Recent patents on CNS drug discovery最新文献_第4页

Possible physiopathological effects of the transglutaminase activity on the molecular mechanisms responsible for human neurodegenerative diseases. 转谷氨酰胺酶活性在人类神经退行性疾病分子机制中可能的生理病理作用。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666141111160124

Martina Iannaccone, Federica Titta, Enrica Serretiello, Marco Monfregola, Vittorio Gentile

{"title":"Possible physiopathological effects of the transglutaminase activity on the molecular mechanisms responsible for human neurodegenerative diseases.","authors":"Martina Iannaccone, Federica Titta, Enrica Serretiello, Marco Monfregola, Vittorio Gentile","doi":"10.2174/1574889809666141111160124","DOIUrl":"https://doi.org/10.2174/1574889809666141111160124","url":null,"abstract":"Transglutaminases are a class of ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). In absence of co-substrates, the nucleophile may be water, resulting in the net deamidation of the glutaminyl residue. Transglutaminase activity has been suggested to be involved in molecular mechanisms responsible for both physiological or pathological processes. Recently, transglutaminase activity has been shown to be responsible for a widespread human autoimmune disease, the Celiac Disease. Interestingly, neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease, supranuclear palsy, Huntington's disease and other polyglutamine diseases, are characterized in part by aberrant cerebral transglutaminase activity and by increased cross-linked proteins in affected brains. This review focuses on the possible molecular mechanisms responsible for such diseases and on the possible therapeutic effects of transglutaminase inhibitors for patients with diseases characterized by aberrant transglutaminase activity. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 2","pages":"76-84"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32806515","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}

引用次数: 7

Drug-drug interactions: antiretroviral drugs and recreational drugs. 药物-药物相互作用:抗逆转录病毒药物和娱乐性药物。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666141127101623

Orietta Staltari, Christian Leporini, Benedetto Caroleo, Emilio Russo, Antonio Siniscalchi, Giovambattista De Sarro, Luca Gallelli

{"title":"Drug-drug interactions: antiretroviral drugs and recreational drugs.","authors":"Orietta Staltari, Christian Leporini, Benedetto Caroleo, Emilio Russo, Antonio Siniscalchi, Giovambattista De Sarro, Luca Gallelli","doi":"10.2174/1574889809666141127101623","DOIUrl":"https://doi.org/10.2174/1574889809666141127101623","url":null,"abstract":"With the advances in antiretroviral (ARV) therapy, patients with Human Immunodeficiency Virus (HIV) infection are living longer, however, some patients encounter co- morbidities which sometimes require treatment. Therefore, during the treatment with ARV drugs these patients could take several recreational drugs (e.g. amphetamines, hallucinogenes, opiates, or alcohol) with a possible development of drug-drug interactions (DDIs). In particular, Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs/NtRTIs) are mainly excreted through the kidney and are not substrates of the cytochrome P450 or P-glycoprotein, therefore the DDIs during this treatment are minimal. In contrast, the other ARV drugs (i.e. non-nucleoside reversetranscriptase inhibitors, Protease inhibitors, Integrase inhibitors, chemokine receptor 5 antagonists and HIV-fusion inhibitors) are an important class of antiretroviral medications that are frequent components of HAART regimens but show several DDIs related to interaction with the cytochrome P450 or P-glycoprotein. In this paper we will review data concerning the possibility of DDI in HIV patients treated with ARV and taking recreational drugs. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 3","pages":"153-63"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32841668","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}

引用次数: 12

Liver growth factor as a tissue regenerating factor in neurodegenerative diseases. 肝脏生长因子是神经退行性疾病中的一种组织再生因子。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666141224123303

Rafael Gonzalo-Gobernado, Lucia Calatrava-Ferreras, Juan Perucho, Diana Reimers, MarIa J Casarejos, Antonio S Herranz, Adriano Jimenez-Escrig, Juan J Diaz-Gil, Eulalia Bazan

