Screen PARG in hours instead of months using the Transcreener® ADPR Assay and the Enzolution™ PARG Assay System TL;DR Poly(ADP-ribose) glycohydrolase (PARG) is a critical enzyme in the DNA damage response that removes poly(ADP-ribose) chains generated by PARP enzymes. Because PARG regulates DNA repair signaling, replication stress, and cell survival pathways, it has emerged as […]
TL;DR A SIRT2 inhibitor is a small molecule that blocks the activity of Sirtuin 2 (SIRT2), a NAD⁺-dependent deacetylase implicated in neurodegeneration, cancer, metabolism, and aging. SIRT2 inhibitors are actively pursued as therapeutic agents, but success depends on robust biochemical assays that accurately measure enzymatic activity and inhibitor potency. A complete SIRT2 screening workflow combines […]
Summary Yes—BellBrook Labs can develop assays for novel enzyme targets, especially when the target’s activity can be measured through universal biochemical readouts (like ADP/ATP turnover, GDP/GTP turnover, AMP/GMP formation, SAH production, cGAMP generation, cyclic nucleotide turnover, and related nucleotide-linked products). BellBrook’s strongest fit is helping teams move from “we have a target and a hypothesis” […]
Introduction Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase that plays a central role in cell-cycle progression, mitotic entry, centrosome maturation, and chromosome segregation. Dysregulated PLK1 activity is strongly associated with oncogenesis, tumor aggressiveness, and poor clinical outcomes across multiple cancer types. As a result, PLK1 has become a high-value target for oncology drug […]
Quick Answer: What Is the Best Way to Screen IRE1a Inhibitors? The most effective way to screen IRE1a inhibitors is to use an HTS-optimized active recombinant IRE1α enzyme combined with a homogeneous biochemical assay that directly measures enzymatic activity, such as an ADP-based readout. This approach enables reliable, scalable detection of ATP turnover, supports clean […]
Best Practices for Reliable, High-Throughput Kinase Inhibitor Screening Quick Answer A robust kinase inhibition assay requires careful control of ATP concentration, enzyme linearity, substrate selection, and detection chemistry. Homogeneous, ADP-based assays—such as the Transcreener ADP Kinase Assay—are widely used because they are universal, HTS-ready, and compatible with inhibitor profiling across diverse kinase families. Introduction: Why […]
Quick answer A PARP2 inhibitor program is worth pursuing (or at least profiling) because PARP2 is a DNA damage–activated ADP-ribosyltransferase that works alongside PARP1 in DNA repair—especially base excision repair (BER)—and has additional emerging roles in replication stress responses. That biology makes PARP2 relevant to cancer mechanisms and potentially other disease settings where DNA repair, […]
Why “Building It Yourself” Often Delays Screening, Burns Budget, and Slows Drug Discovery Quick Answer DIY assay optimization often costs far more than it appears. While building a biochemical assay internally may seem economical, the hidden costs—lost scientist time, delayed screening, failed scale-up, inconsistent reagents, and repeated troubleshooting—can push timelines out by months and consume […]
Introduction: The Rise of XRN1 as a Therapeutic Target The search for novel drug targets demands a convergence of biological insight and powerful screening technologies. One such emerging target is XRN1, a highly conserved 5′→3′ exoribonuclease involved in mRNA decay. Disruptions in mRNA turnover are linked with diseases ranging from cancer to neurodegeneration, making XRN1 […]
Quick Answer: How Do You Screen for WRN Helicase Inhibitors? The most effective way to discover true WRN helicase inhibitors is to use multiple, orthogonal assay methods. A best-practice workflow combines a functional DNA unwinding assay (Heliscreener™) with an ATPase/ADP detection assay (Enzolution™ WRN + Transcreener® ADP). This multi-assay approach improves hit confidence, reduces fluorescence […]
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