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enzymlogic
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We help you to identify and optimize drugs with novel modes of binding.
We help you to identify and optimize drugs with novel modes of binding.

608 followers
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We are proudly helping industry leading companies around the world.

Through science and innovation we enable our customers to accelerate the discovery of breakthrough therapies capable of tackling the medical challenges of our times.

Our binding kinetics and kinetic selectivity screening services enable faster and cost-effective drug discovery by identifying the most promising drug candidates as well as withdrawing those compounds likely to fail in preclinical development.
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PROFILING THE KINETIC SELECTIVITY OF KINASE MARKETED DRUGS

The Human Protein Kinases

Protein kinases represent one of the largest protein families, with more than 500 encoded in the human genome. Their importance is further reflected in the fact that phosphorylation is the most abundant type of cellular regulation, affecting essentially every cellular process, including metabolism, growth, differentiation, motility or membrane transport. For these reason, kinases have been established as promising drug targets for the treatment of various types of human disease.

Beyond potency measurements: what is the value of Kinetic Selectivity in drug discovery?

One of the main challenges in drug discovery is the design of inhibitors with an appropriate balance between drug efficacy and potential adverse effects as early as possible in order to reduce the likelihood of safety issues. The characterization of compound selectivity has been traditionally focused on potency, where concentration-dependent parameters are measured at equilibrium. There is, however, a growing evidence for the physiological relevance of the temporal aspects of kinase-inhibitor interactions and the need of applying binding kinetics to optimize the temporal and functional response profiles of future drug candidates. In the study, the kinetic selectivity profiling of several marketed drugs reveals that parallel affinity and kinetic profiling of a compound towards multiple kinases is a power tool to design inhibitors with the desired selectivity profiles. We have found that compounds with identical affinity for a given kinase can exhibit very different kinetic profiles, which may be the reason for their tolerability in patients.

About Enzymlogic

Enzymlogic offers in vitro biochemical and cell-based assays to the biotechnological and pharmaceutical companies, life science laboratories and academic groups. Our binding kinetics, kinetic selectivity, assay development, profiling and screening services enable faster and cost-effective drug discovery by identifying the most promising drug candidates as well as withdrawing those compounds likely to fail in pre-clinical development. Additionally, Enzymlogic’s pioneering approach provides predictive tools that deliver physiologically relevant insights earlier in the drug discovery process.

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Enzymlogic was invited to the launch of “The NEST-Innovative Solutions Challenge” to present its innovative kinetic platform. KINETICfinder is a robust and highly sensitive binding kinetics platform that can be applied to high throughput kinetic screening and kinetic selectivity profiling to guide the affinity and kinetic optimization of cancer drugs. The NEST is an accelerated program powered by Takeda and Impact Hub for innovative projects developing initiatives and solutions to improve the quality of life for oncology patients.
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Beyond potency measurements: what is the value of Kinetic Selectivity in drug discovery?

One of the main challenges in drug discovery is the design of inhibitors with an appropriate balance between drug efficacy and potential adverse effects as early as possible in order to reduce the likelihood of safety issues.

The characterization of compound selectivity has been traditionally focused on potency, where concentration-dependent parameters are measured at equilibrium. There is, however, a growing evidence for the physiological relevance of the temporal aspects of kinase-inhibitor interactions and the need of applying binding kinetics to optimize the temporal and functional response profiles of future drug candidates.

#Enzymlogic #kinases #selectivity #drugdiscovery #cancer
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MEK drives BRAF activation through allosteric control of KSR pseudokinases, via https://www.nature.com/articles/nature25478

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Selective inhibition of NF-κB inducing kinase (NIK) in vivo leads to inhibition of multiple pathways known to be involved in systemic lupus erythematosus.
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MSK1, the protein kinase that keeps metastatic breast cancer cells dormant.
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