Cyclization in opioid peptides.

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 Targets

journal_title

Current drug targets

authors

Piekielna J,Perlikowska R,Gach K,Janecka A

doi

10.2174/1389450111314070008

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

798-816

issue

7

eissn

1389-4501

issn

1873-5592

pii

CDT-EPUB-20130425-4

journal_volume

14

pub_type

杂志文章,评审
  • Trans-sialidase Associated with Atherosclerosis: Defining the Identity of a Key Enzyme Involved in the Pathology.

    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

    authors: Glanz VY,Myasoedova VA,Grechko AV,Orekhov AN

    更新日期:2019-01-01 00:00:00

  • Osteopontin; as a target molecule for the treatment of inflammatory diseases.

    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

    authors: Morimoto J,Kon S,Matsui Y,Uede T

    更新日期:2010-04-01 00:00:00

  • Intrathecal rituximab therapy in multiple sclerosis: review of evidence supporting the need for future trials.

    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

    authors: Bonnan M,Ferrari S,Bertandeau E,Demasles S,Krim E,Miquel M,Barroso B

    更新日期:2014-01-01 00:00:00

  • Urinary Bone Turnover Markers as Target Indicators for Monitoring Bisphosphonate Drug Treatment in the Management of Osteoporosis.

    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

    authors: Kwon S,Wang AH,Sadowski CA,Yuksel N,Doschak MR

    更新日期:2018-01-01 00:00:00

  • Epigenetic Therapies and Potential Drugs for Treating Human Cancer.

    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

    authors: Lin SQ,Li X

    更新日期:2020-01-01 00:00:00

  • Natural Products as Anticancer Agents.

    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

    authors: Varghese R,Dalvi YB

    更新日期:2020-12-30 00:00:00

  • Design of Zein Conjugation and Surface Modification for Targeting Drug Delivery.

    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

    authors: Tran PH,Tran TT

    更新日期:2020-01-01 00:00:00

  • From "An Enzyme Able to Destroy Penicillin" to Carbapenemases: 70 Years of Beta-lactamase Misbehaviour.

    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

    authors: Frère JM,Sauvage E,Kerff F

    更新日期:2016-01-01 00:00:00

  • Metabolic syndrome as a modifier of atherosclerosis in murine models.

    abstract::The Metabolic Syndrome is a common metabolic disease associated with an increased risk for atherosclerotic cardiovascular disease and mortality. In contrast to "traditional" risk factors for atherosclerosis, such as low-density lipoprotein cholesterol, the Metabolic Syndrome represents a network of interacting risk fa...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945007782403838

    authors: Péterfy M,Davis RC,Lusis AJ

    更新日期:2007-11-01 00:00:00

  • Drug-binding databases.

    abstract::Recent developments in computer power and chemoinformatics methodology make possible that a huge amount of data become available through internet. These databases are devoted to a wide spectrum of scientific fields. Here we are concerned with databases related to protein-drug interactions. More specifically, databases...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945008786949379

    authors: Timmers LF,Pauli I,Caceres RA,de Azevedo WF Jr

    更新日期:2008-12-01 00:00:00

  • Inflammatory Bowel Disease in migrant populations - a narrative review.

    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

    authors: Estevinho MM,Lopes DJM,Souto MT,Magro F

    更新日期:2020-11-19 00:00:00

  • Triplex-forming oligonucleotides - sequence-specific DNA ligands as tools for gene inhibition and for modulation of DNA-associated functions.

    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

    authors: Besch R,Giovannangeli C,Degitz K

    更新日期:2004-11-01 00:00:00

  • State of the art: psychotherapeutic interventions targeting the psychological factors involved in IBD.

    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

    authors: Leone D,Menichetti J,Fiorino G,Vegni E

    更新日期:2014-01-01 00:00:00

  • Raloxifene.

    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

    authors: Kellen JA

    更新日期:2001-12-01 00:00:00

  • Serotonin (5-HT) in the regulation of depression-related emotionality: insight from 5-HT transporter and tryptophan hydroxylase-2 knockout mouse models.

    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

    authors: Araragi N,Lesch KP

    更新日期:2013-05-01 00:00:00

  • The molecular mechanisms of glucocorticoids-mediated neutrophil survival.

    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

    authors: Saffar AS,Ashdown H,Gounni AS

    更新日期:2011-04-01 00:00:00

  • Modulation of GABA(A) receptors by natural products and the development of novel synthetic ligands for the benzodiazepine binding site.

    abstract::Nature provides science and society with a virtually unlimited supply of structurally diverse and biologically active molecules; the natural products. While some are directly useful in commercial applications, others are valuable for studying and understanding biological phenomena at the molecular level. An example is...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945011798109509

    authors: Nilsson J,Sterner O

    更新日期:2011-10-01 00:00:00

  • Chemopreventive and chemotherapeutic potential of curcumin in breast cancer.

    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

    authors: Sinha D,Biswas J,Sung B,Aggarwal BB,Bishayee A

    更新日期:2012-12-01 00:00:00

  • Discovery and design of selective cyclooxygenase-2 inhibitors as non-ulcerogenic, anti-inflammatory drugs with potential utility as anti-cancer agents.

    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

    authors: Kalgutkar AS,Zhao Z

    更新日期:2001-03-01 00:00:00

  • Novel Antigen Targets for Immunotherapy of Acute Myeloid Leukemia.

    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

    authors: Goswami M,Hourigan CS

    更新日期:2017-01-01 00:00:00

  • Human Immunodeficiency Virus-1 Cell-To-Cell Transmission And Antiviral Strategies: An Overview.

    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:

    authors: Casartelli N

    更新日期:2015-08-25 00:00:00

  • Insight into Pain Modulation: Nociceptors Sensitization and Therapeutic Targets.

    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

    authors: Khan A,Khan S,Kim YS

    更新日期:2019-01-01 00:00:00

  • Sedation in PACU: indications, monitoring, complications.

    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

    authors: De Gaudio AR,Rinaldi S

    更新日期:2005-11-01 00:00:00

  • Beneficial effects of plant sources on the treatment of osteoporosis.

    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

    authors: Süntar I,Akkol EK

    更新日期:2013-12-01 00:00:00

  • Faecal Microbiota Transplantation in Inflammatory Bowel Disease: Current Concepts and Future Challenges.

    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

    authors: Zatorski H,Nakov R

    更新日期:2020-01-01 00:00:00

  • Nanocarrier Based Advances in Drug Delivery to Tumor: An Overview.

    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

    authors: Jain A,Kumari R,Tiwari A,Verma A,Tripathi A,Shrivastava A,Jain SK

    更新日期:2018-01-01 00:00:00

  • Study of Monocytes/Macrophages Stimuli as the Targets of Treating Inflammatory Bone Diseases.

    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

    authors: Liu Y,Cao Y,Smith W,He B,Yan L

    更新日期:2020-01-01 00:00:00

  • Vascular and parenchymal mechanisms in multiple drug resistance: a lesson from human epilepsy.

    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

    authors: Marroni M,Marchi N,Cucullo L,Abbott NJ,Signorelli K,Janigro D

    更新日期:2003-05-01 00:00:00

  • Is Galanin a Promising Therapeutic Resource for Neural and Nonneural Diseases?

    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

    authors: Oliveira Volpe CM,Vaz T,Rocha-Silva F,Villar-Delfino PH,Nogueira-Machado JA

    更新日期:2020-01-01 00:00:00

  • Resveratrol as a chemopreventive agent: a promising molecule for fighting cancer.

    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

    authors: Delmas D,Lançon A,Colin D,Jannin B,Latruffe N

    更新日期:2006-04-01 00:00:00