More than 80 percent of the protein in human cells lacks enzyme activity or the drug site on the cell surface, leading to most small molecule drugs or monoclonal antibody agents can't do their job. While PROAC molecules can capture the targeting proteins and make them degraded and cleared. PROTACs research can not only be applied to classical drug targets such as the sexual hormone receptors or protein kinases, but also transcription factors, protein skeleton and so on.
BOC Sciences, a leading CRO company in the pharmaceutical industry, has established a comprehensive PROTAC molecular discovery platform. Our one-stop PROTAC services cover the entire lifecycle of drug discovery. In addition, we provide a variety of target proteins to assist our customers' new drug development, including:
- Cellular Metabolic Enzymes
- Neuro-degenerative Related Proteins
- Nuclear Receptors
- Protein in Transcriptional Regulation
- Protein Kinases
Cellular Metabolic Enzymes
Cellular metabolism is defined by a variety of complex biochemical reactions involving biomolecular synthesis (anabolism), maintenance, or decomposition (catabolism). The molecules involved in these metabolic processes include the basic building blocks of cells, such as lipids, amino acids and carbohydrates, as well as the metabolic enzymes involved in the reactions that drive cellular metabolism. While metabolic abnormality is one of the important features of tumor and other diseases. Tumor cells can not only adjust the classic function of metabolic enzymes to meet the needs of rapid proliferation. Meanwhile, it can also regulate a variety of complex cellular activities and the occurrence and development of diseases through the non-classical/non-metabolic (Moonlighting) function of metabolic enzymes.
Neuro-degenerative Related Proteins
Despite a wide variety of clinical manifestations and affected genes, many common neurodegenerative diseases share similar molecular mechanisms. Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), and prion disease are all characterized by mutated or misfolded proteins that aggregate into amyloid inclusion bodies. And aggregation would occur when the accumulation of misfolded proteins exceeds the ability of the ubiquitin-proteasome degradation pathway to eliminate them.
Nuclear Receptors
Nuclear receptors (NR) are a class of ligand-dependent transcription factors widely distributed in organisms. Nuclear receptors interact with corresponding ligands and their coregulatory factors to regulate the coordinated expression of genes, thus playing an important role in the physiological processes of growth and development, metabolism, cell differentiation and so on. Dysfunction of nuclear receptors can lead to a range of diseases. Nuclear receptors can regulate the development of diseases such as cancer, osteoporosis and diabetes by binding to small molecules designed by drug modified, which are promising drug design targets.
Protein in Transcriptional Regulation
The protein in transcriptional regulation, namely Transcription factors (TFs), are the most basic proteins involved in cell development, differentiation and maintenance of body balance. They drive the complex pattern of gene expression in cells at all stages of body development. And the deficiency of transcription factor signals may lead to the occurrence of developmental disorders and diseases.
Protein Kinases
Protein kinases are enzymes that phosphorylate one third of the proteins in the human proteome. Applications of protein kinases in drug therapy include tumors, inflammation, and neurodegenerative diseases. Because protein kinases are distributed in multiple signaling pathways of immune cells, drug development targeting protein kinases has great promise in the treatment of inflammatory diseases such as amyotrophic lateral sclerosis, rheumatoid arthritis and ulcerative colitis, as well as tissue damage.
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
