Business Wire

Enamine Supplies DSI Poised Fragment and Analogue Libraries to Diamond Light Source XChem Facility and SGC Oxford Screening Efforts

Jaa

Diamond Light Source (Diamond) and the Structural Genomic Consortium (SGC) Oxford announced today that Enamine, a chemical company and producer of novel chemical building blocks and screening libraries, will become a key supplier of poised fragment and analogue libraries to its XChem facility. Enamine will offer a new generation of the hit-finding library, Diamond-SGC-iNEXT (DSI) Poised Library to enable fast and productive fragment-based lead discovery (FBLD).

Diamond, in collaboration with the SGC Oxford, set up the XChem facility for fragment screening by X-ray crystallography to ensure public access to efficient FBLD. In addition, to enable fast and productive lead development, the collaboration developed the concept of “poised fragments” (Cox et al., Chemical Science, 2016), which constitutes its frontline screening strategy. FBLD is a common approach in academia and industry for developing new chemical probes and drug starting points (leads) from weak starting evidence, namely fragment hits. The hits must be chemically altered to improve their binding strength to the target protein, along with other properties.

The DSI Poised Library comprises 768 highly soluble fragments. Each compound is accompanied by its own virtual chemical space, which is readily accessible for synthesis and available for purchase through Enamine. Any hit from this library can be developed with follow-up chemistry within a maximum of three weeks using Enamine’s ground-breaking REAL database.

Prof Frank von Delft, Head of the XChem Collaboration and Principal Beamline Scientist at Diamond Light Source, explained: “The XChem facility has already helped over 60 users find thousands of hits across over 80 targets. To address the subsequent challenge, that chemical elaboration is generally expensive and time consuming, we developed and published the poised approach. Poised fragments can be synthesised in one step from commercially available starting materials using robust, high-yielding reactions, so that libraries of analogues can be synthesised quickly and at a low cost. Coupled with high-throughput biophysical methods, such as XChem screening but also NMR or SPR, this should provide a cost-efficient approach to early-stage fragment-based lead design.”

Dr Anthony Bradley, Project Leader on Fragment Development at SGC Oxford, added: “We quickly discovered that to realise the full power of the approach, we urgently needed to address the problem of compound supply. We are thus delighted to work with Enamine for the materialisation of the DSI Poised Library, fully benefiting from Enamine’s extensive stock of building blocks, capabilities and proven industry solutions. This puts both the primary library and follow-up analogue series within budgets and timelines of even exploratory compound discovery efforts worldwide. The SGC Oxford will be making extensive use of this offering in its many ongoing and future compound development projects.”

Michael Bossert, Head of Strategic Alliances at Enamine, commented: “The high technological degree of specialisation of Diamond and its unique XChem facility, was key to this collaboration. It is important to collaborate with high-tech companies in order to launch high-value technology-based products that aim to improve our customers R&D efficiencies and discovery project successes.”

Prof Paul Brennan, Principal Investigator for Medicinal Chemistry at SGC Oxford, and senior author of the original publication, added: “It is incredibly gratifying to see our original Diamond-SGC Poised Library (DSPL) and poised approach become a commercial offering. We hope this will allow it to become an essential tool in accelerating the development of small molecules probes and drugs.”

The library will be available to a non-exclusive group of nine research institutes operating X-ray and NMR screening located in Europe, USA and China. The European institutes include the partners of the iNEXT fragment screening effort: Diamond, EMBL and ESRF (Grenoble), NKI (Amsterdam), BMRZ (Frankfurt), FMP (Berlin) and CIRMMP (Florence). Other scientists interested in accessing and using the library for their own research are invited to do so.

For further information about the DSI Poised Library: https://xchem.github.io/oxxchem/DSI_poised_fragment_library.xlsx

ENDS

For high-resolution images, please contact lorna.cuddon@zymecommunications.com

Contact information

Zyme Communications
Lorna Cuddon
E: lorna.cuddon@zymecommunications.com
T: +44 7811996942

Tietoja julkaisijasta

For more than 50 years, Business Wire has been the global leader in press release distribution and regulatory disclosure.

Tilaa tiedotteet sähköpostiisi

Haluatko tietää asioista jo ennen kuin ne uutisoidaan? Kun tilaat tiedotteemme tältä julkaisijalta, saat ne sähköpostiisi yhtä aikaa suomalaisen median kanssa. Tilauksen voit halutessasi perua milloin tahansa.

Lue lisää julkaisijalta Business Wire

The Brightline Initiative, Project Management Institute and The Boston Consulting Group Host The Economist Events for Davos Panel20.1.2018 00:13Tiedote

The Brightline™ Initiative, a non-commercial coalition dedicated to helping organizations bridge the gap between strategy design and strategy delivery, along with Project Management Institute (PMI) and The Boston Consulting Group are hosting The Economist Events on the panel discussion, “The Business Case for Openness: Implementing Strategy in a Drawbridge up World.” This event marks Brightline’s debut at Davos. Dovetailing with the World Economic Forum’s overarching theme, “Creating a Shared Future in a Fractured World,” the discussion will address how business leaders can better adapt and implement strategies to promote openness and collaboration. PMI, a founding coalition member of Brightline, is particularly passionate about this topic, given the fact that they focus on collaborating with world-leading organizations to improve infrastructure initiatives in developing and mature communities around the world. “Today the challenges to sustainable growth through strategy implementation

