AACR Virtual Meeting IIへの参加登録はこちら☆
ユーロフィンズディスカバリーでは、表現型スクリーニング（BioMAP System）を用いたより迅速ながん免疫療法開発、JAK2阻害剤のメカニズムの解明、およびPROTAC誘導性タンパク質分解を評価するための新しいツールについて発表をします。各ポスターのアブストラクトは下記のとおりです。
Identifying Novel Immuno-Oncology Therapies with BioMAP Early Screening
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An efficient way to evaluate drug combinations in vitro streamlines R&D efforts. As BioMAP®Oncology Panels are amenable to automation and medium- and high-throughput scaling, for AACR poster presentation 6289 we used BioMAP Oncology Early Screening Services to rapidly screen a library of compounds covering a broad range of mechanisms in order to identify cytotoxicity and immuno-oncology (IO) potential. Evaluation of compound activities at non-cytotoxic concentrations identified a select group that shares immunorestorative activities with already approved IO drugs. We confirmed these activities in the BioMAP Oncology CRC Panel, which allowed further characterization of compound effects in a stromal model versus a vascular model of the tumor microenvironment (TME). Finally, we determined the impacts of a small molecule + anti PD-1 combination on a potentially improved IO window. Utilizing this rapid screening followed by TME contextual assessment approach, drug developers can benefit from an early focus for their oncology indication efforts, prior to clinical evaluation.
Discrimination of Clinical JAK2 Inhibitors for Myeloproliferative Disorders with BioMAP Diversity PLUS
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Discontinuation rates for JAK2 inhibitors are high, mainly due to lack of response, loss of efficacy, intolerance, and drug-induced cytopenias, supporting the need for new approaches that can report early on preclinical efficacy and safety. In AACR presentation 1847 we used BioMAP Diversity PLUS® phenotypic profiling to identify a shared profile signature among the four JAK2 inhibitors RUX, FED, MOM, and GAN, pointing to an efficacy signature in myeloid proliferative disorders for this class of therapeutics. Identification of differentiating activities and network cluster analysis allowed us to discriminate within the JAK2 mechanism class for secondary pharmacology, with implications for safety-related outcomes. From these data, RUX showed the greatest efficacy with the fewest safety flags while FED and GAN demonstrated less advantageous profiles. By profiling preclinical candidates and approved drugs in conditions that preserve the complex crosstalk and feedback mechanisms relevant to in vivo outcomes, drug developers benefit from early insights on efficacy and safety.
E3scan Ligand Binding Assay for Targeted Protein Degradation and PROTAC® Discovery
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E3 ligases have emerged as pivotal targets for drug discovery using the promising new paradigm of targeted protein degradation. As there are hundreds of diverse putative E3 ligases with differentiated tissue expression, this new paradigm has potential to advance precision medicine with selective degradation of disease-specific proteins. In our AACR poster presentation 6408 we introduce E3scanTM, based upon the well-established KINOMEscan® technology. Using these newly launched and validated E3scan assays against cereblon, the double minute 2 homologues MDM2 and MDMX, the Von Hippel–Lindau tumor suppressor VHL, and others, we measured pM KDs and obtained high quality KD curves. Use of this robust, high throughput platform enables researchers to accelerate structure activity relationship (SAR) analysis and library screening campaigns in the E3 drug discovery field.
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