Abstract:
:Endogenous opioid peptides have been studied extensively as potential therapeutics for the treatment of pain. The major problems of using natural opioid peptides as drug candidates are their poor receptor specificity, metabolic instability and inability to reach the brain after systemic administration. A lot of synthetic efforts have been made to opioid analogs with improved pharmacological properties. One important structural modification leading to such analogs is cyclization of linear sequences. Intramolecular cyclization has been shown to improve biological properties of various bioactive peptides. Cyclization reduces conformational freedom responsible for the simultaneous activation of two or more receptors, increases metabolic stability and lipophilicity which may result in a longer half-life and easier penetration across biological membranes. This review deals with various strategies that have been employed to synthesize cyclic analogs of opioid peptides. Discussed are such bridging bonds as amide and amine linkages, sulfur-containing bonds, including monosulfide, disulfide and dithioether bridges, bismethylene bonds, monosulfide bridges of lanthionine and, finally, carbonyl and guanidine linkages. Opioid affinities and activities of cyclic analogs are given and compared with linear opioid peptides. Analgesic activities of analogs evaluated in the in vivo pain tests are also discussed.
journal_name
Curr Drug Targetsjournal_title
Current drug targetsauthors
Piekielna J,Perlikowska R,Gach K,Janecka Adoi
10.2174/1389450111314070008subject
Has Abstractpub_date
2013-06-01 00:00:00pages
798-816issue
7eissn
1389-4501issn
1873-5592pii
CDT-EPUB-20130425-4journal_volume
14pub_type
杂志文章,评审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::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
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journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666141029234644
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abstract:BACKGROUND:Osteoporosis is a debilitating disease characterized by bone micro-architecture degradation contributing to fragility fractures. Currently, determining bone mineral density (BMD) via dual-energy X-ray absorptiometry (DXA) is the most reliable form of diagnosing osteoporosis and managing pharmacological treat...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450118666170704143529
更新日期:2018-01-01 00:00:00
abstract::Epigenetic modifications ensure the maintenance of normal cellular functions, and their dysregulation is frequently found in many disease states, including cancer. Nowadays, the most studied epigenetic dysregulation associated with tumorigenesis, cancer progression and metastasis refers to the variations in DNA methyl...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200325093104
更新日期:2020-01-01 00:00:00
abstract::Medicinal plants and mushrooms have alwaysfascinated the world as an attractive source of natural compounds for cancer therapy. From ancient times, they have been valued as gourmet food and folk medicine in Oriental practice. For over 40 years, world has witnessed the overwhelming interest of western scientific frater...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121999201230204526
更新日期:2020-12-30 00:00:00
abstract::Various strategies for the use of zein for controlled drug release have been investigated and reported in the literature, especially engineering strategies for using zein conjugates to enhance oral bioavailability and targeted delivery, which has attracted interest in recent research. Although still limited, the abili...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450120666190913124629
更新日期:2020-01-01 00:00:00
abstract::As early as 1940, Abraham and Chain described "an enzyme able to destroy penicillin". In the late 1940's, penicillin-resistant strains of Staphylococcus aureus were found to be a clinical problem. They produced a penicillinase that could hydrolyze the amide bond in the β-lactam ring. Later, an enzyme mediated by an R-...