New US Patent for Solidia Technologies’ CO2-cured Concrete Advances Performance and Sustainability of Building Materials19.1.2018 21:07Tiedote

The U.S. Patent and Trademark Office issued a patent for the structure of CO2-cured Solidia Concrete™, advancing the performance and sustainability of materials available to the global construction and materials industries. Solidia Technologies® holds the exclusive licensing rights to the patent, which is held by Rutgers University, where the original generation of the material was invented. This press release features multimedia. View the full release here: http://www.businesswire.com/news/home/20180119005608/en/ Solidia Concrete™ pavers. (Photo: Business Wire) U.S. Patent No. 9,868,667, "Bonding Element, Bonding Matrix and Composite Material Having the Bonding Element and Method of Manufacturing Thereof," covers the composition of matter of the non-hydraulic concrete. “The hydrate bonds in conventional concrete can compromise that material’s strength and durability,” explained Solidia Chief Technology Officer Nicholas DeCristofaro, Ph.D. “With CO2-cured concrete, bonding elements bas

Schlumberger Announces Full-Year and Fourth-Quarter 2017 Results19.1.2018 15:00Tiedote

Schlumberger Limited (NYSE:SLB) today reported results for full-year 2017 and the fourth quarter of 2017. Full-Year Results (Stated in millions, except per share amounts) Twelve Months Ended Change Dec. 31, 2017 Dec. 31, 2016 Year-on-year Revenue $30,440 $27,810 9% Pretax operating income $3,921 $3,273 20% Pretax operating margin 12.9% 11.8% 111 bps Net loss (GAAP basis) $(1,505) $(1,687) n/m Net income, excluding charges and credits* $2,085 $1,550 35% Diluted EPS (loss per share) (GAAP basis) $(1.08) $(1.24) n/m Diluted EPS, excluding charges and credits* $1.50 $1.14 32% *These are non-GAAP financial measures. See section below entitled "Charges & Credits" for details. n/m = not meaningful Full-year 2017 revenue of $30.4 billion increased 9% year-on-year. This included a full year’s activity from the acquired Cameron businesses as compared to three quarters of activity in 2016. Excluding the addition of Cameron, revenue growth was driven by land activity in North America, which increa

The Coca-Cola Company Announces New Global Vision to Help Create a World Without Waste19.1.2018 14:55Tiedote

The Coca-Cola Company announced today that it is fundamentally reshaping its approach to packaging, with a global goal to help collect and recycle the equivalent of 100% of its packaging by 2030. This press release features multimedia. View the full release here: http://www.businesswire.com/news/home/20180119005104/en/ In 2017, employees from Heartland Coca-Cola Bottling Co. joined with other volunteers in St. Louis to collect and sort 14,480 pounds of debris; 63 percent was diverted for recycling. Coca-Cola then partnered with manufacturer Phoenix Technologies to convert plastic bottles into recycled PET plastic for use in new bottles. (Photo: Business Wire) This goal is the centerpiece of the Company’s new packaging vision for a World Without Waste, which the Coca-Cola system intends to back with a multi-year investment that includes ongoing work to make packaging 100% recyclable. This begins with the understanding that food and beverage containers are an important part of people’s m

Researchers and Scientists from Five Countries Named Winners of King Faisal Prize 201819.1.2018 13:33Tiedote

Five researchers and scientists from Malaysia, Jordan, Tunisia, the US and the UK have been named winners of the King Faisal Prize 2018 as the 40th edition of the renowned award recognized their distinguished contributions towards humanity. The Prize honours exceptional achievements in five categories: Service to Islam, Islamic Studies, Arabic Language & Literature, Medicine, and Science. This press release features multimedia. View the full release here: http://www.businesswire.com/news/home/20180119005245/en/ His Royal Highness Prince Khalid Al-Faisal, Chairman of King Faisal Prize Board, Abdulaziz (Photo: AETOSWire) Professor Irwandi Jaswir, Deputy Dean of the International Institute for Halal Research and Training (INHART) and Secretary of Council of Professors at the International Islamic University Malaysia (IIUM), has been named the winner in the Service to Islam category for contributions to the development of ‘Halal Science’ and Halal food and consumer goods. Professor Bashar

E.ON Chooses Corinex Broadband over Powerline Technology for their Smart Metering Rollout19.1.2018 09:00Tiedote

E.ON, an international energy company that serves 32 million customers across multiple countries, has decided to use broadband over powerline (BPL) as the key technology in their communication mix, in the smart metering communication infrastructure for the low voltage part of their grid. E.ON chose Corinex as the solution provider for the initial two years of the deployment. The initial deployment will be several ten thousands of repeaters and head ends providing secure communication for a couple of hundred thousands of households. Corinex Grid Value network management based on IBM Tivoli platform will manage the network. “After extensive field trials, we found that Corinex broadband over powerline technology meets our requirements for mass rollout of smart metering services. We are convinced BPL is ideally suited to address the needs of many other utilities, so E.ON is interested in supporting BPL industry standardization in order to create a broad ecosystem of silicon and system vend

Uutishuoneessa voit lukea tiedotteitamme ja muuta julkaisemaamme materiaalia. Löydät sieltä niin yhteyshenkilöidemme tiedot kuin vapaasti julkaistavissa olevia kuvia ja videoita. Uutishuoneessa voit nähdä myös sosiaalisen median sisältöjä. Kaikki STT Infossa julkaistu materiaali on vapaasti median käytettävissä.

Tutustu uutishuoneeseemme