PROTAC

The products from CD Bioparticles include specialized delivery techniques, PROTAC, exact drug design and modification, and cutting-edge technology platforms that can help you with:

Figure 1. Functional mechanism of PROTACs.

The challenges you might meet:

• Drug resistance of traditional small molecule drugs due to target protein mutations or adaptive changes;
• Some targets are not druggable due to lack of binding pockets suitable for small molecule inhibitors;
• The development of drugs cannot precisely target the disease-causing protein, and brings large side effects;
• Less potent traditional small molecule inhibitors;
• Disrupting protein-protein interactions using small molecules is challenging due to the large and flat surfaces involved.
• Some drugs have poor pharmacokinetic properties;
• Combination therapy with multiple therapeutic approaches is required.

PROTAC Key features:

• Ligands for Target Protein for PROTAC
• PROTAC Linkers

PROTAC Key benefits:

Drug resistance: PROTACs can target disease-causing proteins that are difficult to inhibit with traditional small molecule drugs. By promoting protein degradation, PROTACs can overcome drug resistance mechanisms that develop due to mutations or adaptive changes in the target protein.

Undruggable targets: Many disease-associated proteins are considered "undruggable" because they lack suitable binding pockets for small molecule inhibitors. PROTACs can bypass this limitation by targeting the protein for degradation, regardless of its druggability.

Selectivity: PROTACs can achieve high selectivity by exploiting the cellular machinery responsible for protein degradation. This enables precise targeting of disease-causing proteins while minimizing off-target effects on other cellular proteins.

Improved potency: PROTACs often exhibit higher potency than traditional small molecule inhibitors. By continuously removing the target protein through degradation, PROTACs can achieve a sustained reduction in protein levels, leading to enhanced therapeutic efficacy.

Tackling protein-protein interactions (PPIs): PPIs are challenging to disrupt using small molecules due to the large, flat surfaces involved. PROTACs can selectively recruit E3 ubiquitin ligases to the protein complex, leading to ubiquitination and degradation of the target protein, thereby disrupting the PPI.

Overcoming drug pharmacokinetic limitations: Some drugs suffer from poor pharmacokinetic properties, such as low bioavailability or rapid clearance. PROTACs can potentially enhance drug-like properties by facilitating intracellular delivery and extending the half-life of the target protein through continuous degradation.

Combination therapies: PROTACs can be employed in combination with existing drugs to enhance therapeutic outcomes. By targeting specific proteins for degradation, PROTACs can synergize with other drugs, leading to improved efficacy and overcoming drug resistance.

PROTAC Application candidates:

• Cancer treatment: Targeting and destroying particular proteins linked to the initiation and progression of cancer has shown promise for PROTACs. To target and degrade proteins like the androgen receptor (AR) in prostate cancer, the estrogen receptor (ER) in breast cancer, and the BCR-ABL in chronic myeloid leukemia, for instance, PROTACs have been designed.
• Neurodegenerative diseases: Targeting disease-associated proteins involved in neurodegenerative disorders may be made possible by PROTACs. For instance, studies into PROTACs ability to breakdown proteins like tau and alpha-synuclein, which are linked to Alzheimer's and Parkinson's illnesses, respectively, are currently underway.
• Immunology and autoimmune disorders: By focusing on and selectively destroying particular immune regulation-related proteins, PROTACs have the ability to modify immune responses. This method might be investigated for the treatment of autoimmune diseases like inflammatory bowel disease or rheumatoid arthritis.
• Infectious diseases: To target and degrade proteins required for the survival and reproduction of infectious organisms, PROTAC technology may be used. By breaking down these proteins, PROTACs may thwart the spread of infection and open a new door for antiviral or antibacterial treatments.

Protein misfolding diseases: Misfolded protein buildup is a hallmark of some illnesses, including amyloidosis and cystic fibrosis. PROTACs may aid in the breakdown of these aberrant proteins, providing a therapeutic approach to deal with the situation.