Gossypol acetic acid Bcl-2 inhibitor AT101 (AT-101) is a small-molecule inhibitor produced by Ascenta Therapeutics. It has been shown to have anti-tumor properties and is currently being investigated as a potential cancer treatment. The chemical name of AT-101 is (S)-(+)-2,2'-Bis(1-methyl-4-aminoisoquinoline) Acetic acid. Its molecular formula is C34H34N4O4, its formula weight is 570.67g/mol, and its CAS number is 866541-93-7.
Top Ten Keywords and Synonyms
According to a Google search for AT-101, these are the top ten keywords related to it: "cancer", "tumor", "Bcl-2", "apoptosis", "ovarian cancer", "prostate cancer", "breast cancer", "non-small cell lung cancer", "multiple myeloma", and "clinical trials".
Some of the Synonyms for AT-101 include R-(-)-gossypol acetic acid, Gossypol acetic acid (1:1) mixture with its (S)-(+)- isomer, (-)-Gossypol acetic acid, R-isomer, S-isomer, Ascenta-3, Ascenta-042580, and Ascenta-042574.
Health Benefits of AT-101
AT-101 is a promising anti-cancer agent that can induce apoptosis in tumor cells. It has been shown to have beneficial effects in the treatment of various types of cancer, including prostate cancer, ovarian cancer, breast cancer, non-small cell lung cancer, and multiple myeloma. AT-101 has also been shown to improve the efficacy of chemotherapy and radiation therapy, and it may prevent the development of drug resistance in cancer cells.
Potential Effects
AT-101 can selectively target the Bcl-2 family of proteins, which are overexpressed in many types of cancer cells and promote tumor cell survival by inhibiting apoptosis. By inhibiting these proteins, AT-101 can promote the activation of caspases and induce the apoptosis of cancer cells. AT-101 also possesses anti-angiogenic properties and can inhibit the growth of blood vessels that support the growth of tumors.
Product Mechanism
The molecular mechanism of AT-101 involves the inhibition of the anti-apoptotic Bcl-2 family of proteins. Bcl-2 proteins are involved in the regulation of apoptosis and their overexpression in cancer cells can inhibit apoptosis and promote tumor cell survival. AT-101 binds specifically to the BH3 domain of Bcl-2, Bcl-XL, and Mcl-1, and promotes their degradation by the proteasome. This process induces apoptosis and leads to the elimination of cancer cells.
Safety of AT-101
Studies of AT-101 have shown that it can be administered safely to cancer patients at doses that induce anti-cancer activity. AT-101 has been given safely to patients in clinical trials of advanced solid tumors, and the recommended dose ranges from 10 mg/d to 40 mg/d.
Side Effects
The side effects of AT-101 are generally mild, with the most common side effects being gastrointestinal disorders such as nausea, vomiting, and diarrhea. AT-101 may also cause fatigue, headache, and mild hematological abnormalities. However, the incidence of severe adverse events is low, and most patients tolerate treatment well.
Dosing Information
AT-101 is administered orally, and the recommended dose varies depending on the type of cancer being treated and the patient's condition. AT-101 is typically administered in cycles of several weeks, and the dosage may be adjusted based on the patient's response to treatment.
Conclusion
AT-101 has shown promising results as a potential cancer treatment with a good safety and tolerability profile. As a Bcl-2 inhibitor, it can selectively target tumor cells and induce apoptosis, leading to the elimination of cancer cells. The efficacy of AT-101 has been demonstrated in clinical trials in patients with various types of cancer. The ongoing research is expected to provide more insights and develop AT-101 into a novel anti-cancer agent with a broad range of clinical applications
