Metal-catalyzed cross-couplings of carbon bonds could enable creation of libraries of drug candidates to accelerate drug discovery

Main Category: Pharma Industry / Biotech Industry
Article Date: 20 Aug 2013 - 0:00 PDT Current ratings for:
Metal-catalyzed cross-couplings of carbon bonds could enable creation of libraries of drug candidates to accelerate drug discovery

James Bond had his reasons for ordering his martinis "shaken, not stirred." Similarly, drug manufacturers need to make sure the molecules in a new drug are arranged in an exact manner, lest there be dire consequences. Specifically, they need to be wary of enantiomers, mirror-image molecules composed of the same atoms, but arranged differently.

"One mirror image could be therapeutic while another could be poisonous," said Dr. Mark R. Biscoe, assistant professor of chemistry at The City College of New York. The classic case is thalidomide, a drug marketed in the 1950s and 1960s to treat morning sickness, which resulted in serious birth defects.

Professor Biscoe led a team of researchers at CCNY that developed a new method for preparing libraries of single-enantiomer molecules for therapeutic and toxicity studies that is faster and potentially less costly than methods now used in the pharmaceutical industry. Their findings were reported in Nature Chemistry.

Currently, drug developers typically rely on a chiral resolution process whereby compounds with roughly equal parts of the two enantiomers are separated into the individual enantiomers. Bioenzymatic processes can also be employed to generate single-enantiomer molecules. These strategies are wasteful and costly, Professor Biscoe explained.

He and colleagues found that a metal such as palladium could be employed to achieve a cross-coupling reaction with a single-enantiomer molecule without impacting the integrity of the mirror image formed in the product. By doing so, they could isolate one mirror image for evaluation as a drug candidate.

"By using a single-enantiomer partner in a cross-coupling reaction, we can rapidly generate a diverse library of biologically active molecules for use in drug screening," he said.

Article adapted by Medical News Today from original press release. Click 'references' tab above for source.
Visit our pharma industry / biotech industry section for the latest news on this subject.

The research was funded by the National Institutes of Health, City College, the Alfred P. Sloan Foundation and PSC-CUNY, with additional support from the National Science Foundation and the American Chemical Society Petroleum Research Fund.

Stereoretentive Pd-catalysed Stille cross-coupling reactions of secondary alkyl azastannatranes and aryl halides

Ling Li, Chao-Yuan Wang, Rongcai Huang & Mark R. Biscoe; Nature Chemistry 5, 607–612 (2013) doi:10.1038/nchem.1652

City College of New York

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Study features practical solution for MRI-ultrasound fusion to enable tumor-targeted, tissue-preserving prostate HIFU treatment

Main Category: MRI / PET / Ultrasound
Also Included In: Prostate / Prostate Cancer
Article Date: 27 Jul 2013 - 0:00 PDT Current ratings for:
Study features practical solution for MRI-ultrasound fusion to enable tumor-targeted, tissue-preserving prostate HIFU treatment

Study results published in the current issue of British Journal of Urology International (10.1111/bju.12223) demonstrate that new software to register and fuse information from magnetic resonance imaging (MRI) and ultrasound (US) images enables intraoperative visualization of tumors, not ordinarily seen in a US image. This technology has the potential to support new tissue-preserving treatments for prostate cancer, such as focal therapy.

In the study, "Image-Directed, Tissue-Preserving Focal Therapy of Prostate Cancer: a Feasibility Study of a Novel Deformable MR-US Registration System" researchers from University College London (UCL) evaluated the feasibility of using a computer-assisted, deformable image registration software to enable three-dimensional, multi-parametric MRI derived information on tumor location and extent to inform both the planning and treatment phase of focal high intensity focused ultrasound (HIFU) therapy using SonaCare Medical's Sonablate® 500 system.

Nested within the multi-center INDEX Trial, this pilot study employed computer assisted MRI-US image registration software within the planning of the first 26 men with a MRI-visible tumor treated at UCL with HIFU using a tissue-preserving quadrant, hemispheric (hemi) or extended hemi ablation therapy. Results demonstrated that thesoftware, developed at UCL, enables information of tumor location to be used for therapy planning using the Sonablate® 500 system without adding significant extra time to the standard procedural workflow. Such planning is particularly important for new tissue-preserving treatment approaches to ensure that the tumor is completely treated.

"Multi-parametric MRI has shown promise as an accurate method for determining the focality of tumors, and has promise as a potentially important enabler for minimally-invasive, tissue-preserving, or focal, HIFU treatments. However, most ablative technologies for localized prostate cancer use an ultrasound platform to plan and deliver treatment, on which the tumor cannot be accurately localized. This often results in discrepancies between the tumor and target volumes, potentially leading to under-treatment at the margins, or treatment of larger tissue volumes to compensate for inaccuracies in targeting," said lead author Louise Dickinson of UCL. "We are very pleased that the results of this pilot study demonstrate that deformable image registration is feasible and safe when introduced into a HIFU ablative therapy setting and suggests potential for improving the accuracy of targeting lesions using a tissue-preserving focal therapy approach."

The researchis based on breakthrough image analysis algorithms developed at the UCL Centre for Medical Image Computing and has undergone extensive clinical evaluation as part of clinical research studies led by Professor Mark Emberton, MD, Professor of Interventional Oncology and Director of the Division of Surgery and Interventional Science at UCL. Twenty-six prostate cancer patients have been successfully treated at UCLH using the Sonablate(®) 500 with the aid of this software as part of the INDEX Trial.

