PARP-2 Selective Inhibitor Development

Poly(ADP-ribose) polymerase 2 (PARP-2) is an enzyme that plays a vital role in cellular processes such as DNA repair, transcription regulation, and chromatin remodeling. At Alfa Cytology, we specialize in the development of selective PARP-2 inhibitors, leveraging our extensive expertise in medicinal chemistry and preclinical research.

Introduction to PARP-2 Selective Inhibitor

Unlike its more well-known counterpart, PARP-1, which is predominantly associated with DNA damage response, PARP-2 has emerged as a key player in androgen receptor (AR) signaling, particularly in prostate cancer (PCa). Recent studies have shown that selective inhibition of PARP-2 can disrupt AR-mediated transcription and inhibit the growth of AR-positive prostate cancer cells, presenting a promising therapeutic approach.

Fig. 1 Principles of selective targeting of PARP-2 to attenuate AR signaling and inhibit prostate cancer growth. (Gui B., et al. 2019)

The mechanism by which PARP-2 influences AR activity involves its interaction with the pioneer factor FOXA1. This interaction facilitates the recruitment of the AR to prostate-specific enhancer regions, thereby enhancing AR-mediated gene expression. Elevated levels of PARP-2 have been observed in primary PCa tumors. This overexpression correlates with tumor aggressiveness and poor clinical outcomes, making PARP-2 a compelling target for selective inhibition.

PARP-2 Selective Inhibitor Development

Inhibiting PARP-2 selectively offers several advantages over broader PARP inhibitors that target both PARP-1 and PARP-2. While PARP-1 inhibitors have shown efficacy in specific cancer types, the unique role of PARP-2 in AR signaling suggests that its inhibition could provide a novel therapeutic avenue for patients with advanced prostate cancer, particularly those resistant to conventional therapies.

Our Services

At Alfa Cytology, we are committed to advancing the field of disease therapeutics through our comprehensive preclinical contract research organization (CRO) services. Our expertise in the development of PARP-2 selective inhibitors encompasses a range of specialized services designed to support drug discovery and development processes.

PARP-2 Inhibitor Development

• Target Validation
• Hit Identification
• Hit-to-Lead Service
• Lead Optimization Service

Modeling Services

• Cell Line Development
• Animal Models
• Organoid Models

Preclinical Studies

• Efficacy Studies
• Pharmacokinetic (PK) Studies
• Safety and Toxicology Studies
• Mechanistic Studies

For more information about our PARP-2 selective inhibitor development services or to discuss potential collaborations, please contact us at Alfa Cytology. Our team of experts is ready to assist you in advancing your drug development projects.

For research use only. Not intended for any clinical use.