Fatty acid binding protein (FABP) inhibitors: a patent review (2012-2015)

ABSTRACT

Introduction: Obesity, diabetes, atherosclerosis, hypertension, dyslipidemia, and metabolic syndrome are synergistically operating diseases that endanger human health. Many studies provide evidence for excessive free fatty acid (FFA) as the pathogenic factor of these diseases. Fatty acid binding proteins (FABPs), which are responsible for the transfer of FFA to different cell compartments, play a key role in cellular functions. Therefore, the discovery and application of FABP inhibitors may be a potential strategy to control obesity, atherosclerosis, diabetes, and metabolic syndrome diseases in humans.

Areas covered: This review focuses on the applications of FABP inhibitors in the prevention and treatment of obesity, atherosclerosis, diabetes, and metabolic syndromes. A comprehensive description of patents related to FABP inhibitors from 2012 to 2015 is included.

Expert opinion: FABP has proven to be a promising target for the treatment of obesity, atherosclerosis, diabetes, and metabolic syndrome, and there have been major advances in the development of FABP inhibitors for this purpose. However, there continue to be new claims for novel FABP inhibitors with higher activity and specificity. Moreover, FABP inhibitors are potential drugs for other applications involving anti-cancer and neurological regulatory functions.

KEYWORDS:

• Obesity
• atherosclerosis
• diabetes
• insulin resistance
• metabolic syndrome
• FABP
• inhibitors
• target

Article highlights

• Obesity, diabetes, atherosclerosis, hypertension, dyslipidemia and metabolic syndrome have all become serious diseases worldwide. One disease could probably cause one or more of the other diseases in this group. Novel drugs used for treating these diseases are urgently needed.

• FABP plays an essential role in the transfer of FFA, which is the pathogenic factor of these diseases. Therefore, FABP has currently become a new target for the design of novel drugs for obesity, atherosclerosis, diabetes and metabolic syndrome.

• Many kinds of FABP inhibitors have been reported in patent applications. They can be categorized into different classes according to their structures.

• These FABP inhibitors could possibly be novel effective drugs for obesity, atherosclerosis, diabetes and metabolic syndrome.

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Declaration of interest

This work was supported by the Projects (Nos. CXY1409 & CG1305) from the Science & Technology Bureau of Lianyungang City of Jiangsu Province. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.