Assays incorporate small molecule organic dye

Optimisation of cyclic AMP (adenosine 3',5'-cyclic monophosphate) assay formats with d2 acceptor molecule complements existing assay to enhance G-protein coupled receptor (GPCR) platform

Cisbio international, a developer of homogenous time resolved fluorescence (HTRF) technology and services used in assay development and drug screening, announced the launch of three new cyclic AMP (Camp) assays at the 2005 SBS conference in Geneva, Switzerland.

The assays incorporate d2, a novel small molecule organic dye developed by Cisbio to optimise assay performance and stability when measuring G-protein coupled receptor (GPCR) activation.

The upgraded Camp dynamic 2 and Camp femto 2 assays, along with the new Camp Hirange assay, take into account the variability of customers' biological material and cover a wide range of Camp concentration.

The Camp dynamic 2 assay is the kit of reference, suitable for most applications; Camp femto 2 is the most sensitive of the three; and Camp Hirange is used when the target has high level of expression.

First introduced in the IP-One assay, the d2 acceptor molecule has the same photophysical properties as XL665 - the current HTRF acceptor.

It brings additional benefits to the assays, including a straightforward immunochemistry and negligible compound interference.

Results show extreme consistency and are highly stable over time, so plates can be read for days afterwards, and the assays offer high miniaturisation capabilities, ie down to 6-10ul.

Since Camp and IP-One both run on the same industry-standard hardware and follow the same methodology and procedure, the introduction of the d2-based Camp assays creates a GPCR screening synergy for Cisbio's current customers that requires no additional technical resources or know-how.

"The development of the d2-based Camp assays is testimony to Cisbio's dedication to new products, as well as to innovative research and development initiatives," said Francois Degorce, head of HTRF marketing and business development, Cisbio international.

"d2 is the fruit of our technological research involved in improving HTRF technology for the benefit of our customers, and this acceptor is the cement of all of our assays: after Camp and IP-One, d2 performance should also benefit other assays in the HTRF product line".

GPCRs are among the most important target class investigated within drug discovery, involved in every aspect of human physiology, including sleep regulation, blood pressure, mood, food intake, perception of pain, control of cancer growth and immune response.

Upon activation, GPCRs carry information within the cell via two major signalling pathways: one results in variations of the Camp level whereas the other one results in a transient increase of intracellular Ca2+ triggered by inositol (1,4,5) tri-phosphate (IP3).

The optimisation of Cisbio's Camp assays to include the d2 already used in its IP-One Assay creates a technical platform for GPCR investigators to examine both GPCR pathways, and allows HTRF to be the technology of choice for all GPCR targets, says the company.

HTRF, homogenous time resolved fluorescence, is described as a robust and integrated technology platform that provides critical benefits to Cisbio's drug development customers.

HTRF can limit assay development time, while offering exceptional possibilities for miniaturisation and scale-up, and is particularly well-suited to evolving HTS needs.

Cisbio's bio-organic and protein chemistry resources, as well as its assay development knowledge and mastery of large-scale manufacturing procedures, are used by R and D teams seeking a powerful, reliable, sensitive technology which will contribute to major reductions in development and screening time.

HTRF helps create a homogenous assay format that is high-throughput screening (HTS)-friendly while also being scalable and/or miniaturisable depending upon the customer's needs.

HTRF has expanded its application field by implementing a growing range of processes, like kinases, protein-protein or ligand-receptor interactions, induced overexpressions of biomarkers or of secondary messengers.

Cisbio international is a developer of technologies that are used in assay development and drug screening procedures to enhance drug discovery, and offers a comprehensive technological platform for GPCR screening.

The company is also a pioneer in the field of homogenous fluorescence methodologies via its proprietary technology, HTRF, and produces a selection of biological reagents and methods used by pharmaceutical and biotechnology companies, as well as contract research organisations (CROs).

In addition, Cisbio international develops, manufactures and markets antibody-based diagnostic assays for the quantification of tumour markers and other biomarkers in clinical biology.

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