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Allosteric in Medical News

Migraine prevention by targeting glutamate receptors?

...erican Academy of Neurology in Seattle (April 25 May 2), Addex Pharmaceuticals (SIX: ADXN) will present Phase IIa data on ADX10059, a negative mGluR5 allosteric modulator, which shows efficacy in treating acute migraine attacks and provides evidence that inhibition of this glutamate receptor subtype could play...

Evotec Reports Positive Top-Line Results in Phase II Study With EVT 201 in Elderly Insomniacs With Daytime Sleepiness

...ine Withdrawal Questionnaire. About EVT 201 EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex. Acting on GABAA receptors i...c has three programmes in clinical development: EVT 201, a partial positive allosteric modulator (pPAM) of the GABAA receptor complex for the treatment of insomni...
Allosteric in Medical Technology

deCODE Files IND for DG071, a Novel PDE4 Modulator Being Developed for Alzheimer's and Other Cognitive Disorders

...ures allowed the deCODE chemistry team to identify a novel binding site for allosteric modulators in the PDE4 regulatory domain. Binding of an allosteric modulator at that site is non-competitive with cAMP. DG071 has been shown i...

Genaera Corporation Presents Data on Mechanism of Inhibition of PTP-1B for Trodusquemine (MSI-1436) at Federation of American Societies for Experimental Biology (FASEB) Meeting

..., Colorado. The poster presentation entitled, "Trodusquemine (MSI-1436), An allosteric Inhibitor of Protein Tyrosine Phosphatase 1B," concluded that MSI-1436 is a...noncompetitive inhibitor of PTP-1B in clinical stage development. It is the allosteric nature of MSI-1436 and its ability to reversibly inhibit PTP-1B that is bel...

Xytis Names Gordon H. Busenbark as Chief Financial Officer

...siderable partnering interest in two of our pre-clinical programs; positive allosteric modulators of GABA-A receptor and of alpha-7 nicotinic acetylcholine recept...folio of proprietary preclinical compounds that are novel, highly selective allosteric modulators of nicotinic acetylcholine receptors (nAChRs), GABA-A receptors ...

Addex Achieves Statistically Significant Outcome in Phase IIa Clinical Trial With ADX10059 in Gastro-Esophageal Reflux Disease

...iabetes type 2. Addex's competence in drug development and its expertise in allosteric modulation were recognised through the establishment of a partnership for co-development of mGluR2 positive allosteric modulators for anxiety and schizophrenia with Johnson & Johnson in 2004...

Addex Reports Positive Results in Phase IIa Clinical Trial With ADX10059 in Migraine

...g a Phase IIa study in anxiety. ADX10059 is a potent, selective, negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5 NAM). Various pre-cl...nson's disease. Addex's competence in drug development and its expertise in allosteric modulation were recognised in a collaboration established in 2004 with Orth...

Genelabs Technologies Announces Presentation of Data on Non-Nucleoside HCV Polymerase Inhibitor at 20th International Conference on Antiviral Research Meeting

...Genelabs. The oral presentation was given by Christopher D. Roberts, Ph.D., Director of Medicinal Chemistry at Genelabs, entitled "GL59728: A Potent allosteric Inhibitor of the HCV NS5b RNA Dependent RNA Polymerase with Excellent Pharmacokinetic Properties." GL59728 is one of a number of non-nucleoside HCV ...

Evotec Reports Positive Proof-of-Concept Top-Line Results with Insomnia Drug Candidate EVT 201

...y positive top-line results from its first phase II clinical trial of EVT 201 in patients with chronic primary insomnia. EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex. The double-blinded, placebo controlled cross-over study design of two doses of EVT 201 (1.5mg and 2.5m...

Newly Published Data Demonstrates Superiority of Cipralex Over Duloxetine for Acute Treatment of Depression

...f patients with major depressive disorder (MDD) and was at least as efficacious in long-term treatment(1). The study directly compared Cipralex(R) (an allosteric serotonin reuptake inhibitor - ASRI) to duloxetine (the most recently introduced serotonin and noradrenaline reuptake inhibitor - SNRI) and these find...

Evotec AG (DE) - Evotec Reports Positive Proof-of-Concept Top-Line Results with ...

...y positive top-line results from its first phase II clinical trial of EVT 201 in patients with chronic primary insomnia. EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex. The double-blinded, placebo controlled cross-over study design of two doses of EVT 201 (1.5mg and 2.5m...

