Recent advances in stearoyl-CoA desaturase 1 inhibitors for dyslipidemia and obesity. 2010

Gang Liu
Ambit Biosciences, 4215 Sorrento Valley Blvd., San Diego, CA 92121, USA. gliu@ambitbio.com

SCD1 is a novel target for the treatment of dyslipidemia, obesity, and other symptoms of metabolic syndrome. Extensive target validation has been obtained using SCD1-deficient mice, anti-sense oligonucleotide and RNA interference-mediated knockdown of SCD1, and has supported a controlling role for SCD1 in regulation of lipid biosynthesis and energy expenditure. In this review, the recent advances in small-molecule SCD1 inhibitors will be summarized. The pharmacological and adverse effects of SCD1 inhibitors in relevant rodent models will also be reviewed. The future prospect of SCD1 inhibition in the treatment of metabolic diseases will be discussed.

UI MeSH Term Description Entries
D008659 Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed) Thesaurismosis,Diseases, Metabolic,Disease, Metabolic,Metabolic Disease,Thesaurismoses
D009765 Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013230 Stearoyl-CoA Desaturase An enzyme that catalyzes the formation of oleoyl-CoA, A, and water from stearoyl-CoA, AH2, and oxygen where AH2 is an unspecified hydrogen donor. Stearyl-CoA Desaturase,Stearate Desaturase,delta-9 Desaturase,Desaturase, Stearate,Desaturase, Stearoyl-CoA,Desaturase, Stearyl-CoA,Desaturase, delta-9,Stearoyl CoA Desaturase,Stearyl CoA Desaturase,delta 9 Desaturase
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D050171 Dyslipidemias Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL. Dyslipoproteinemias,Dyslipidemia,Dyslipoproteinemia
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

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