Recent patents on endocrine, metabolic & immune drug discovery最新文献

{"title":"Metreleptin Treatment in Patients with Non-HIV Associated Lipodystrophy.","authors":"Gulcin Akinci, B. Akıncı","doi":"10.2174/1574892811666151111142554","DOIUrl":"https://doi.org/10.2174/1574892811666151111142554","url":null,"abstract":"Lipodystrophies are a heterogeneous group of disorders characterized by congenital or acquired loss of adipose tissue. Recently, metreleptin, a recombinant human leptin analog, has been approved for the treatment of patients with generalized lipodystrophy. Leptin is an adipokine which has a fundamental role in glucose and lipid homeostasis. Metreleptin treatment has been demonstrated to improve metabolic abnormalities such as hyperglycemia, hypertriglyceridemia, increased hepatic fat content and elevated liver enzymes alanine transaminase and aspartate transaminase in patients with generalized lipodystrophy, and to correct hyperphagia that likely occurs as a result of leptin deficiency. Limited data has also suggested that metreleptin treatment might be beneficial on metabolic abnormalities in patients with partial lipodystrophy. This review focuses on potential benefits of metreleptin in various forms of non-HIV associated lipodystrophy. Safety issues have been discussed. Recent patent submissions have also been reviewed.","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"13 1","pages":"74-8"},"PeriodicalIF":0.0,"publicationDate":"2015-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78994114","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The antioxidant properties of organosulfur compounds (sulforaphane).","authors":"Sonia M de Figueiredo,&nbsp;Nancy S Binda,&nbsp;Jose A Nogueira-Machado,&nbsp;Sidney A Vieira-Filho,&nbsp;Rachel B Caligiorne","doi":"10.2174/1872214809666150505164138","DOIUrl":"https://doi.org/10.2174/1872214809666150505164138","url":null,"abstract":"<p><p>Sulforaphane (SFN) is a molecule within the isothiocyanate (ITC) group of organosulfur compounds. SFN is a phytochemical commonly found in cruciferous vegetables such as broccoli, brussels sprouts and cabbages. It has been widely studied in order to evaluate its chemopreventive properties and some of those have already been established by means of animal and human models. The SFN induces Phase I and II enzymes involved in detoxification processes of chemical carcinogens in order to prevent the start of carcinogenesis. It also presents anti-tumor action at post-initiation Phase, suggesting supplementary roles in cancer prevention. In a dose dependent manner, ITC inhibits the viability of human cancer cells, modifies epigenetic events that occur in cancer cells and present antiinflammatory effect acting during the initial of uncontrolled cell proliferation. This protective effect may be due to its antioxidant status, its recognized capacity to induce the expression and/or activity of of different cytoprotective proteins involved in the activating \"Nuclear factor erythroid-derived 2-like 2\" (Nrf2). Nevertheless, the effects on health and the possible connections among different diet constituents in humans must be carefully studied as there are limitations in the current data in order to better understand the molecular mechanisms responsible for those effects. This survey also includes relevant patents on the use of SFN, like its use in skin cancer treatment (US2015038580); and as an adjuvant in anti-cancer treatment (US2014228419). The use of SFN as an antioxidant dietary supplement, methods for compositions that promote glutathione production (WO2015002279) and methods for extracting and purifying SFN from broccoli seeds (CN104086469) are also included in this review. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 1","pages":"24-39"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872214809666150505164138","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33151458","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Adjudin--A Male Contraceptive with Other Biological Activities.","authors":"Yan-Ho Cheng,&nbsp;Weiliang Xia,&nbsp;Elissa W P Wong,&nbsp;Qian R Xie,&nbsp;Jiaxiang Shao,&nbsp;Tengyuan Liu,&nbsp;Yizhou Quan,&nbsp;Tingting Zhang,&nbsp;Xiao Yang,&nbsp;Keyi Geng,&nbsp;Bruno Silvestrini,&nbsp;Chuen-Yan Cheng","doi":"10.2174/1872214809666151029113043","DOIUrl":"https://doi.org/10.2174/1872214809666151029113043","url":null,"abstract":"<p><strong>Background: </strong>Adjudin has been explored as a male contraceptive for the last 15 years since its initial synthesis in the late 1990s. More than 50 papers have been published and listed in PubMed in which its mechanism that induces exfoliation of germ cells from the seminiferous epithelium, such as its effects on actin microfilaments at the apical ES (ectoplasmic specialization, a testis-specific actin-rich anchoring junction) has been delineated.