Abstract:
:Currently, the long-term usage of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in HIVAIDS patients eventually leads to the development of drug resistance and severe side effect. Therefore, it is imperative to look for the novel NNRTIs with potent and broad spectrum anti-mutant activity that are also safe and have excellent pharmacokinetic profiles. In this article, newly emerging NNRTIs scaffolds in recent three years, together with the underlying strategies for developing new generation HIV-1 NNRTIs with improved resilience to current drug resistant mutants, are reviewed and analysed.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Zhan P,Liu X,Li Zdoi
10.2174/092986709788803231subject
Has Abstractpub_date
2009-01-01 00:00:00pages
2876-89issue
22eissn
0929-8673issn
1875-533Xjournal_volume
16pub_type
杂志文章,评审abstract::Dipeptidyl peptidase 4 (DPP-4), a substrate-specific serine protease, has been validated as a promising drug target for the treatment of type 2 diabetes. DPP-4 inhibitors significantly lowered blood glucose levels in patients with type 2 diabetes without common body weight gain, hypoglycemia and gastrointestinal distu...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712802002491
更新日期:2012-01-01 00:00:00
abstract::Farnesylthiosalisylic acid (FTS) is a potent non-toxic anticancer drug that targets oncogenic and pathologically activated Ras. The mechanism of action of FTS is well understood. It interferes with the binding of activated Ras proteins to their escort chaperons and with Ras tethering to the plasma membrane. This agent...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311320100002
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abstract::Recent advances in endoscopic techniques such as capsule endoscopy have revealed that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) often cause mucosal lesions not only in the upper gastrointestinal tract, but also in the small intestine in humans. Gastric and duodenal lesions caused by NSAIDs can be ...
journal_title:Current medicinal chemistry
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doi:10.2174/092986712803413980
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Numerous studies have demonstrated that halogenated agents elicit myocardial conditioning effects when adminis-tered perioperatively in cardiac surgery. Recent evidence has been published of the benefits of maintaining exposure to halogenated agents during the early postoperative period. The enzymatic mechan...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327999201001202607
更新日期:2020-10-01 00:00:00
abstract::Cellular interactions among platelets, leukocytes and endothelial cells are considered as a major cause of inflammation and atherosclerosis in many diseases. Via exposed surface receptors and released soluble substances, activated platelets play a crucial role in the initiation of inflammatory processes, resulting in ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712798918770
更新日期:2012-01-01 00:00:00
abstract::In recent years there has been a growing interest in computer-based screening. One of the driving forces has been the increased efficiency of protein crystallography leading to the real possibility of using structure-based design as a significant contributor to the discovery of novel ligands. In 1957 after 22 years of...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033457809
更新日期:2003-05-01 00:00:00
abstract::Raltegravir, the only drug targeting the integration step in HIV-1 life cycle, makes β-ketoenol integrase (IN) strand transfer inhibitor (STI) gain a definitive place in the treatment of HIV-1 infection. However, the emergence of viral strains resistant to β-ketoenol STI demands a continued effort toward the discovery...
journal_title:Current medicinal chemistry
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更新日期:2012-01-01 00:00:00
abstract::A comprehensive outline for understanding and recommending the therapeutic use of ozone in combination with established therapy in diseases characterized by a chronic oxidative stress is currently available. The view of the absolute ozone toxicity is incorrect, because it has been based either on lung or on studies pe...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666151221150420
更新日期:2016-01-01 00:00:00
abstract::Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
abstract::This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researc...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666190808122929
更新日期:2020-01-01 00:00:00
abstract::More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:
更新日期:1999-03-01 00:00:00
abstract::This review focuses on the development of nanoparticle systems for antimicrobial drug delivery. Numerous antimicrobial drugs have been prescribed to kill or inhibit the growth of microbes such as bacteria, fungi and viruses. Even though the therapeutic efficacy of these drugs has been well established, inefficient del...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710790416290
更新日期:2010-01-01 00:00:00
abstract::Advanced enteropancreatic (EP) neuroendocrine tumors (NETs) can be treated with several different therapies, including chemotherapy, biotherapy, and locoregional treatments. Over the last few decades, impressive progress has been made in the biotherapy field. Three main druggable molecular targets have been studied an...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/09298673113209990237
更新日期:2014-01-01 00:00:00
abstract::The development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. Millions of dollars and man-hours are devoted to the discovery of new therapeutical agents. As, the activity of a drug is the result of a multitude of factors such as bi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867003375317
更新日期:2000-02-01 00:00:00
abstract::Paclitaxel has been proven to be effective against different types of cancer. A delivery system loaded with paclitaxel at tumor site should provide a high local concentration of the drug detrimental to malignant cells, which prevents the re-growth and metastasis of tumor. In this review, paclitaxel formulations for sy...
