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Bcl-2-Specific Inhibitor (GDC-0199)

Bcl-2 is overexpressed in several hematologic malignancies, including non-Hodgkin’s lymphoma.1,2

GA101
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Bcl-2 acts as a key regulator of the intrinsic apoptotic signaling pathway by sequestering and neutralizing pro-apoptotic molecules, such as Bax.3 Thus, the anti-apoptotic protein promotes B-cell survival by inhibiting apoptosis, which may result in oncogenic chemotherapy resistance in hematologic malignancies.

GDC-0199 is a small-molecule inhibitor being developed in collaboration with Abbott Laboratories. GDC-0199 is designed to bind to and inhibit the function of Bcl-2 specifically, which may lead to cancer cell apoptosis.1

  1. Apoptosis is often evaded in hematologic malignancies via overexpression of anti-apoptotic protein Bcl-2 and dysregulation of pro-apoptotic proteins.2 Bcl-2 regulates pro-apoptotic proteins to prevent apoptosis mediated by the intrinsic pathway.3

    Bcl-2 Vignette 1
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  2. GDC-0199 is a small-molecule inhibitor designed to inhibit the function of Bcl-2 specifically, which may restore the ability of the intrinsic apoptotic pathway to respond to apoptotic stimuli.1

    Bcl-2 Vignette 2
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  3. GDC-0199 is a small-molecule inhibitor designed to bind and inhibit the function of Bcl-2 specifically, which may restore the ability of the intrinsic apoptotic pathway to respond to apoptotic stimuli.2

References:
1.
Jin Z., El-Deiry, WS. Overview of cell death signaling pathways. Cancer Biol Ther. 2005;4:139-163.
2.
Reed, JC. Bcl-2 family proteins and hematologic malignancies: history and future prospects. Blood. 2008;111:3322-3300.
3.
Lessene G, Cazbolar PE, Coleman PM. BLC-2 family antagonists for cancer therapy. Nat Rev Drug Disc. 2008;7:989-1000.