Toxins/Payloads (Classification and function) of Innovative drugs

Apoptosis inducer (BCL XL inhibitor)

Overexpression of anti apoptotic Bcl-2 family members (including BCL XL) is one of the mechanisms for cancer cells to obtain apoptosis resistance. Drugs that block the BH3 binding domain on BCL XL can trigger cancer cell apoptosis.

Telanstadine and its analogues

Targeted spliceosome is a large ribonucleoprotein complex involved in mRNA processing, which provides a promising treatment option for targeted cancer therapy. Several natural products can inhibit RNA splicing by binding to different splice subunits. The most representative is thailanstatin A, which can bind to the SF3B subunit of spliceosome to prevent RNA splicing.

Amanita toxin

In the field of ADC technology, the use of transcription inhibitors similar to Amatoxins is a relatively new method. Nine naturally occurring amatoxin derivatives have the same skeleton structure. A macrocycle composed of eight L-configuration amino acids is partially connected between tryptophan and cysteine residues by sulfoxide. The three side chains of Amatoxins are hydroxylated, and the OH group has good water solubility and binds to the target molecule. Two peptides, α- Amanita glycoprotein and β- Amanita toxin accounts for 90% of all toxins.

Nicotinamide phosphoribosyltransferase

Nicotinamide phosphoribosyltransferase (Nampt) is an enzyme responsible for converting nicotinamide to nicotinamide mononucleotide. Its inhibitor has shown effectiveness in various preclinical and clinical studies, but its clinical application is limited by targeted toxicity and dose limiting toxicity, such as thrombocytopenia and gastrointestinal adverse reactions.

Camamycin

Two new protease inhibitors, camamycin A and camamycin B, were isolated from Curacao bacteria.

Product list

View the Knowledge base of Antibody-drug Conjugate (ADC):     - The Landscape of Antibody-drug Conjugate (ADC): Production, Mechanisms of Action (MOA), FDA approved-antibodies, and Functional assay     - What is antibody-drug conjugate (ADC)?     - Antibody-drug conjugate (ADC) in clinical application (Approved/BLA, phaseI/II/III)     - Main elements of antibody-drug conjugate (ADC)： Antibodies and their targets     - Main elements of antibody-drug conjugate (ADC)：Linker (cleavable/non-cleavable, structure and mechanism)     - Main elements of antibody-drug conjugate (ADC)：Toxins/Payloads (Classification and function)     - Toxins/Payloads (Classification and function) of Microtubule destroying drug     - Toxins/Payloads (Classification and function) of DNA damage drugs     - Toxins/Payloads (Classification and function) of Innovative drugs     - Biological coupling technology Chemical based specific in situ antibody modification     - Endogenous coupling of amino acids and Disulfide re bridging strategy     - Glycan coupling     - Site specific biological coupling of engineered antibodies and Enzymatic method     - Biological coupling with engineered unnatural amino acids     - Review for ADC production, quality control and functional assay     - Product data of ADC