Recent Patents on CNS Drug Discovery 
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Authors: Holscher C
Abstract
Analogues of the incretins Glucagon-like peptide 1 (GLP-1) and Glucose-dependent insulinotropic peptide (GIP) have been developed to treat type 2 diabetes mellitus. They are protease resistant and have a longer biological half life than the native peptides. Some of these novel analogues can cross the blood-brain barrier, have neuroprotective effects, activate neuronal stem cells in the brain, and can improve cognition. The receptors for GIP and GLP-1 are expressed in neurons, and both GIP and GLP-1 are expressed and released as transmitters by neurons. GIP analogues such as DAl...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Cerebrospinal fluid proteins in the diagnosis of Alzheimer's disease.
Authors: Papaliagkas VT, Tsolaki M, Anogianakis G
Abstract
Alzheimer's disease (AD) is rapidly grooving incidence that affects millions of people worldwide, therefore there is an immediate need for its' early and accurate diagnosis. Many research studies have been performed on possible accurate and reliable diagnostic biomarkers of AD. This review study provides an overview on the cerebrospinal fluid (CSF) proteins that are used as biochemical markers for the early diagnosis of AD and their future prospects, as well as relevant patents.
PMID: 20408808 [PubMed - indexed for MEDLINE] (Source: Recent ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
New devices for treating acute ischemic stroke.
Authors: Rosenberg N, Chen M, Prabhakaran S
Abstract
The past decade has witnessed an explosion of devices available for treating acute ischemic stroke. Here, we review a range of recently patented devices and the data supporting their use. These include devices to enhance thrombolysis, thrombectomy devices, stents, devices for augmenting global brain tissue perfusion, and devices that provide neuroprotection after stroke. We discuss specific design elements of these devices and directions for future research. Ultimately, individually tailored combinations of these devices will likely prove most useful in ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Transglutaminases as possible therapeutic targets in neurodegenerative diseases.
Authors: Martin A, De Vivo G, Ricotta M, Iannuzzi M, Gentile V
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 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 ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Neurogenic drugs and compounds.
Authors: Taupin P
Abstract
The advent of adult neurogenesis and neural stem cell (NSC) research opens new avenues and opportunities for treating neurological diseases and disorders, particularly for the discovery and development of novel drugs. Adult neurogenesis is modulated by a broad range of stimuli, physio- and pathological processes, trophic factors/cytokines and drugs, particularly drugs used for treating neurological diseases and disorders. Hence, adult neurogenesis is the target of drugs used for treating neurological diseases and disorders, such as Alzheimer's disease and depression, and the acti...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Current options in the treatment of mitochondrial diseases.
Authors: Scarpelli M, Cotelli MS, Mancuso M, Tomelleri G, Tonin P, Baronchelli C, Vielmi V, Gregorelli V, Todeschini A, Padovani A, Filosto M
Abstract
Mitochondrial diseases (MD) are disorders caused by an impairment of the mitochondrial respiratory chain function. They are usually progressive, isolated or multi-system diseases and have variable times of onset. Because mitochondria have their own DNA (mtDNA), MD can be caused by mutations in both mtDNA and nuclear DNA (nDNA). The complexity of genetic control of mitochondrial function is in part responsible for the intra- and inter-familiar clinical hetero...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
On the future development of optimally-sized lipid-insoluble systemic therapies for CNS solid tumors and other neuropathologies.
Authors: Sarin H
Abstract
It remains a challenge to deliver effective concentrations of therapeutics into CNS pathologies, which is primarily due to the fact that current and investigational CNS therapeutics are suboptimally-sized to accumulate to effective concentrations in individual diseased CNS tissue cells. The blood-CNS barrier of blood capillary microvasculature within neuropathologic tissues is known to be permeable to lipid-insoluble macromolecules in a wide-spectrum of neuropathologies. In the case of CNS solid tumor tissue blood capillaries, the physiological upper limit of pore size to the tran...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
PTI-609: a novel analgesic that binds filamin A to control opioid signaling.
Authors: Burns LH, Wang HY
Abstract
Binding a critical pentapeptide region on the scaffolding protein filamin A regulates signaling of mu opioid receptors (MORs) so that their activation should not result in the opioid tolerance, dependence and addiction associated with current opioid painkillers. Additionally, we show that compounds that bind this site on filamin A reduce release of inflammatory cytokines. PTI-609 is a new chemical entity that binds filamin A with picomolar affinity and also activates opioid receptors via a novel binding domain. PTI-609 and analogs have similar analgesic efficacy to morph...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Copper status abnormalities and how to measure them in neurodegenerative disorders.
