Patent landscape for discovery of promising acyltransferase DGAT and MGAT inhibitors.
Expert Opin Ther Pat
; 30(11): 873-896, 2020 Nov.
Article
em En
| MEDLINE
| ID: mdl-32878484
ABSTRACT
INTRODUCTION:
DGAT and MGAT enzymes play an important role in triacylglycerol (TGA) biosynthesis. Overexpression of these enzymes may lead to accumulation of TGA in adipose tissues causing development of diseases such as obesity and diabetes. High triglyceride levels increase risk factors for atherosclerosis, and increase the risk of heart attack, stroke and other heart diseases. DGAT and MGAT inhibitors are used for the treatment of such metabolic diseases. A number of DGAT and MGAT inhibitors entered into clinical and preclinical stages. However, some adverse effects are associated with them. Thus there is need to develop new, potent and safe DGAT and MGAT inhibitors. AREA COVERED In this review, the authors carefully searched patent literature and reviewed recent advances since the year 2014. Diverse chemical classes reported in the patents belonging to the category DGAT and MGAT inhibitors have been highlighted. EXPERT OPINION DGAT and MGAT inhibitors are now gaining significant importance in the treatment of metabolic diseases. Fused heterocycles with a combination of aromatic and aliphatic hydrophobic substituents could offer more potent DGAT and MGAT inhibitors. Previously reported chemical scaffolds and their DGAT and MGAT inhibitory activity could be employed as an input for some in silico studies to discover novel, potent and safe DGAT and MGAT inhibitors.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Aciltransferases
/
Inibidores Enzimáticos
/
Diacilglicerol O-Aciltransferase
Tipo de estudo:
Prognostic_studies
/
Risk_factors_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Expert Opin Ther Pat
Assunto da revista:
TERAPEUTICA
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
Índia