{"title":"Liver growth factor as a tissue regenerating factor in neurodegenerative diseases.","authors":"Rafael Gonzalo-Gobernado, Lucia Calatrava-Ferreras, Juan Perucho, Diana Reimers, MarIa J Casarejos, Antonio S Herranz, Adriano Jimenez-Escrig, Juan J Diaz-Gil, Eulalia Bazan","doi":"10.2174/1574889809666141224123303","DOIUrl":"10.2174/1574889809666141224123303","url":null,"abstract":"Liver growth factor (LGF) is a hepatic mitogen purified by our group in 1986. In the following years we demonstrated its activity both in \"in vivo\" and \"in vitro\" systems, stimulating hepatocytes mitogenesis as well as liver regeneration in several models of liver injury. Furthermore, we established its chemical composition (albumin-bilirubin complex) and its mitogenic actions in liver. From 2000 onwards we used LGF as a tissue regenerating factor in several models of extrahepatic diseases. The use of Liver growth factor as a neural tissue regenerator has been recently protected (Patent No US 2014/8,642,551 B2). LGF administration stimulates neurogenesis and neuron survival, promotes migration of newly generated neurons, and induces the outgrowth of striatal dopaminergic terminals in 6-hidroxydopamine-lesioned rats. Furthermore, LGF treatment raises striatal dopamine levels and protects dopaminergic neurons in hemiparkinsonian animals. LGF also stimulates survival of grafted foetal neural stem cells in the damaged striatum, reduces rotational behaviour and improves motor coordination. Interestingly, LGF also exerts a neuroprotective role both in an experimental model of cerebellar ataxia and in a model of Friedrich´s ataxia. Microglia seem to be the cellular target of LGF in the CNS. Moreover, the activity of the factor could be mediated by the stimulation of MAPK´s signalling pathway and by regulating critical proteins for cell survival, such as Bcl-2 and phospho-CREB. Since the factor shows neuroprotective and neurorestorative effects we propose LGF as a patented novel therapeutic tool that may be useful for the treatment of Parkinson´s disease and cerebellar ataxias. Currently, our studies have been extended to other neurological disorders such as Alzheimer's disease (Patent No: US 2014/0113859 A1). ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"9 3","pages":"173-80"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/63/68/RPCN-9-173.PMC4485410.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32930929","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}

引用次数: 0

Recent patents on novel MCH1 receptor antagonists as potential anti-obesity drugs. 新型MCH1受体拮抗剂作为潜在的抗肥胖药物的最新专利。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889809666140613115426

Katalin K Szalai, Gyula Beke, János Éles, Tamás Kitka, Péter Kovács, József Nagy, Sándor Farkas, András Boros

引用次数: 11

Genetic and bioinformatic studies of antidepressant drug therapeutic efficacy and toxicity: a current overview. 抗抑郁药物治疗效果和毒性的遗传和生物信息学研究:当前综述。

Recent patents on CNS drug discovery Pub Date : 2014-01-01 DOI: 10.2174/1574889810666150209103931

Da-Yong Lu, Ting-Ren Lu, Jin-Yu Che, Peng-Peng Zhu

引用次数: 0

An ion channel chip for diagnosis and prognosis of autoimmune neurological disorders. 一种用于自身免疫性神经系统疾病诊断和预后的离子通道芯片。

Recent patents on CNS drug discovery Pub Date : 2013-12-01 DOI: 10.2174/15748898113086660004

Franck C Chatelain, Michel Mazzuca, Marie-Madeleine Larroque, Veronique Rogemond, Jerome Honnorat, Florian Lesage

引用次数: 0

Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions. TRPV1通道的调节:目前的临床试验和最近的专利，重点是神经系统疾病。

Recent patents on CNS drug discovery Pub Date : 2013-12-01 DOI: 10.2174/1574889808666131209124012

Luciano De Petrocellis, Aniello S Moriello

{"title":"Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions.","authors":"Luciano De Petrocellis, Aniello S Moriello","doi":"10.2174/1574889808666131209124012","DOIUrl":"https://doi.org/10.2174/1574889808666131209124012","url":null,"abstract":"The transient receptor potential vanilloid-1 cat ion channel (TRPV1) is a nonspecific cation channel that can be activated by multiple endogenous stimuli and is expressed predominantly in sensory neurons, where it serves as a key nodal point in pain transmission pathways. In mammals, TRPV1 displays a wide tissue and cellular expression including both the peripheral and central nervous system, and in the latter it is now recognized to have a broader distribution and function. The pharmacological modulation of TRPV1 represents a strategy for the treatment of a variety of disease states, particularly those requiring chronic pain management. The validation of the TRPV1 channel as a therapeutic target for the control of pain and inflammatory conditions in a variety of diseases and injury states, has prompted the development of several TRPV1 agonists and antagonists that have entered clinical trials. Studies comparing the analgesic effects of TRPV1 antagonists with and without significant CNS penetration demonstrated that a dual (both peripheral and central) action is required to produce broad-spectrum analgesia. TRPV1 can be considered as a target for next generation analgesics. However, although a number of compounds are in clinical trials, the therapeutic utility of TRPV1 agonist and antagonists is yet to be validated unequivocally. This review summarizes current clinical trials and recent patents with small molecule TRPV1 agonists and antagonists with a focus on neurological conditions. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"8 3","pages":"180-204"},"PeriodicalIF":0.0,"publicationDate":"2013-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31947907","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}

引用次数: 39

Cerebrovascular ultrasonography for selecting patients for stroke intervention. 脑血管超声在脑卒中干预患者选择中的应用。

Recent patents on CNS drug discovery Pub Date : 2013-12-01 DOI: 10.2174/1574889808666131209124519

