PROTACs for Breast Cancer

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As a leading provider of contract research services, BOC Sciences is committed to providing the one-stop services for PROTAC molecule drug discovery. We are constantly expanding my vision and capabilities to meet our customers' new drug discovery goals. With the comprehensive and advanced platform, we help our customers develop innovative and effective PROTAC molecules for breast cancer. The service portfolio covers the entire process of PROTAC development.

Introduction

Breast cancer is the second most common and the most occurring type of cancer among women, except for skin cancers. Breast cancer is cancer that develops from breast tissue. Types of breast cancer include ductal carcinoma in situ, invasive ductal carcinoma, inflammatory breast cancer, and metastatic breast cancer. Breast cancer cells have receptors on their surface and in their cytoplasm and nucleus. Chemical messengers such as hormones bind to receptors, and this causes changes in the cell. Breast cancer cells may or may not have three important receptors: estrogen receptor (ER), progesterone receptor (PR), and HER2. There are currently three main groups of medications used for adjuvant breast cancer treatment: hormonal therapy, chemotherapy, and monoclonal antibodies.

Agents targeting proteins with enzymatic activity have shown positive results, such as small molecular inhibitors or antibodies against membrane receptors. Recently, degradation of targeted proteins using PROTACs has attracted industrial interest. PROTAC is a heterobifunctional molecule consisting of two different ligands joined by a linker, one of the ligands recruits target protein (warhead ligand), the other ligand is specific for a E3 ubiquitin ligase. PROTACs have shown strong potency compared with the small molecule inhibitor and antibody, some of them have reached the clinical phase, like those developed against the estrogen receptors in breast cancer.

PROTACs in Breast Cancer

Aberrant or increased expression of pathogenic proteins often results in the initiation of many diseases. The PROTAC technology utilizes the ubiquitin-proteasome system to achieve select degrade pathological proteins to treat disease. The estrogen receptor (ER) is a validated target for the treatment of breast cancer. In recent years, many research of PROTAC targeting ER have been reported. For example, ERD-308, a PROTAC containing small molecule ERα degrader, achieves nanomole DC50 values in breast cancer cell lines. Currently, two PROTAC drug development programs with indication for breast cancer are in the clinical phase: ARV-471 (phase 2) and AC682 (phase 1). Thus, PROTACs are considered to have a promising future in the treatment of breast cancer.

SNIPERs in Breast Cancer

Specific and nongenetic IAP-dependent protein erasers (SNIPERs) have been developed to induce ubiquitylation and proteasomal degradation of various target proteins. Similar to PROTAC, SNIPER consists of a protein-binding ligand, a linker, and an E3 ligase-binding ligand. SNIPER(ER)-87 and improved SNIPER(ER)s, SNIPER(ER)-110, have been reported reported to exhibit high binding affinities to IAPs and induce potent degradation of ERα protein.

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  • Indication-directed molecular development of PROTAC
  • High-quality one-stop service
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  • Experienced experts team and extensive expertise
  • Data analysis, detailed report with results and discussion
  • Short turn-around time and competitive price
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PROTACs for Breast Cancer

References:

  1. Hu, J., et al., Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER), J. Med. Chem. 2019, 62, 3, 1420-1442.
  2. Ohoka, N., et al., Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation, PROTEIN SYNTHESIS AND DEGRADATION, 2018, 293, P6776-6790.

* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

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