</p><p><strong>Objective: </strong>Recent studies have demonstrated that, besides its activity to induce germ cell exfoliation from the seminiferous epithelium to cause reversible infertility in male rodents, adjudin possesses other biological activities, which include anti-cancer, anti-inflammation in the brain, and anti-ototoxicity induced by gentamicin in rodents. Results of these findings likely spark the interest of investigators to explore other medical use of this and other indazole-based compounds, possibly mediated by the signaling pathway(s) in the mitochondria of mammalian cells following treatment with adjudin. In this review, we carefully evaluate these recent findings.</p><p><strong>Methods: </strong>Papers published and listed at www.pubmed.org and patents pertinent to adjudin and its related compounds were searched. Findings were reviewed and critically evaluated, and summarized herein.</p><p><strong>Results: </strong>Adjudin is a novel compound that possesses anti-spermatogenetic activity. Furthermore, it possesses anti-cancer, anti-inflammation, anti-neurodegeneration, and anti-ototoxicity activities based on studies using different in vitro and in vivo models.</p><p><strong>Conclusion: </strong>Studies on adjudin should be expanded to better understand its biological activities so that it can become a useful drug for treatment of other ailments besides serving as a male contraceptive.</p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"63-73"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5802880/pdf/nihms938764.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34192864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biology and Regulatory Roles of Nuclear Lamins in Cellular Function and Dysfunction.","authors":"Syeda G Khadija,&nbsp;Fei Chen,&nbsp;Timothy Hadden,&nbsp;Randall L Commissaris,&nbsp;Anjaneyulu Kowluru","doi":"10.2174/1872214809666151009120402","DOIUrl":"https://doi.org/10.2174/1872214809666151009120402","url":null,"abstract":"<p><p>Nuclear lamins, namely lamins A, B and C, surround the nucleoplasmic contents in a meshlike network called the nuclear lamina. These intermediate filaments provide a structural framework to the nuclear envelope (NE), play a role in arrangement of the chromatin within the nucleus, in DNA replication and also participate in DNA damage repair. In order for lamins to be involved in these important nuclear processes and to be functionally active, they undergo a series of post-translational modifications (farnesylation, endoproteolytic cleavage, carboxylmethylation etc.), of which farnesylation is the most studied. Improper farnesylation of lamin proteins, especially lamin A, leads to a number of diseases affecting the striated muscle (e.g. Emery- Dreifuss Muscular Dystrophy, Dilated Cardiomyopathy), adipose tissue (e.g. Dunnigan-type familial partial lipodystrophy) and could result in abnormal senescence and growth deformities (e.g. Progeria syndrome); these are referred to as laminopathies. Despite the existing literature and evidence regarding functions of lamins and diseases associated with abnormal lamin processing, a lot remains to be understood in regards to lamin biology and their role as potential therapeutic targets. In this brief review, we have attempted to summarize the roles of lamins in physiology and pathology of the cell and in type 2 diabetes mellitus [T2DM] and also enlisted patents on methods, systems and devices developed for improving pancreatic beta cell function in diabetes mellitus. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"111-20"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34074067","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biochemical Markers of Bone Turnover and their Role in Osteoporosis Diagnosis: A Narrative Review.","authors":"Patricia Khashayar,&nbsp;Hamidreza Aghaei Meybodi,&nbsp;Ghassem Amoabediny,&nbsp;Bagher Larijani","doi":"10.2174/1872214809666150806105433","DOIUrl":"https://doi.org/10.2174/1872214809666150806105433","url":null,"abstract":"<p><p>Osteoporosis diagnosis, which is nowadays generally made based on bone mineral density (BMD) measurements, suffers from certain limitations. Thus it is believed that bone turnover markers (BTMs) can help improve osteoporosis detection. The shifting interest toward this topic made us perform a review to gather information on existing markers and their role in osteoporosis diagnosis. Based on the results, in this review, a list of existing markers and some of their characteristics is provided. Moreover, a brief explanation of different types of variability met while using these markers is also described. Finally some of the patents provided for the diagnosis of these markers are presented. While the use of BTMs in osteoporosis diagnosis has certain advantages over BMD and clinical risk assessment tools, more studies are needed before they can be used as a separate tool in this regard. It could be concluded that despite the fact that BTMs are better than BMD not only in monitoring treatment but also in identifying those at-risk, the diagnostic value of BTMs in predicting osteoporosis is low, and thus a model is needed to assess several BTMs at the same time with higher accuracy and lower variability to overcome this limitation.