Abstract:
:Mitochondria are organelles which play an important role not only in cellular metabolism but also in controlling pathways related with cell death, ionic and redox regulation. Alterations in mitochondrial metabolism are implicated in a variety of diseases, including cancer. Cellular and mitochondrial metabolism are both altered during the different stages of tumor development. As cancer cells have altered metabolic profiles, these alterations are a valid and promising target for anti-cancer agents. We hereby review several molecules that are in different stages of development and which target mitochondria in cancer cells. However, not all compounds are efficiently delivered into mitochondria, especially due to the difficulty of these agents to cross the membranes that surround the organelle, contributing to a loss of effectiveness and specificity. This led to the development of effective strategies aimed at delivering useful cargo to mitochondria, including the use of delocalized lipophilic cations coupled to useful molecules, or peptides that insert in mitochondrial membranes. Although several of those targeting strategies have still a very limited use against cancer cells, we present here the advantages and disadvantages of each combination.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Deus CM,Santos GL,Loureiro R,Vega-Naredo I,Faneca H,Oliveira PJdoi
10.2174/0929867322666150209155957subject
Has Abstractpub_date
2015-01-01 00:00:00pages
2438-57issue
20eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-65098journal_volume
22pub_type
杂志文章,评审abstract::With many advantages over other therapeutic agents such as monoclonal antibodies, aptamers have recently emerged as a novel and powerful class of ligands with excellent potential for diagnostic and therapeutic applications. Typically generated through Systematic Evolution of Ligands by EXponential enrichment (SELEX), ...
journal_title:Current medicinal chemistry
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doi:10.2174/092986711797189673
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abstract::Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...
journal_title:Current medicinal chemistry
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abstract:BACKGROUND:Lipids are essential components of cells that participate in metabolic and endocrine regulation and reproductive functions. The main organs where lipid regulation takes place are the liver and adipose tissue. Besides, when each tissue specific action cannot be exerted, it could lead to several endocrine-meta...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867328666210106142912
更新日期:2021-01-06 00:00:00
abstract::The cellular response to DNA damage is critical for determining whether carcinogenesis, cell death or other deleterious biological effects will ensue. Numerous cellular enzymatic mechanisms can directly repair damaged DNA, or allow tolerance of DNA lesions, and thus reduce potential harmful effects. These processes in...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708783497328
更新日期:2008-01-01 00:00:00
abstract::Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180320120054
更新日期:2019-01-01 00:00:00
abstract::Breakdown of glucose under physiological conditions gives rise to glucose degradation products (GDPs). GDPs are also formed during heat sterilization of glucose-containing peritoneal dialysis fluids (PD-fluids). In PD-fluids GDPs have been shown in many different in vitro assays to be responsible for adverse effects s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706778201576
更新日期:2006-01-01 00:00:00
abstract::Osteoporosis is a pathological loss of bone mass due to an imbalance in bone remodeling where osteoclast-mediated bone resorption exceeds osteoblast-mediated bone formation resulting in skeletal fragility and fractures. Anti-resorptive agents such as bisphosphonates and SERMs, and anabolic drugs that stimulate bone fo...
journal_title:Current medicinal chemistry
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abstract::The transport of organic and inorganic molecules, along with inorganic ions across the plasma membrane results in chemical fluxes that reflect the cellular function in healthy and diseased states. Measurement of these chemical fluxes enables the characterization of protein function and transporter stoichiometry, chara...
journal_title:Current medicinal chemistry
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更新日期:2019-05-06 00:00:00
abstract::Schizophrenia is a chronic psychiatric disorder that affects about 1 in 100 people around the world and results in persistent emotional and cognitive impairments. Untreated schizophrenia leads to deterioration in quality of life and premature death. Although the clinical efficacy of dopamine D2 receptor antagonists ag...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867326666190710172002
更新日期:2019-01-01 00:00:00
abstract::The use of antisense oligonucleotides as therapeutic agents has generated considerable enthusiasm in the research and medical community. Antisense oligonucleotides as therapeutic agents were proposed as far back as in the 1970s when the antisense strategy was initially developed. Nonetheless, it has taken almost a qua...
journal_title:Current medicinal chemistry
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更新日期:2005-01-01 00:00:00
abstract:BACKGROUND:Pollutants are diverse chemical entities, including gases such as ozone and particulate matter PM. PM contains toxic chemicals such as polycyclic aromatic hydrocarbons (PAHs). Some PAHs can induce strong oxidative stress under UVA exposure. Pollution aggravates some skin diseases such as atopy or eczema, but...
journal_title:Current medicinal chemistry
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更新日期:2018-01-01 00:00:00
abstract::In the human brain several cell types are capable of initiating and amplifying a brain specific inflammatory response involving the synthesis of cytokines, prostaglandins and oxygen free radicals. In Alzheimer's disease (AD), signs of an inflammatory activation of microglia and astroglia are present inside and outside...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867023371292
更新日期:2002-01-01 00:00:00
abstract::Demyelination occurs in several central nervous system (CNS) disorders, including multiple sclerosis, viral infection and spinal cord injury and can result in severe functional impairment. Therefore there is great interest in developing therapies promoting repair in CNS demyelinating diseases and trauma. Cell replacem...