Vijay K Sharma, Kusuma Yohanna, Ghulam Kawnayn, Nabin Sarkar, Amit Batra

{"title":"Cerebrovascular ultrasonography for selecting patients for stroke intervention.","authors":"Vijay K Sharma, Kusuma Yohanna, Ghulam Kawnayn, Nabin Sarkar, Amit Batra","doi":"10.2174/1574889808666131209124519","DOIUrl":"https://doi.org/10.2174/1574889808666131209124519","url":null,"abstract":"Currently employed diagnostic ultrasonography provides clinically relevant information about cerebral hemodynamic changes in patients with cerebrovascular ischemia. The information thus obtained is often helpful to the physician for establishing or confirming the diagnosis and prognosis as well as in taking appropriate therapeutic decisions. It is associated with a high temporal resolution and can be performed bedside for rapid diagnosis as well as prolonged monitoring. Transcranial Doppler (TCD) ultrasonography is a non-invasive diagnostic modality that provides physiological information regarding various intracranial hemodynamic alterations in patients with cerebrovascular ischemia. Extended applications of TCD are useful in understanding various pathophysiological mechanisms responsible for the clinical manifestations of cerebrovascular ischemia. Thus, TCD is aptly called as the 'stethoscope' of a stroke neurologist. Cerebrovascular ultrasonography is considered as an essential component of a comprehensive stroke center. We have reviewed various recent patents pertaining to the applications of cerebrovascular ultrasonography employed in the selection of stroke patients for various therapeutic interventions. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"8 3","pages":"205-19"},"PeriodicalIF":0.0,"publicationDate":"2013-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31947908","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}

引用次数: 2

Transglutaminase activity as a possible therapeutical target in neurodegenerative diseases. 转谷氨酰胺酶活性作为神经退行性疾病可能的治疗靶点。

Recent patents on CNS drug discovery Pub Date : 2013-12-01 DOI: 10.2174/1574889808666131128105630

Martina Iannaccone, Federica Titta, Enrica Serretiello, Giulia De Vivo, Antonio Martin, Vittorio Gentile

{"title":"Transglutaminase activity as a possible therapeutical target in neurodegenerative diseases.","authors":"Martina Iannaccone, Federica Titta, Enrica Serretiello, Giulia De Vivo, Antonio Martin, Vittorio Gentile","doi":"10.2174/1574889808666131128105630","DOIUrl":"https://doi.org/10.2174/1574889808666131128105630","url":null,"abstract":"Transglutaminases are ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). In absence of co-substrates, the nucleophile may be water, resulting in the net deamidation of the glutaminyl residue. Transglutaminase activity has been suggested to be involved in molecular mechanisms responsible for both physiological or pathological processes. For example, neurodegenerative diseases, such as Alzheimer's Disease, Parkinson's Disease, supranuclear palsy, Huntington's Disease and other polyglutamine diseases, are characterized in part by aberrant cerebral transglutaminase activity and by increased cross-linked proteins in affected brains. This review focuses on the possible molecular mechanisms responsible for such diseases and on the possible therapeutic effects of selective transglutaminase inhibitors for patients with diseases characterized by aberrant transglutaminase activity. The article presents some promising patents on the transglutaminase activity. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"8 3","pages":"235-42"},"PeriodicalIF":0.0,"publicationDate":"2013-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31911413","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}

引用次数: 3

Patents on brain permeable nanoparticles. 脑渗透纳米颗粒专利。

Recent patents on CNS drug discovery Pub Date : 2013-12-01 DOI: 10.2174/1574889808666131128105141

Monica Gulati, Dimple S Chopra, Sachin K Singh, Vikrant Saluja, Purnima Pathak, Parikshit Bansal

{"title":"Patents on brain permeable nanoparticles.","authors":"Monica Gulati, Dimple S Chopra, Sachin K Singh, Vikrant Saluja, Purnima Pathak, Parikshit Bansal","doi":"10.2174/1574889808666131128105141","DOIUrl":"https://doi.org/10.2174/1574889808666131128105141","url":null,"abstract":"The blood-brain barrier (BBB) presents a combination of physical and electrostatic barriers. It is a highly complex structure that tightly regulates the movement of molecules from the blood to brain, protecting it from injuries and diseases. However, the BBB also significantly precludes the delivery of drugs to the brain, thus, preventing the therapy of a number of neurological disorders like brain cancer, epilepsy, Alzheimer's disease, schizophrenia etc. Numerous drug delivery strategies have been developed to circumvent this barrier. Out of those, one popular approach is the use of nanoparticles. Nanoparticles form solid, colloidal drug delivery system that consists of macromolecular materials in which the active principle is dissolved, entrapped or encapsulated or onto which the active principle is adsorbed or attached. Brain targeted polymeric nanoparticles have been found to increase the therapeutic efficacy and reduce the toxicity for a large number of drugs. By coating the nanoparticles with surfactants, higher concentrations of the drugs can be delivered. The article presents various approaches used in design and delivery of nanoparticles to brain. It also reviews various patents that describe the use of nanoparticles to deliver various neurotherapeutics to brain. ","PeriodicalId":87737,"journal":{"name":"Recent patents on CNS drug discovery","volume":"8 3","pages":"220-34"},"PeriodicalIF":0.0,"publicationDate":"2013-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31911414","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}

引用次数: 10