Abstract:
:Anticancer drugs are often nonselective antiproliferative agents (cytotoxins) that preferentially kill dividing cells by attacking their DNA at some level. The lack of selectivity results in significant toxicity to noncancerous proliferating cells. These toxicities along with drug resistance exhibited by the solid tumors are major therapy limiting factors that result into poor prognosis for patients. Prodrug and conjugate design involves the synthesis of inactive drug derivatives that are converted to an active form inside the body and preferably at the site of action. Classical prodrug and conjugate design have focused on the development of prodrugs that can overcome physicochemical (e.g., solubility, chemical instability) or biopharmaceutical problems (e.g., bioavailability, toxicity) associated with common anticancer drugs. The recent targeted prodrug and conjugate design, on the other hand, hinge on the selective delivery of anticancer agents to tumor tissues thereby avoiding their cytotoxic effects on noncancerous cells. Targeting strategies have attempted to take advantage of low extracellular pH, elevated enzymes in tumor tissues, the hypoxic environment inside the tumor core, and tumor-specific antigens expressed on tumor cell surfaces. The present review highlights recent trends in prodrug and conjugate rationale and design for cancer treatment. The various approaches that are currently being explored are critically analyzed and a comparative account of the advantages and disadvantages associated with each approach is presented.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Singh Y,Palombo M,Sinko PJdoi
10.2174/092986708785132997subject
Has Abstractpub_date
2008-01-01 00:00:00pages
1802-26issue
18eissn
0929-8673issn
1875-533Xjournal_volume
15pub_type
杂志文章,评审abstract::Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708784638861
更新日期:2008-01-01 00:00:00
abstract::Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infection has been a global challenge. The complicated forms of the Coronavirus Disease 2019 (COVID-19) can evolve to multiple-organ failure, including several coagulopathies related to a sudden worsening of respiratory status. This article aimed to review s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666201005112231
更新日期:2020-10-05 00:00:00
abstract::Preterm labour is a major cause of perinatal mortality and morbidity. However, during the past 40 years of clinical studies and despite the use of multiple therapeutic agents, the rate of preterm birth has not drastically declined. In 1991, it was estimated that in the US approximately 116,000 women admitted with acut...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033457331
更新日期:2003-08-01 00:00:00
abstract::In situ hybridization (ISH) is a type of hybridization that uses a labeled complementary DNA or RNA strand to localize a specific DNA or RNA sequence on a chromosome or section of tissue (in-situ) fixed on a slide. Flourescence in-situ hybridization (FISH) technique facilitates the localization of genes to different c...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801661031
更新日期:2012-01-01 00:00:00
abstract::Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170529101810
更新日期:2019-01-01 00:00:00
abstract::The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA synthetases (AaRS). Aminoacyl-tRNA synthetases are the...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801323199
更新日期:2012-01-01 00:00:00
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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::Ageing is an aggravating factor leading to alterations in the biotransformation of drugs, and therefore their therapeutic efficacy and safety. In this review we discuss the influence of ageing on drug metabolizing enzymes in male Wistar rats. We report that drug metabolizing enzymes can be affected by ageing either by...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707780090981
更新日期:2007-01-01 00:00:00
abstract::The bi-aryl urea multi-kinase inhibitor Sorafenib (BAY 43-9006, Nexavar) was initially approved for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Eleven years after its first description in PubMed, the therapeutic potential of Sorafenib has been evaluated in an increasing nu...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712803341548
更新日期:2012-01-01 00:00:00
abstract::The clinical treatment of multifactorial pathologies (e.g. cancer, Alzheimer's disease, psychiatric disorders), is still a major challenge. Many researches have been published dealing with the design of multiple ligands, able to act at the same time towards several targets relevant for a given pathology. In the presen...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801215883
更新日期:2012-01-01 00:00:00
abstract::Nature as a source of inspiration has been shown to have a great beneficial impact on the development of new computational methodologies. In this scenario, analyses of the interactions between a protein target and a ligand can be simulated by biologically inspired algorithms (BIAs). These algorithms mimic biological s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711795029573
更新日期:2011-01-01 00:00:00
abstract::The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170911162331
更新日期:2018-01-01 00:00:00