journal_title:Current drug targets
pub_type: 历史文章,杂志文章,评审
doi:10.2174/1389450116666151001112859
更新日期:2016-01-01 00:00:00
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journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945007782403838
更新日期:2007-11-01 00:00:00
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journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008786949379
更新日期:2008-12-01 00:00:00
abstract:BACKGROUND:The incidence of inflammatory bowel disease (IBD) continues to rise worldwide and despite the advances on pharmacotherapy, the etiopathogenesis of Crohn's disease (CD) and ulcerative colitis (UC) remains underexplained. In this context, the migratory waves of the last decades created a challenging setting to...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666201119142045
更新日期:2020-11-19 00:00:00
abstract::The down regulation of gene expression is a promising strategy for molecular medicine and experimental biology. Molecules that bind to the DNA double helix may interfere with gene expression and, in addition to potential therapeutic applications, can be helpful for the investigation of DNA processing, chromatin packag...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450043345100
更新日期:2004-11-01 00:00:00
abstract::The present article aims to review the literature on the relationship between psychology and inflammatory bowel disease (IBD). In particular, the first section is dedicated to explore the role of psychological factors in the etiopathology of the disease, its development and the efficacy of treatments, while the second...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140627151702
更新日期:2014-01-01 00:00:00
abstract::Efforts to interfere with the initiation and promotion of breast and other cancers by endocrine manipulation are not new. It is of obvious benefit to cancer patients to administer substances that combine minimal general toxicity with maximal oestrogen inhibition. Raloxifene is a relatively recent addition to a group o...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450013348263
更新日期:2001-12-01 00:00:00
abstract::Disorders of emotion regulation such as anxiety disorders and depression are common and yet debilitating. Accumulating evidence suggests involvement of serotonin (5-HT) in the regulation of emotion. Mice with targeted deletion of genes encoding mediators of the serotonergic transmission have proven to be a powerful to...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450111314050005
更新日期:2013-05-01 00:00:00
abstract::Neutrophil-dominated inflammation plays an important role in many airway diseases including asthma, chronic obstructive pulmonary disease (COPD), bronchiolitis and cystic fibrosis. In cases of asthma where neutrophil-dominated inflammation is a major contributing factor to the disease, treatment with corticosteroids c...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011794751555
更新日期:2011-04-01 00:00:00
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journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011798109509
更新日期:2011-10-01 00:00:00
abstract::Breast cancer remains the leading cause of cancer death among females worldwide. It signifies a shift from the previous decade during which the most common cause of cancer death was cervical cancer. Current treatment modalities, including surgery, radiotherapy, and adjuvant chemotherapy or hormone therapy, have not be...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945012804545632
更新日期:2012-12-01 00:00:00
abstract::The recent marketing of two selective cyclooxygenase-2 (COX-2) inhibitors, celecoxib and rofecoxib is remarkable considering that COX-2 was only discovered eight years ago as a growth factor- and cytokine-inducible gene. Concomitant with these pharmaceutical successes is the advances in our understanding of the molecu...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450013348830
更新日期:2001-03-01 00:00:00
abstract::Acute myeloid leukemia (AML) was the first malignancy for which immunotherapy, in the form of allogeneic hematopoietic stem cell transplantation (allo-HSCT), was integrated into the standard of care. Allo-HSCT however is an imperfect therapy associated with significant morbidity and mortality while offering only incom...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150223120005
更新日期:2017-01-01 00:00:00
abstract::HIV-1 replicates by infecting new target cells either as cell-free viral particle or, much more efficiently, via cell-to-cell viral transmission. Cell-mediated viral spread, in which the infected cell directly transfers the viral particles to target cells via cell-cell contacts, in vitro is up to three orders of magni...
journal_title:Current drug targets
pub_type: 杂志文章
doi:
更新日期:2015-08-25 00:00:00
abstract::Pain is a complex multidimensional concept that facilitates the initiation of the signaling cascade in response to any noxious stimuli. Action potential generation in the peripheral nociceptor terminal and its transmission through various types of nociceptors corresponding to mechanical, chemical or thermal stimuli le...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450120666190131114244
更新日期:2019-01-01 00:00:00
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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::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::Dysbiosis has been repeatedly observed in inflammatory bowel disease (IBD) and is now recognized as an essential factor in the gut inflammatory process. IBD is a significant burden to health-care systems, mainly due to treatment-related costs. Available treatments have several limitations: up to 30% of patients are pr...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200602125507
更新日期:2020-01-01 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::Inflammation is the most common pathology in many orthopedic diseases, such as: rheumatoid arthritis (RA), osteoarthritis (OA) and other reasons caused osteolysis. The leading factor of inflammation was considered as the differentiation of monocyte and the polarization of macrophage. However, cytokines and different c...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450120666191015211737
更新日期:2020-01-01 00:00:00
abstract::Long term treatment with antiepileptic drugs (AEDs) is the standard therapeutic approach to eradicate seizures. However, a small but significant number of patients fail AED treatment. Intrinsic drug resistance may depend on two main and not necessarily mutually exclusive mechanisms: 1) Loss of pharmacological target (...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450033491109
更新日期:2003-05-01 00:00:00
abstract:BACKGROUND:Galanin (GAL) constitutes a family of neuropeptides composed of four peptides: (i) galanin (GAL), (ii) galanin-message associated peptide (GAMP), (iii) galanin-like peptide (GALP), and (iv) alarin. GAL contains 29/30 amino acids, and its biological action occurs through the interactions with its various rece...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200225112055
更新日期:2020-01-01 00:00:00
abstract::Resveratrol (3,4',5 tri-hydroxystilbene) is a phytoalexin produced in hudge amount in grapevine skin in response to infection by Bothrytis cinerea. This production of resveratrol blocks the proliferation of the pathogen, thereby acting as a natural antibiotic. Numerous studies have reported interesting properties of t...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945006776359331
更新日期:2006-04-01 00:00:00