Therapeutic approaches for lysosomal storage diseases: a patent update.
Authors: Urbanelli L, Sagini K, Polidoro M, Brozzi A, Magini A, Emiliani C Abstract Lysosomal Storage Diseases (LSDs) are inherited metabolic disorders caused by specific lysosomal protein deficiencies, which lead to abnormal storage of macromolecular substrates. Most LSDs are characterized by central nervous system (CNS) pathology, intracellular deposition and protein aggregation, events also found in age-related neurodegenerative diseases. Over the past two decades, a few approaches for the cure of these disorders have been approved for clinical use, i.e. enzyme replacement therapy (ERT) and substrate re...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

The role of Cnidaria in drug discovery. A review on CNS implications and new perspectives.
Authors: Mariottini GL, Pane L Abstract Many organisms produce bioactive substances used in the production of drugs. In this context, Cnidaria occupy a major position; for this reason, research on new bioactive substances has focused upon them as an interesting target. As a matter of fact, substances and extracts able to fight human diseases have been found in cnidarians, several of which have been studied in laboratories using animal models or cell cultures and, at present, some are in the pre-clinical phase. This review aims to highlight the research on existing drugs or new drug candidates extracted fro...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

An ion channel chip for diagnosis and prognosis of autoimmune neurological disorders.
Authors: Chatelain FC, Mazzuca M, Larroque MM, Rogemond V, Honnorat J, Lesage F Abstract Autoantibodies directed against ion channels and ionotropic receptors are associated with neuromuscular and neurological disorders. Their detection has proven to be useful for diagnosis, prognosis and treatment of these autoimmune syndromes. We have designed an ion channel chip for the systematic and rapid screening of antibodies directed against tens of different ion channels. The chip has been validated by confirming the presence of autoantibodies in patients with anti-NMDA receptor encephalitis. Such a chip will be ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Transglutaminase activity as a possible therapeutical target in neurodegenerative diseases.
Authors: Iannaccone M, Titta F, Serretiello E, De Vivo G, Martin A, 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 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,...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Patents on brain permeable nanoparticles.
Authors: Gulati M, Chopra DS, Singh SK, Saluja V, Pathak P, Bansal P 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 ba...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions.
Authors: De Petrocellis L, Moriello AS 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 ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Cerebrovascular ultrasonography for selecting patients for stroke intervention.
Authors: Sharma VK, Yohanna K, Kawnayn G, Sarkar N, Batra A 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 diagnost...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Recent advances in the treatment of neurogenic erectile dysfunction.
Authors: Calabro RS, Polimeni G, Bramanti P Abstract Neurogenic erectile dysfunction (ED) can be broadly defined as an inability to sustain or maintain a penile erection owing to a neurological impairment, either centrally or peripherally or both. Although significant advances in the pharmacological treatment of ED have occurred in recent years, especially after the introduction of oral selective phosphodiesterase type 5 inhibitor, the treatment of neurological patients with ED may be challenging for prescribers, given poor data available on this topic and the variety of etiologic factors (iatrogenic, endo...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Therapeutic potential of cannabinoids in schizophrenia.
Authors: Kucerova J, Tabiova K, Drago F, Micale V Abstract Increasing evidence suggests a close relationship between the endocannabinoid system and schizophrenia. The endocannabinoid system comprises of two G protein-coupled receptors (the cannabinoid receptors 1 and 2 [CB1 and CB2] for marijuana's psychoactive principle Δ(9)-tetrahydrocannabinol), their endogenous small lipid ligands (namely anandamide [AEA] and 2-arachidonoylglycerol [2-AG], also known as endocannabinoids), and proteins for endocannabinoid biosynthesis and degradation. It has been suggested to be a pro-homeostatic and pleiotropic signal...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Migraine attack treatment : a tailor-made suit, not one size fits all.
We present an update on the treatment of the migraine attack. PMID: 24605940 [PubMed - in process] (Source: Recent Patents on CNS Drug Discovery)
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Antisense oligonucleotides in the treatment of cerebral gliomas. Review of concerning patents.
Authors: Caruso G, Caffo M Abstract Gliomas are the most common and malignant primary brain tumors in the adult population. Despite the intensive research on cancer pathology, real mechanisms concerning glioma progression are not completely understood. The prognosis in patients affected by malignant gliomas is still very unfavorable. Recent genomic analyses have revealed patterns of molecular changes within tumor subclasses that harbor distinct underlying biology, clinical prognosis, and pathogenic routes. So, novel treatments will have to be able to interfere at different molecular levels in gliomagenesis...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Treatment of insulin resistance in the neurodegeneration.
Authors: Stefanelli M, Martocchia A, De Marinis EA, Falaschi GM, Romano G, Rufo M, Falaschi P Abstract The association between diabetes and neurodegenerative diseases is increasing with aging. Several common mechanisms are involved in both these diseases. The endothelial cells of the blood brain barrier, neurons and glia express typical and different receptors of the glucose metabolism (glucose transporters, insulin receptors and glucagon-like peptide-1 receptors). The impairment in insulin signaling leads to an impairment of neuronal function and increases neurodegeneration, and, conversely, neurodegenera...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

This first 2014 issue of Recent Patents in CNS Drug Discovery covers a range of rather diverse, but not necessarily unrelated topics. Introduction.
Authors: Marzo VD PMID: 24805823 [PubMed - in process] (Source: Recent Patents on CNS Drug Discovery)
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Recent Patents on Novel MCH1 Receptor Antagonists as Potential Anti-Obesity Drugs.
Authors: Szalai KK, Beke G, Eles J, Kitka T, Nagy J, Farkas S, Boros A Abstract Today, the "obesity pandemic" is one of the biggest health issues around the world. As hypothalamic neuropeptide melanin-concentrating hormone (MCH) is one of the most potent central stimulators of feeding, regulating energy balance, inhibition of its receptor, melanin concentrating hormone receptor-1 (MCHR1), has attracted considerable attention during the last decade. There are is now a great selection of known MCHR1 antagonists that provide clues to for the development of new structures with high potency and good pharmacokin...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Possible Physiopathological Roles of the Transglutaminase Activity in the Etiopathogenesis of Human Neurodegenerative Diseases.
Authors: Titta F, Iannaccone M, Martin A, 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 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 the 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