abstract::Whether the increased atrial fibrillation (AF) risk in metabolic syndrome (MetS) patients is due to the syndrome as a whole or simply the sum of the risks of its individual component parts is still obscure. These two clinical entities share many pathophysiological links and thus distinction between a casual observatio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666171012105528
更新日期:2019-01-01 00:00:00
abstract::Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform asso...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801661112
更新日期:2012-01-01 00:00:00
abstract::Plant foods are not only a main source of nutrients, but they are also rich in physiologically bioactive bionutrients or phytochemicals. Consumption of fruit and vegetables is associated with a decreased risk of pathological status, including cancer. Reactive oxygen species play a key role in the genesis and developme...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711795656036
更新日期:2011-01-01 00:00:00
abstract:BACKGROUND:The therapeutic properties of cannabinoids are well-known since ancient years. Growing evidence exist on endocannabinoid system (ECS) modulation related with human tumorigenesis. OBJECTIVE:Taking into account the substantial role of ECS on immune cell regulation, the present review is aimed to summarize the...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160530144934
更新日期:2016-01-01 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::β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710793361261
更新日期:2010-01-01 00:00:00
abstract::Alzheimer's disease (AD) is a complex and progressive neurodegenerative disorder. The available therapy is limited to the symptomatic treatment and its efficacy remains unsatisfactory. In view of the prevalence and expected increase in the incidence of AD, the development of an effective therapy is crucial for public ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666141106122628
更新日期:2015-01-01 00:00:00
abstract::Over the past few years, use of the genome-wide association study (GWAS) has made it possible to identify the primary genetic mechanisms of essential hypertension. GWAS results have helped identify many loci in or near genes that generally were not expected to be associated with blood pressure or essential hypertensio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666141216124537
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:In the last two decades, there have been significant technological advances in the early detection of brain tumors. However, no notable improvements have been observed in the treatment of Glioblastoma Multiforme (GBM), the most common brain neoplasm coupled with the worst prognosis. GBM is characterized by a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170303122241
更新日期:2017-01-01 00:00:00
abstract::Giving a glance to the report of Wound Care Market by Product updated in 2017, we can see that wound care market is expected to reach USD 22.01 billion by 2022 from USD 18.35 billion at a CAGR of 3.7%. Numerous factors are driving the growth of this market, including the increasing prevalence of chronic wounds and acu...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180713150626
更新日期:2019-01-01 00:00:00
abstract::Some DNA or RNA sequences rich in guanine (G) nucleotides can adopt noncanonical conformations known as G-quadruplexes (G4). In the nuclear genome, G4 motifs have been associated with genome instability and gene expression defects, but they are increasingly recognized to be regulatory structures. Recent studies have r...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180228165527
更新日期:2019-01-01 00:00:00
abstract::A dramatical decline in human male reproductive function has been reported for the past 20 years. Many recent epidemiological, clinical and experimental findings suggest that the reproductive dysfunction could result from prenatal and neonatal chemical compound exposure. Even if numerous studies argue for a relationsh...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711797636117
更新日期:2011-01-01 00:00:00
abstract:: ...
journal_title:Current medicinal chemistry
pub_type: 社论
doi:10.2174/092986732533181024105316
更新日期:2018-01-01 00:00:00
abstract::Sweat is an alternative biological matrix useful to detect drugs of abuse intake. It is produced by eccrine and apocrine glands originating in the skin dermis and terminating in secretory canals that flow into the skin surface and hair follicles. Since many years it has been demonstrated that endogenous and exogenous ...
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:BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00
abstract::Bipolar disorder (BD) is a long-term illness with mood swings which are characterized by recurrent episodes of mania/hypomania and depression, with variable interpolations of relatively asymptomatic periods, called euthymic, in which, however, some psychopathological symptoms may persist. Although mood stabilizers, su...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709787909604
更新日期:2009-01-01 00:00:00
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journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2001-07-01 00:00:00
abstract::Over the last decade there has been significant progress in understanding the molecular basis of disease processes. At the same time the technological advances in the area of genomics and the efforts in proteomics research have increased the possibility of discovering many proteins with defined therapeutic functions. ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708785132924
更新日期:2008-01-01 00:00:00