NASH Target Development Service for LOXL2 Inhibitors

Inhibitors have played an important role in a number of disease treatments, especially in fibrotic disease therapy. As a service provider in drug development, Creative Biolabs is dedicating to offering a wide spectrum of LOXL2 inhibitors services to illustrate inhibitor bioactivity and mechanism of action. We have experienced experts and advanced platforms that are able to provide excellent services on LOXL2 inhibitors.

Introduction of LOXL2

LOXL2, also known as lysyl oxidase-like protein 2, belongs to lysyl oxidase protein family. It is a protein that plays an important role in producing the connective tissue, encoding the extracellular copper-based amine oxidases, as well as forming the crosslinks of collagens. Meanwhile, the C-terminus of LOXL2 is essential to the catalytic activity of amine oxidase, and N-terminus has been proved to be critical to regulating the cell growth, aging and tumor suppression. Pilot studies have demonstrated that LOXL2 is associated with a wide variety of diseases, such as certain cancers and fibrosis. LOXL2 can promote tumor progression and metastasis by changing the structure of histones of normal cells. It is often related to the poor prognosis in patients of tumors, suggesting it should be a potential target for cancer treatment. Furthermore, several antibodies have been generated to restrict the activity of LOXL2 in a number of disease models including NASH, which have shown that LOXL2 inhibitors are attractive tools for disease therapies.

Fig.1 Schematic diagram of the role of lysyl oxidase-like protein-2 (LOXL2) in liver disease and potential therapeutic use in different aetiologies. (Magdaleno, 2017)

Our Services for LOXL2 Inhibitors

Recent researchers have illustrated that LOXL2 inhibitors could be a promising tool for a range of fibrotic diseases treatment, such as idiopathic pulmonary fibrosis (IPF), NASH, liver fibrosis, and heart fibrosis. The small molecule inhibitor is one of the most common inhibitors that has been developed and widely used in a series of preclinical trials and the early phase of clinical trials. For instance, a LOXL2 inhibitor (simtuzumab) has been discovered and applied to the treatment of several cancers, liver, kidney and heart fibrosis. Currently, Creative Biolabs has established a panel of platforms to provide a comprehensive service on LOXL2 inhibitors design and modification as well as the safety evaluation. In addition, we also offer services of analyzing the expression level of LOXL2 in a series of tissues, and studying the safety and PK/PD profile of LOXL2 inhibitors in different types of animal models, hope to find the new candidates in the treatment of NASH.

Fig.2 Targeting LOXL2 with a therapeutic antibody suppresses the progression of biliary fibrosis in BALB/c.Mdr2−/− mice. (Ikenaga, 2017)

Creative Biolabs is a leading global CRO company which is dedicated to helping our worldwide customers shorten the discovery and development time in dug exploitation. Additionally, experienced experts in Creative Biolabs are also specialized in designing and performing high-quality custom assays, with different formats, endpoints, parameters, to satisfy any specific requirement at a most competitive price. For more detailed information, please feel free to contact us or directly sent us an inquiry.

References

1. Magdaleno, F.; et al. Selective LOXL2 inhibition: potent antifibrotic effects in ongoing fibrosis and fibrosis regression. Gut. 2017, 66(9): 1540-1541.
2. Ikenaga, N.; et al. Selective targeting of lysyl oxidase-like 2 (LOXL2) suppresses hepatic fibrosis progression and accelerates its reversal. Gut. 2017, 66(9): 1697-1708.