Transcription factors (TFs) play a coordinated role in cells, directing the cell's life cycle and various responses. Based on customer requirements, CD BioSciences provides comprehensive peptidomimetics development services targeting TFs.
Introduction to Transcription Factors
Transcription factors are a class of protein molecules that specifically bind to a specific sequence of a gene, thereby controlling the expression of a target gene at a specific time and space with a specific intensity.
As an important part of gene expression regulation, TFs are widely involved in physiological and pathological processes in vivo. It is estimated that there are at least 1600 transcription factors in the human genome, of which about 19% are closely related to various diseases, including cancer, autoimmune diseases, diabetes, cardiovascular diseases, etc.
Fig. 1 Anatomy of a TF. (Henley M J & Koehler A N, 2021)
- Advantages for Targeting TFs
In view of the direct regulation effect of TFs on target genes, they have higher specific disease regulation ability than upstream signaling proteins such as kinases and GPCRs, and can avoid the side effects caused by crosstalk of signaling pathways.
- Dysregulated Transcription in Diseases
As the basic driver of selective gene expression, TFs is closely related to transcriptional dysregulation, which is an important cause of various diseases, so TFs are regarded as popular targets for disease research.
Table 1 Selected examples of TFs that drive disease. (Henley M J & Koehler A N, 2021)
| Classification of diseases |
TF |
Associated diseases |
Dysregulation mechanisms |
| Cancer |
MYC |
Various forms of cancer |
Amplifies oncogenic transcriptional programs |
| MYB |
Various forms of cancer |
Overactivation by gene duplication, overexpression and genetic fusions to other proteins |
| E2F |
Various forms of cancer |
Overactivation by dysregulation of co-repressor pRB |
| TAL1 |
T cell acute lymphoblastic Leukaemia |
Overexpression and overactivation |
| PAX3-FOXO1 |
Alveolar rhabdomyosarcoma |
Oncogenic fusion TF, dysregulates muscle development transcriptional programs |
| p53 |
Various forms of cancer |
Downregulation by the ubiquitin–proteasome system or loss-of-function mutations |
| Autoimmune and inflammatory disease |
STAT1 |
Atherosclerosis, infection |
Overactivation by signalling pathways |
| STAT3 |
Various forms of autoimmune and inflammatory disease, as well as cancer and diabetes |
Gain-of-function mutations and/or overactivation by signalling pathways (cancer, autoimmune disease), or loss-of-function mutations (hyper IgE syndrome) |
| STAT6 |
Asthma and allergy |
Overactivation by signalling pathways |
| T-bet |
Multiple sclerosis, systematic |
lupus erythematosus TH1 cell master TF, drives and/or increases severity of autoimmunity |
| GATA3 |
Atopic asthma, allergies |
TH2 cell master TF, drives and/or increases severity of autoimmunity |
| Diabetes |
HNF1α |
Maturity-onset diabetes of the young |
Loss-of-function mutation |
| HNF4α |
Maturity-onset diabetes of the young |
Loss-of-function mutation |
| NEUROD1 |
Maturity-onset diabetes of the young |
Loss-of-function mutation |
| Cardiovascular disease |
GATA4 |
Maladaptive cardiac hypertrophy, congenital heart disease |
Overactivation (cardiac hypertrophy) or loss-of-function mutation (congenital heart disease) |
| Nkx2-5 |
Congenital heart disease |
Loss-of-function mutation |
| Tbx5 |
Congenital heart disease |
Loss-of-function mutation |
Our Services
CD BioSciences uses the high-throughput peptidomimetic development platform PepDomTM to provide global customers with peptidomimetic development services targeting various transcription factors. Our targeting is not limited to common transcription factors, and customers can leverage our platform to further develop on difficult-to-drug transcription factors.
- The unique advantage of our technology is that the developed peptidomimetics have higher stability, stronger targeting and biosolubility than traditional peptide drugs.
- Based on the advanced PepDomTM platform, we also provide Peptidomimetic Modification Service, Drug Screening Service, Diagnostic Reagents Development Service, etc.
Features of Our Service
We are committed to providing the best service to our customers around the world!
Rapid Turnaround
Industrial Leadership
Customer First
Cost Efficient
CD Biosciences focuses on the development of peptidomimetics related to transcription factors. As long as you provide the target you are interested in, our professional team will solve it for you immediately. Welcome to contact us for the best solution.
Reference
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Henley, M. J., & Koehler, A. N. (2021). Advances in targeting 'undruggable' transcription factors with small molecules. Nature Reviews Drug Discovery. 20, 669–688.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.
