用于治疗阿尔茨海默氏症的可溶性γ分泌酶调节剂的优化-猫眼课题宝

用于治疗阿尔茨海默氏症的可溶性γ分泌酶调节剂的优化

批准号：

8287539

负责人：

Steven Lee Wagner

金额：

$25.53万

依托单位：

UNIVERSITY OF CALIFORNIA, SAN DIEGO

依托单位国家：

美国

项目类别：

财政年份：

2011

资助国家：

美国

项目状态：

已结题

起止时间：

2011-07-01 至 2016-06-30

来源：

https://reporter.nih.gov/project-details/8287539

关键词：

Acetylcholinesterase Inhibitors Acute Affect Age Alzheimer&apos s Disease Amino Acids Amyloid Amyloid beta-Protein Amyloid beta-Protein Precursor Animal Model Behavioral Bioavailable Biochemical Biological Testing Brain Brain region Caregivers Cerebrum Chemical Structure Chronic Clinical Development Diffuse Disease Disease Progression Dose Drug Formulations Elderly Family member Funding Goals Healthcare Systems Human In Vitro Investigational Drugs Lead Learning Left Mediating Memory Molecular Neurodegenerative Disorders Neurofibrillary Tangles Neurons Oral Administration Parents Pathogenesis Patients Peptides Pharmaceutical Chemistry Pharmacologic Substance Phase Plasma Preclinical Testing Process Prodrugs Production Property Proteolytic Processing Reagent Regimen Research Senile Plaques Series Site Societies Solubility Structure-Activity Relationship Testing Therapeutic Toxic effect Transgenic Animals Transgenic Mice Work aging population analog aqueous base gamma secretase improved meetings mouse model notch protein novel pre-clinical preclinical study prevent receptor secretase

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DESCRIPTION (provided by applicant): The broad goals of our project are to pharmacologically optimize, mechanistically characterize (in the most appropriate molecular, cellular and transgenic animal models) and complete the entire preclinical development (through IND filing) of a potent orally bioavailable therapeutic compound carefully selected from a novel series of recently discovered gamma-secretase modulators (GSMs) for the treatment of Alzheimer's disease (AD). AD is neurodegenerative disorder that affects regions of the brain associated with learning and memory. AD affects over 24 million people world-wide and is an enormous burden to society. The extent at which it will affect our aging population will continue to escalate. A recently discovered a series of aryl 2-aminothiazole gamma-secretase modulators (AGSMs) that are pharmaceutical-like small organic molecules that are able to lower Abeta42 production without measurably affecting -Secretase-mediated enzymatic processing of other known gamma-secretase substrates such as the Notch-1 receptor. This project will focus on the pharmacological optimization of a series of AGSMs with improved physicochemical properties known as SGSMs. If successful in a number of predictive preclinical studies, these molecules will undergo further IND-enabling preclinical development and ultimately be tested in humans.

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