journal_title:Current medicinal chemistry
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doi:10.2174/092986708783330593
更新日期:2008-01-01 00:00:00
abstract::Two-component signal transduction systems and their expanded variants known as phosphorelays are integral elements of the virulence and antimicrobial resistance responses of a wide range of pathogenic bacteria and fungi and also regulate essential functions. As a consequence, two-component systems and phosphorelays ar...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867043455765
更新日期:2004-03-01 00:00:00
abstract::Staphylococcus aureus is a notorious pathogenic bacterium causing a wide range of diseases from soft-tissue contamination, to more serious and deep-seated infections. This species is highlighted by its ability to express several kinds of virulence factors and to acquire genes related to drug resistance. Target this nu...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867325666180327105842
更新日期:2018-01-01 00:00:00
abstract::Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867023369853
更新日期:2002-07-01 00:00:00
abstract:BACKGROUND:Nitric oxide (NO) plays important regulatory roles in a plethora of biological functions and thus holds tremendous potential to be exploited for clinical uses. However, the chemistries in the molecular design of nano-nitric oxide delivery systems is currently lacking. OBJECTIVE:The overarching aim of this r...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170407141222
更新日期:2018-01-01 00:00:00
abstract::Cellular resistance to anthracyclines is a major limitation of their clinical use in the treatment of human tumors. Resistance to doxorubicin is described as a multifactorial phenomenon involving the overexpression of defense factors and alterations in drug-target interactions. Such changes do not account for all mani...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867013373994
更新日期:2001-01-01 00:00:00
abstract::Over the years, natural products have shown success as antidiabetics in in vitro, in vivo studies and clinical trials. Because natural product-derived drugs are more affordable and effective with fewer side-effects compared to conventional therapies, pharmaceutical research is increasingly leaning towards the discover...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867323666160813222436
更新日期:2018-01-01 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
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更新日期:2010-01-01 00:00:00
abstract::gamma-Amino butyric acid is an extremely important inhibitory neurotransmitter in the mammalian central nervous system and is essential for the overall balance between neuronal excitation and inhibition. It is well documented that GABA deficiency is associated with several important neurological disorders such as Hunt...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710791698549
更新日期:2010-01-01 00:00:00
abstract::The vascular system distributes oxygen and nutrients to all tissues in the body. Additionally, the vascular system also functions in hosting and instructing tissue-specific stem and progenitor cells. Both cell- or blood-derived signals from the vascular system regulate stem cell properties in health and disease. Studi...
journal_title:Current medicinal chemistry
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更新日期:2014-01-01 00:00:00
abstract::Mammalian ecto ADP-ribosyltransferases (ARTs) constitute a family of structurally related proteins expressed on the cell surface or secreted in the extracellular compartment. Using NAD+ as substrate, they transfer ADP-ribose groups onto target proteins. In contrast to intracellular poly(ADP-ribosyl)transferases (PARPs...
journal_title:Current medicinal chemistry
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更新日期:2004-04-01 00:00:00
abstract::Cellular signaling is regulated by several biochemical reactions, whose dynamics depends on changes in the fluxes of specific ligands through the containment barriers that are the biological membranes. The regulation of this complex dynamic equilibrium is mainly due to the activity of border proteins, that must be abl...
journal_title:Current medicinal chemistry
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更新日期:2010-01-01 00:00:00
abstract::Endothelial cells (ECs) play a pivotal role in physiological and altered tissue neovascularization. They face multiple morphological, biochemical and functional changes during the different phases of angiogenesis, under the regulation of a great number of proangiogenic and antiangiogenic signals, including soluble and...
journal_title:Current medicinal chemistry
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更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Since the serendipitous discovery of the antitumor activity of cisplatin there has been a continuous surge in studies aimed at the development of new cytotoxic metal complexes. While the majority of these complexes have been designed to interact with nuclear DNA, other targets for anticancer metallodrugs att...
journal_title:Current medicinal chemistry
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更新日期:2019-01-01 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
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更新日期:2015-01-01 00:00:00
abstract::Poisoning of DNA topoisomerase I is the mechanism by which camptothecins interfere with tumor growth. Although the clinical use of camptothecins has had a significant impact on cancer therapy, de novo or acquired clinical resistance to these drugs is common. Clinical resistance to camptothecins is still a poorly under...
journal_title:Current medicinal chemistry
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更新日期:2013-01-01 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
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更新日期:2020-10-01 00:00:00
abstract::Nitric oxide (NO) is a diatomic free radical produced from L-arginine by constitutive and inducible nitric oxide synthase (cNOS and iNOS) in numerous mammalian cells and tissues. Nitric oxide (NO), superoxide (O2-) and their reaction product peroxynitrite (ONOO-) may be generated in excess during the host response aga...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711795029690
更新日期:2011-01-01 00:00:00