journal_title:Current medicinal chemistry
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更新日期:2004-02-01 00:00:00
abstract::The discovery of cannabinoid receptors at the beginning of the 1990s, CB1 cloned in 1990 and CB2 cloned in 1993, and the availability of selective and potent cannabimimetics could only be justified by the existence of endogenous ligands that are capable of binding to them. Thus, the characterisation and cloning of the...
journal_title:Current medicinal chemistry
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更新日期:2019-01-01 00:00:00
abstract::Nicotinamide adenine dinucleotide (NAD), generally considered a key component involved in redox reactions, has been found to participate in an increasingly diverse range of cellular processes, including signal transduction, DNA repair, and post-translational protein modifications. In recent years, medicinal chemists h...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708783885282
更新日期:2008-01-01 00:00:00
abstract::Vitamin D has been known for a long time as a major factor involved in the calcium- phosphate balance and homeostasis, along with parathyroid hormone (PTH). While vitamin D effects on calcium and phosphate are fully known, recent studies attempted to link vitamin D status and cardiovascular diseases. The involvement o...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160405112019
更新日期:2016-01-01 00:00:00
abstract::COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867327999200917150939
更新日期:2020-09-17 00:00:00
abstract::Cardiotrophin-1 (CT-1), a member of the interleukin (IL)-6 family, is reported to exhibit a plethora of pleiotropic effects in the heart such as cytoprotective, pro-proliferative and pro-fibrotic ones. An extensive research has been devoted on proliferative and profibrotic effects of CT-1 on the heart. Thus the presen...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2013-01-01 00:00:00
abstract:: ...
journal_title:Current medicinal chemistry
pub_type: 社论
doi:10.2174/092986732618190821115641
更新日期:2019-01-01 00:00:00
abstract::Poly(aminoester) dendrimers are expected to hold great promise as biodegradable nanocarriers for drug delivery due to their advantageous properties allowing their biodegradability, potentially lower toxicity and possibility of diverse chemical conjugations. The synthetic strategies for constructing such dendrimers inc...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311209025011
更新日期:2012-01-01 00:00:00
abstract::Nowadays, the use of synthetic carriers as biochemical reagents and immunogens is entering a new phase. The multimeric nature of these constructs, the unambiguous composition and the ease, reliability and versatility of their production, make this type of carriers well-suited to various biotechnological and biochemica...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867054039062
更新日期:2005-01-01 00:00:00
abstract::Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2011-01-01 00:00:00
abstract::Inflammation plays a critical role in the atherosclerotic process in various vascular beds, starting from endothelial dysfunction and counting all stages of plaque development. The significant contribution of inflammation in the initiation and progression of atherosclerosis has been documented over many years but its ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867322666150630141035
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:The incidence of pancreatic cancer (PC) is rising in parallel with the deaths caused by this malignant disease largely due to limited improvement in current treatment strategies. In spite of aggressive PC research, for the past three decades, there has been no significant improvement in the five-year surviva...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170209104453
更新日期:2018-01-01 00:00:00
abstract::Onychomycosis (fungal nail infections) is very common worldwide but is fortunately not often lethal. Several powerful drugs have been introduced into clinical practice in recent years, but these infections remain difficult to cure primarily due to the difficulty of penetration of drug to the site of the infection in t...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160411130103
更新日期:2016-05-27 00:00:00
abstract:BACKGROUND:The sterile alpha motif (Sam) domain is a small helical protein module, able to undergo homo- and hetero-oligomerization, as well as polymerization, thus forming different types of protein architectures. A few Sam domains are involved in pathological processes and consequently, they represent valuable target...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666181009114445
更新日期:2020-01-01 00:00:00
abstract::HupA is a potent, reversible AChEI, which crosses the blood-brain barrier smoothly, and shows high specificity for AChE with a prolonged biological half-life. It has been approved as the drug for the treatment of AD in China, and marketed in USA as a dietary supplement. HupA has been the subject of investigations by a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033456747
更新日期:2003-11-01 00:00:00
abstract::Cervical spondylotic myelopathy (CSM) is a very common and debilitating disease; however, its underlying pathocellular process remains uncertain. Attempts have been made to reproduce CSM in experimental animal models in order to deepen the knowledge on the molecular pathobiology of this disease. The up-to-date observa...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2010-01-01 00:00:00