</p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"79-89"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33965990","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correlation of Urine Biomarkers: Microalbuminuria and Spot Urine Protein among Diabetic Patients. Application of Spot Urine Protein in Diabetic Kidney Disease, Nephropathy, Proteinuria Estimation, Diagnosing and Monitoring.","authors":"Kamran M A Aziz","doi":"10.2174/1872214809666150708111022","DOIUrl":"https://doi.org/10.2174/1872214809666150708111022","url":null,"abstract":"<p><p>Current study has invented a new method for utilizing spot urine protein among diabetic patients. There have been various efforts and strategies in research internationally to detect, diagnose and monitor nephropathy/DKD. Although 24-hour urine studies are gold standard, however, there exist some controversies about microalbuminuria and spot urine protein. The current study was designed to utilize spot urine protein among diabetic patients and to find its association with routine dipstick urine test for albumin, and microalbuminuria. The study demonstrated significant association of spot urine protein with urine dipstick albumin, and has demonstrated increasing spot urine protein with increasing albumin in urine (p-value < 0.0001). This study also demonstrated significantly higher levels of spot urine protein between the groups with nephropathy/DKD as compared to those without nephropathy/DKD (p-value < 0.0001). Similarly, spot urine protein and spot urine protein/creatinine were also significantly associated with microalbumin and microalbumin/creatinine in urine. Significant regression models for spot urine protein and microalbuminuria were also developed and proposed to detect and estimate microalbumin in urine while utilizing spot urine protein (< 0.0001). Synthesized regression equations and models can be used confidently to detect, rule out and monitor proteinuria and DKD. ROC curves were utilized to detect spot urine protein cutoff points for nephropathy and DKD with high specificity and sensitivity. Some important patents were also discussed in the paper regarding albuminuria/proteinuria detection and management. Current study has demonstrated and concluded, for the first time, that there exists a significant association of spot urine protein with routine dipstick albumin in urine and microalbuminuria. It is also essential to detect early, monitor and manage proteinuria, hypertension and dyslipidemia with good glycemic control to prevent diabetes complications. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"121-33"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34269859","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Current Approaches to the Diagnosis of Classical form of Congenital Adrenal Hyperplasia.","authors":"Elwira Przybylik-Mazurek,&nbsp;Anna Kurzynska,&nbsp;Anna Skalniak,&nbsp;Alicja Hubalewska-Dydejczyk","doi":"10.2174/1872214809666151005123928","DOIUrl":"https://doi.org/10.2174/1872214809666151005123928","url":null,"abstract":"<p><p>Congenital adrenal hyperplasia (CAH) is one of the most common diseases transmitted in an autosomal recessive manner and is caused by mutations of enzymes which are responsible for the process of adrenal steroidogenesis. According to the impairment of enzymes involved in steroidogenesis, several types of CAH can be distinguished. The most common type is associated with mutations in the CYP21A2 gene, encoding 21-hydroxylase enzyme and has different clinical forms: Classical (in which there are two types: salt wasting and simple virilization) and non-classical, characterized by less severe symptoms and late onset. CAH is characterized by a strong correlation between the genotype and the phenotype. Mutations in the CYP21A2 gene can cause different degrees of loss of 21-hydroxylase enzyme activity which result in a wide spectrum of clinical pictures. Several methods used to diagnose CAH (such as determining steroids in serum or urine) have been known from the 70's. Modern diagnosis of CAH is based primarily on the use of genetic testing, which is the subject of numerous constantly updated patents. In this paper the most recent patents on the diagnosis of CAH were assessed. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"103-10"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34127528","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abatacept and Glomerular Diseases: The Open Road for the Second Signal as a New Target is Settled Down.","authors":"Hernan Trimarchi","doi":"10.2174/1872214809666150302104542","DOIUrl":"https://doi.org/10.2174/1872214809666150302104542","url":null,"abstract":"<p><p>Glomerulopathy is the third most important cause of kidney disease. Proteinuria is the hallmark of glomerular damage, and a marker of progression of kidney disease, cardiovascular morbidity and mortality. Strategies to reduce proteinuria are partially successful, and despite proteinuria management, renal disease may still progress. Immunosuppression to treat