-01 00:00:00
abstract::The growing number of cellular and molecular pathways believed to be involved in mechanisms of ischemic cell death in the brain has spurred a similar growth in the number of potential neuroprotective modalities, the majority of which are pharmacological in nature. Preventing or minimizing the first few steps in the ca...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450043345209
更新日期:2004-10-01 00:00:00
abstract::The use of predictive biomarkers provides potential individualized cancer therapeutic options to prevent therapy failure as well as serious toxicities. Several recent studies showed that predictive and prognostic biomarkers are a notable personalized strategy to improve patients' care in several cancers. Trabectedin (...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200128161733
更新日期:2020-01-01 00:00:00
abstract::Excessive production of reactive oxygen species is an important mechanism underlying the pathogenesis of diabetes associated macrovascular and microvascular complications including diabetic nephropathy. Diabetic nephropathy is characterized by glomerular enlargement, early albuminuria and progressive glomerulosclerosi...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140321120635
更新日期:2014-05-01 00:00:00