Authors: Siotto M, Bucossi S, Squitti R
Abstract
Copper is essential for life. It plays a pivotal role in the central nervous system, in which a low concentration of copper results in incomplete development, whereas an excess of copper is injurious. Redox reactions are at the basis of copper toxicity: in fact, it catalyses the production of reactive oxygen species in Fenton or Haber-Weiss reactions. Abnormalities of copper homeostasis in neurodegenerative disorders were discovered decades ago. The steady increase in reports from the literature demonstrating copper involvement in neurodegenerative disorders...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Pharmacological therapy of Parkinson's disease: current options and new avenues.
Authors: Simola N, Pinna A, Fenu S
Abstract
Parkinson's disease is a neurodegenerative pathology which affects the dopaminergic neurons in the mesencephalon, leading to a progressive and relentless motor disability and to non-motor symptoms of different severity. The aim of this review is to summarize the features of drugs currently used in the pharmacotherapy of Parkinson's disease, with a look at their beneficial effects and limitations. Drugs acting on dopamine transmission, as L-DOPA, direct dopaminergic agonists, inhibitors for either the MAO or COMT enzymes and drugs acting on neurotransmitters other...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Future targeted disease modifying drugs for Alzheimer's disease.
Authors: Dash SK
Abstract
Alzheimer's disease is the most common form of dementia. Alzheimer's disease will be responsible for an enormous burden on the individual and the society, as with the aging of the population, the incidence and the prevalence will grow. Presently, the drugs used in Alzheimer's disease are only effective symptomatically and improve functioning. They do not halt the progression of the disease. With the recent advances in our understanding of the pathogenesis of this disease, there have been tremendous advances in the clinical trials of compounds that can modify the disease process. N...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Towards drug discovery for brain tumours: interaction of kinins and tumours at the blood brain barrier interface.
Authors: Harford-Wright E, Lewis KM, Vink R
Abstract
Cancers of the brain are intrinsically more complicated to treat than systemic malignancies due to the unique anatomical features of the brain. The blood-brain barrier prevents chemotherapeutic agents from reaching brain neoplasms, and angiogenesis occurs as the metabolic needs of the tumour increase, thus further complicating treatment. The newly formed blood vessels form the blood-tumour barrier and are distinct from the blood-brain barrier in that they are more permeable. Being more permeable, these abnormal blood vessels lead to the formation of peri...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Recent developments in therapeutic approaches for lysosomal storage diseases.
Authors: Urbanelli L, Magini A, Polchi A, Polidoro M, Emiliani C
Abstract
Genetic mutations that cause specific lysosomal protein deficiencies account for more than 45 Lysosomal Storage Diseases (LSDs), mostly pre-adult disorders which are associated with neurological symptoms and mental retardation. Interestingly, such diseases are often characterized by intracellular deposition and protein aggregation, events also found in age-related neurodegenerative diseases. During the past twenty years, different approaches have been introduced for the treatment of these disorders, several of which are now in routin...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Current and future therapies of erectile dysfunction in neurological disorders.
Authors: Calabrò RS, Polimeni G, Bramanti P
Abstract
Erection is a neurovascular event characterized by the tumescence of the cavernous bodies that relies upon integration of neural and humoral mechanisms requiring the participation of autonomic and somatic nerves and the integration of numerous spinal and supraspinal sites. Erectile dysfunction (ED) is a highly prevalent problem increasing with age, as well as the major men's sexual concern. Significant advances in the pharmacological treatment of ED have occurred in recent years, most notably after the introduction of sildenafil, the first oral selectiv...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
Recent developments in tau-based therapeutics for neurodegenerative diseases.
Authors: Medina M
Abstract
Neurodegenerative diseases constitute a major public health issue due to an increasingly aged population as a consequence of generally improved medical care and demographic changes. Current drug treatment of Alzheimer's disease (AD), the most prevalent dementia, with cholinesterase inhibitors or NMDA antagonists has demonstrated very modest, symptomatic efficacy, leaving an unmet medical need for new, more effective therapies. Drug development efforts for AD in the last two decades have primarily focused on targets defined by the amyloid cascade hypothesis, so far with disappoint...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research
