Corporate Banner
Satellite Banner
Scientific Community
Become a Member | Sign in
Home>News>This Article

Nimbus Discovery Presents Preclinical Data on Sought-After ACC Inhibitors

Published: Tuesday, January 29, 2013
Last Updated: Tuesday, January 29, 2013
Bookmark and Share
Company successfully discovered and optimized the first small molecule allosteric inhibitors of ACC achieving excellent potency, selectivity and drug-like properties within 12 months.

Nimbus Discovery LLC, a biotechnology company discovering novel medicines against exciting but previously inaccessible drug targets, will present preclinical data today at the Keystone Symposia Conference: Adipose Tissue Biology in Keystone, Colo., that show that the company has identified a series of novel, highly potent, and highly selective Acetyl CoA Carboxylase (ACC)1/2 allosteric inhibitors. Inhibition of ACC reduces fatty acid synthesis and stimulates fatty acid oxidation and has the potential to favorably affect the morbidity and mortality associated with obesity, diabetes, and fatty liver diseases.

Most efforts to discover ACC inhibitors have focused on interactions within the carboxyltransferase (CT) domain of the enzyme active center resulting in poor drug-like properties and have thus failed to provide benefit to patients. In contrast, Nimbus focused on the biotin carboxylase (BC) domain where the natural product soraphen interacts. Nimbus ACC allosteric inhibitors demonstrate excellent drug-like properties and show liver-muscle exposure that is aligned with driving outstanding pharmacology in preclinical models of disease.

Key findings of the Nimbus compounds presented at the conference include:

•    Development of this series of ACC inhibitors has yielded deep structure-activity relationships, sub-nanomolar enzyme inhibition, functional activity in cellular assays and favorable drug-like properties leading to in vivo proof of concept.
•    ND-630, the Nimbus lead compound, potently inhibits hepatic fatty acid synthesis (ED50 = 0.14 mg/kg) in a highly dose-dependent manner and stimulates whole body fatty acid oxidation (minimum effective dose 3 mg/kg) in preclinical models of disease.

“Using our state-of-the art structure-based drug design approach, Nimbus was able to identify potent small molecule ACC inhibitors, with excellent pharmaceutical properties, 12 months after hits were generated from an in silico screen. We believe that we are the first company to create drug-like allosteric inhibitors against ACC. The impressive potency and selectivity of our molecules could translate into significant safety and efficacy benefits in the clinic,” said Rosana Kapeller, M.D., Ph.D., Chief Scientific Officer of Nimbus. “We are now conducting a detailed pharmacological evaluation of this broad portfolio of potent allosteric inhibitors, including ND-630, and will provide an update on these data in metabolic disease, diabetes and cancer tumor metabolism models in the near future.”

Further Information

Join For Free

Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 3,500+ scientific posters on ePosters
  • More than 5,200+ scientific videos on LabTube
  • 35 community eNewsletters

Sign In

Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.

Scientific News
Salford Lung Study - The First Real World Clinical Trial
In this podcast, we learn about the Salford Lung Study and its potential to revolutionize the way we assess new drugs and treatments around the world.
Nanoparticles Offer Promising Platform for Flavivirus Treatment
New nanoparticle effectively vaccinated mice against one dengue strain and could be created to target all four.
First Entirely 3D-printed Organ-on-a-Chip with Integrated Sensors
New approach to manufacturing may allow researchers to rapidly design organs-on-chips that match the properties of a specific disease or individual patient's cells.
Study Finds Key Regulator in Pulmonary Fibrosis
Researchers identify an enzyme that could open the way to therpies for chronic fatal lung disease.
Signaling Pathway Could Be Key to Improved Osteoporosis Treatment
Inhibition of SIK2 enzyme both stimulates bone formation and reduces bone breakdown in animal model.
Ovarian Cancer Insight
Study showed tumours release cytokines to attract macrophages, which secrete growth factors that in turn promote tumour growth.
Substance Can Potentially Postpone Aging
Researchers bridge the gap between two main aging theories - repairs to the DNA and poor functioning mitochondria.
Untangling Cause Of Memory Loss In Neurodegenerative Diseases
NIH-funded mouse study identifies a possible therapeutic target for a family of disorders.
New Model for Understanding Human Myeloma
Researchers develop mouse model where mice carry six human genes involved in human tumour growth.
Preventing Alzheimer's in Mice
Researchers have prevented the Alzheimer’s development in mice by using a virus delivery system to transport a specific gene into the brain.

SELECTBIO Market Reports
Go to LabTube
Go to eposters
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
3,500+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
5,200+ scientific videos