Kinase Target Screening Services
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Introduction: The Pivotal Role of Kinases in Drug Discovery
Protein kinases, constituting one of the largest enzyme families in the human genome, are pivotal regulators of virtually all cellular processes, including signal transduction, cell growth, differentiation, apoptosis, and metabolism. Their dysregulation is intrinsically linked to the pathophysiology of numerous human diseases, most notably cancer, inflammatory disorders, and neurodegenerative conditions. This critical role has positioned kinases as one of the most intensively pursued target classes in modern drug discovery. The development of selective kinase inhibitors has revolutionized treatment paradigms for various cancers, yet the complexity of the human kinase members poses significant challenges. Achieving therapeutic efficacy while minimizing off-target effects necessitates a profound understanding of a compound's interaction profile across a broad spectrum of kinases. Kinase target screening services have therefore become indispensable, enabling researchers to decipher compound selectivity, elucidate mechanisms of action (MOA), and identify potential liabilities early in the drug development pipeline. At Creative Biolabs, we leverage cutting-edge technologies and deep scientific expertise to provide comprehensive kinase screening solutions that empower our clients to accelerate their journey from discovery to clinical application.
Fig.1 Protein Kinases mediate several cellular activities.1
Kinase Target Screening Services at Creative Biolabs
At Creative Biolabs, we offer a comprehensive and flexible suite of kinase target screening services, employing a range of state-of-the-art assay technologies to cater to diverse research needs. Our platforms allow for detailed interrogation of kinase-compound interactions in both biochemical and cellular settings, including precise Affinity/Potency Determination.
Diverse Assay Technologies:
Biochemical Assays: These assays directly measure the effect of a compound on the enzymatic activity of purified kinases or its binding affinity.
We employ Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) assays to directly quantify substrate phosphorylation or competitive inhibitor binding. These assays offer a robust, homogeneous format ideal for high-throughput screening (HTS) and precise IC50 determination.
We employ cell lines like Ba/F3, which are dependent on specific kinase signaling pathways for proliferation and survival. Inhibition of the target kinase by a test compound leads to measurable anti-proliferative effects, providing a functional readout of cellular activity.
Utilizing cellular kinase target engagement assays, we can quantitatively measure compound binding to specific kinases directly within live cells. This confirms target engagement in a cellular context and provides crucial insights into cell permeability and intracellular potency.
Assessing kinase activity and pathway modulation by measuring the phosphorylation status of specific kinases (autophosphorylation) or their downstream substrates within cell lysates or intact cells using techniques such as Western blotting, ELISA, or flow cytometry.
Our Advantages
Choosing Creative Biolabs for your kinase target screening needs offers several distinct advantages:
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Unparalleled Scientific Expertise
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Comprehensive & Integrated Technology Platforms
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Extensive and Customizable Kinase Panels
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Focus on Physiological Relevance
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Rapid Turnaround Times & High-Quality Data
FAQs
Q1: What types of compounds can Creative Biolabs screen?
A1: We can screen a wide variety of compounds, including small molecules, peptides, natural products, and fragments. Please contact with us to discuss the specific requirements for your test samples.
Q2: What data and report format will I receive?
A2: You will receive a comprehensive report including raw data, processed data (e.g., % inhibition, IC50 curves and values), various data visualizations, detailed experimental protocols, and expert scientific interpretation of the results.
Q3: Why is kinase selectivity crucial in drug discovery?
A3: Since off-target effects may lead to toxicity, kinase selectivity is crucial for minimizing off-target effects. A highly selective inhibitor is more likely to have a cleaner safety profile. However, in some cases, inhibiting multiple specific kinases (polypharmacology) can offer enhanced therapeutic benefits, particularly in complex diseases like cancer. Profiling helps understand this balance.
Q4: Does Creative Biolabs offer screening against mutant kinases?
A4: Yes, Creative Biolabs offers screening for a wide range of clinically relevant mutant kinases, which is particularly important in the discovery of oncology drugs, where acquired drug resistance caused by kinase mutations is common.
Contact Us
Advance your kinase inhibitor drug discovery program with Creative Biolabs' expert screening services. We are ready to meet your specific needs and design a tailored screening strategy to accelerate your research.
Reference
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Bansal, Isha et al. "Small-molecule inhibitors of kinases in breast cancer therapy: recent advances, opportunities, and challenges." Frontiers in pharmacologyvol. 14 1244597. 30 Aug. 2023. DOI: 10.3389/fphar.2023.1244597. Distributed under Open Access License CC BY 4.0, without modification.
For Research Use Only | Not For Clinical Use