MGI Pharma, Inc. Summarizes Data Presented at the 2007 American Society of Clinical Oncology (ASCO) Annual Meeting

...and granisetron, were reported. Competitive versus allosteric interactions between these agents and the 5-HT(3) ...emonstrated dual action suggesting competitive and allosteric interactions with the 5-HT3 receptor. In contrast,...hibited strictly competitive antagonism. The Aloxi allosteric interaction with the 5-HT3 receptor indicates that...
Allosteric in Biological News

Uncooperative voltage sensors

... by Gagnon and Bezanilla, in addition to other recent complementary techniques, "promises to unmask some of the previously inscrutable features of the allosteric communication among entwined Kv subunits and between the homologous domains of sodium channels." ...
Allosteric in Biological Technology

InterMune to Present Abstracts on HCV Protease Inhibitor ITMN-191 and HCV Development Program at the EASL Meeting

...dditional InterMune posters to be presented at EASL are as follows: Combination of the NS3/4A Protease Inhibitor ITMN-191 with the allosteric NS5B Polymerase Inhibitor ITMN-8020 Enhances Replicon Clearance and Reduces the Emergence of Drug Resistant Variants . Discovery of Potent,...

deCODE genetics Announces Third Quarter 2008 Financial Results

...s been to discover compounds that would modulate PDE4 activity via an allosteric mechanism to improve safety and tolerability. Towards this goal, the dec...s allowed the deCODE chemistry team to identify a novel binding site for allosteric modulators in the PDE4 regulatory domain. In animal models, DG071 has be...

Evotec AG: R&D Update on 16 October 2007 Live on the Internet

...in finding new treatments for diseases of the Central Nervous System. Evotec has three programmes in clinical development: EVT 201, a partial positive allosteric modulator (pPAM) of the GABAA receptor complex for the treatment of insomnia, EVT 101, a subtype selective NMDA receptor antagonist for the treatment ...

Evotec to Present at the UBS 2007 Global Life Sciences Conference in New York

...in finding new treatments for diseases of the Central Nervous System. Evotec has three programmes in clinical development: EVT 201, a partial positive allosteric modulator (pPAM) of the GABAA receptor complex for the treatment of insomnia, EVT 101, a subtype selective NMDA receptor antagonist for the treatment ...

Evotec Reports Details of the Positive Proof-of-Concept Phase II Study in Insomnia With EVT 201

...ive Director of the Sleep Medicine and Research Center, St John's Mercy Medical Center, Chesterfield, Missouri, US, said: "Due to its partial positive allosteric modulation of GABAA receptors, EVT 201 provides a novel approach to the treatment of insomnia, yet since the GABAA system is a well understood pathway...

Evotec to Present Details of the Positive Phase II Study in Insomnia With EVT 201 at the Worldsleep07 Congress in Cairns/Australia

...ed by current treatments, there is no drug yet available which meets all the needs of insomnia patients. About EVT 201 EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex. Acting on GABAA receptors it addresses the gold standard mechanism for insomnia with more than 90% of ...

Preparative Nondenaturing Gel Electrophoresis to Purify NADP-Specific Glutamate Dehydrogenase From Chlorella, Rev B

...mes are nearly identical; however, kinetic characterization of the enzymes showed them to have strikingly different K m values, allosteric properties, and turnover rates (Bascomb and Schmidt 1987). Recent molecular genetic analysis indicates that minor modifications in ...
Allosteric in Biological Products

PTP1B Inhibitor from Calbiochem

Description:...ECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable sulfanamido-benzbromarone compound that acts as a selective, reversible and non-competitive allosteric inhibitor of PTP1B (IC 50 = 4 μM and 8 μM for PTP1B 403 and PTP1B 298 , respectively). Binds to a novel site away from the catalytic pocket an...
Company:Calbiochem
Allosteric in Biological Definition

Active site

...inds to the active site but cannot be processed by the enzyme. In noncompetitive inhibition , the inhibitor binds to the enzyme at another site, the allosteric site , and this causes a structural change in the enzyme such that the active site is rendered useless. Uncompetitive inhibition , is similar to nonco...

Allostery

... biochemistry , an enzyme or other protein is allosteric if its activity or efficiency changes in response...inding of an effector molecule at a so-called allosteric site . Changes that enhance activity are referred to as allosteric activation , while the opposite is called ...

Allostery

... biochemistry , an enzyme or other protein is allosteric if its activity or efficiency changes in response...inding of an effector molecule at a so-called allosteric site . Changes that enhance activity are referred to as allosteric activation , while the opposite is called ...

Insulin

...ubstances, most prominently glucose increase of DNA replication and protein synthesis modification of the activity of numerous enzymes ( allosteric effect ) The actions of insulin on cells include: increased glycogen synthesis – insulin forces storage of glucose in liver (and musc...

Lac repressor

...lactose is present the lac repressor hooks up to lactose and changes shape and detaches from the DNA. The technical term for this shape-shifting is " allosteric signal transduction ". See also Lac operon ...

Protein

...refore depend on controlling protein activity. Regulation can involve a protein's shape or concentration . Some forms of regulation include: allosteric modulation : When the binding of a ligand at one site on a protein affects the binding of ligand at another site. Covalent modulation : When t...
Allosteric in Biological Dictionary

Allostery

... In biochemistry, allosteric regulation is the regulation of an enzyme or oth...nding an effector molecule at the protein's allosteric site . Effectors that enhance the protein's activity are referred to as allosteric activators, whereas those that decrease... ...

Allosteric site

... In biochemistry, allosteric regulation is the regulation of an enzyme or ot...nding an effector molecule at the protein's allosteric site . Effectors that enhance the protein's activity are referred to as allosteric activators, whereas those that decrease... Asp...
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