glomerulopathies is nonspecific, partially effective and presents side-effects. It is critical to find safe drugs with specific podocyte molecular targets. Podocytes contain a complex array of proteins. Lymphocyte activation antigen B7-1 (CD80) is located on antigen presenting cells modulating CD4+ and CD8+ T cells by interacting with co-stimulator CD28, a glycoprotein located on T-cells, or with cytotoxic T-lymphocyte protein 4 (CTLA-4) co-inhibitor. Normally, podocytes do not express B7-1. However, certain glomerulopathies are associated with an increase on the surface of podocytes of B7-1, which reduces the ability of podocytes to attach to the surrounding glomerular basement membrane, favouring podocyturia and proteinuria. When the B7-1-CTLA-4 interaction takes place, the immune response is abrogated, while a B7-1-CD28 coupling leads to T cell activation. Abatacept binds to B7-1 by blocking the CD28 or potentiating the CTLA-4 signals. In B7-1 positive podocytes, abatacept may be a specific tool to decrease proteinuria. Selected patents are also briefly presented in this review. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 1","pages":"2-14"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872214809666150302104542","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33427046","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Resveratrol Pretreatment Ameliorates TNBS Colitis in Rats.","authors":"Gulserap Yildiz, Yuksel Yildiz, Pinar A Ulutas, Asl Yaylali, Muruvvet Ural","doi":"10.2174/1872214809666150806105737","DOIUrl":"10.2174/1872214809666150806105737","url":null,"abstract":"<p><p>Inflammatory bowel disease (IBD) is a chronic intestinal inflammatory disease in humans constituting a major health concern today whose prevalence has been increasing over the world. Production of reactive oxygen species (ROS) and disturbed capacity of antioxidant defense in IBD subjects have been reported. Antioxidants may play a significant role in IBD treatment. This study aimed at evaluating ameliorative effects of intraperitoneal resveratrol pretreatment on trinitrobenzene sulphonic acid (TNBS)-induced colitis in rats. Thirty five Wistar-Albino female rats were divided equally into five groups. Inflammation was induced by the intrarectal administration of TNBS under anesthesia. Intraperitoneal administration of resveratrol (RSV) at a concentration of 10mg/kg/day for 5 days before the induction of colitis significantly reduced microscopy score and malondialdehyde (MDA) levels and increased glutathione peroxidase (GSH Px) activity compared to TNBS and vehicle groups. Also an insignificant increase in catalase (CAT) activity was observed in the RSV treated group compared to TNBS and vehicle groups. In this paper, the most recent patent on the identification and treatment of IBD was indicated. In conclusion, antioxidant RSV proved to have a beneficial effect on TNBS colitis in rats. In light of these advantageous results, the RSV can be considered as adjuvant agent in IBD treatments. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 2","pages":"134-40"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872214809666150806105737","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33965991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent patents on new steroid agents targeting the steroidogenesis for endocrine cancer treatments.","authors":"Donald Poirier","doi":"10.2174/1872214809666150201214602","DOIUrl":"https://doi.org/10.2174/1872214809666150201214602","url":null,"abstract":"<p><p>Cancer is a leading cause of death in the population and despite the significant technological advances that have been made over the last years, there is a great need for new and better treatments with fewer side effects. Among the various types, hormone-dependent cancers are stimulated by the presence of certain steroidal hormones such as androgens and estrogens, which act through a nuclear receptor. The use of small molecules to block the biosynthesis (steroidogenesis) or the action of hormones (androgens or estrogens) is a therapeutic approach that has yielded interesting results and whose development continues. This review article emphasizes the patents and patent applications published over the last five years. It deals exclusively with steroid compounds developed as inhibitors of key enzymes (17α-hydroxylase/17,20-lyase, steroid sulfatase, 5α-reductases, aromatase and 17β-hydroxysteroid dehydrogenases) involved in the steroidogenesis and identified as therapeutic targets. Such inhibitors could be used as a drug to reduce the concentration of androgens or estrogens and, consequently, for treating hormone-dependent diseases such as prostate cancer, breast cancer and endometriosis. </p>","PeriodicalId":89474,"journal":{"name":"Recent patents on endocrine, metabolic & immune drug discovery","volume":"9 1","pages":"15-23"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872214809666150201214602","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33022754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}