Dr. Dickinson added: "Indeed, if on-going clinical trials demonstrate clinical utility for focal therapy as an alternative to current standards of care, it is possible that image registration software may be essential for the efficient implementation of truly focal therapy techniques in which individual tumors are treated within an appropriate and safe surgical margin. The use of MRI-US registration potentially provides a cost-effective solution that, as shown in this study, can be easily integrated within existing workflows and interfaces, using standard surgical equipment."

Subsequent to this research, the team at UCL, led by Dr. Dean Barratt, is now developing a commercial version of their prostate image registration/fusion software, called "SmartTarget", with funding from the UK Department of Health and Wellcome Trust Health Innovation Challenge Fund. The SmartTarget project focuses on translating technology, which combines state-of-the-art diagnostic imaging with advanced image guidance technology to provide doctors with information on cancer location, size and shape so that it can be used to direct and guide prostate biopsy and minimally-invasive cancer treatments. In particular, the SmartTarget system exploits MRI, which can detect and characterize clinically significant cancers in a large proportion of patients.

"The adoption of tissue preserving approaches for the treatment of prostate cancer has been hampered by limitations in diagnosing and localizing clinically significant prostate cancers," said Mark Carol, M.D., Chief Development Officer for SonaCare Medical. "The publication of these results in the British Journal of Urology International is a tremendous validation of UCL's pioneering research in image registration and fusion technology that has led to significant advances in the validation and adoption of focal HIFU. We are proud to work with UCL to expand access to this breakthrough technology designed to enable targeted treatment of clinically significant prostate cancers."

Article adapted by Medical News Today from original press release. Click 'references' tab above for source.
Visit our mri / pet / ultrasound section for the latest news on this subject.

Recently SonaCare Medical, a global leader in minimally-invasive High-Intensity Focused Ultrasound (HIFU) technologies, and UCL Business PLC (UCLB), a leading technology transfer company that supports and commercializes research and innovations from UCL, announced a partnership to integrate SmartTarget image registration and fusion software into SonaCare Medical's innovative Sonablate® 500 HIFU system.

SonaCare Medical

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Understanding the strength of the mussels' underwater attachments could enable better glues and biomedical interfaces

Main Category: Medical Devices / Diagnostics
Article Date: 25 Jul 2013 - 1:00 PDT Current ratings for:
Understanding the strength of the mussels' underwater attachments could enable better glues and biomedical interfaces

Unlike barnacles, which cement themselves tightly to the surfaces of rocks, piers or ships, the clamlike bivalves called mussels dangle more loosely from these surfaces, attached by a collection of fine filaments known as byssus threads. This approach lets the creatures drift further out into the water, where they can absorb nutrients - although in the process, it exposes them to the risk of being torn away by the force of crashing waves.

But that almost never happens.

Despite the outwardly thin and fragile appearance of these threads, it turns out that in the dynamic, sloshing environment of waves and currents they can withstand impact forces that are nine times greater than the forces exerted by stretching in only one direction.

The secret to these tiny natural bungee cords has now been unraveled by MIT research scientist Zhao Qin and professor of civil and environmental engineering Markus Buehler. Their findings appear this week in the journal Nature Communications.

Byssus threads, they found, are composed of a well-designed combination of soft, stretchy material on one end and much stiffer material on the other. Both materials, despite their different mechanical properties, are made of a protein closely related to collagen, a main constituent of skin, bone, cartilage and tendons.

The team combined computer modeling and laboratory tests on the threads. To carry out their experiments, they placed an underwater cage in Boston Harbor for three weeks, during which time mussels attached themselves to the surfaces of glass, ceramics, wood and clay in the cage. Back in the lab, the mussels, threads and substrates were mounted in a tensile machine designed to test their strength by pulling on them with controlled deformation and recording the applied force during deformation.

"Many researchers have studied mussel glue before," Qin says, referring to the sticky substance that anchors byssus threads to a surface. But the static strength of the glue, and of the thread itself, "is not sufficient to withstand the impact by waves," he says. It's only by measuring the system's performance in simulated wave conditions that he and Buehler could determine how it accomplishes its amazing tenacity.

"We figured there must be something else going on," says Buehler, who heads MIT's Department of Civil and Environmental Engineering. "The adhesive is strong, but it's not sufficient."

The distribution of stiffness along the threads is key, Qin and Buehler found, suggesting that the distribution of intrinsic material properties and the overall architecture of the mussel attachment are important.

The distribution of stiffness in the mussels' threads enables them to be subjected to very large impact forces from waves. About 80 percent of the length of the byssus threads is made of stiff material, while 20 percent is softer and stretchier. This precise ratio may be critical, the researchers found: The soft and stretchy portions of the threads attach to the mussel itself, while the stiffer portion attaches to the rock. "It turns out that the ... 20 percent of softer, more extensible material is critical for mussel adhesion," Qin says.

In their simulations, Qin and Buehler systematically tested other ratios of the material composition and found that the 80-20 ratio of stiff to soft leads to the smallest reaction force. Having more of the softer material increases the reaction force because the material cannot effectively slow down deformation. Moreover, having more stiff material in byssus threads has other advantages, as it prevents the mussels from being pulled too far out by waves, which "would make it easier to hit other objects" and be damaged, Qin says.

These findings, Qin and Buehler say, could help in the design of synthetic materials that share some of these properties. For example, surgical sutures used in blood vessels or intestines are subjected to pulsating or irregular flows of liquid; the use of materials that combine stiffness and stretchiness, as byssus threads do, might provide advantages. The researchers say there may also be applications for materials to attach instruments to buildings, or sensors to underwater vehicles or sensing equipment in extreme conditions.

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Written by David Chandler, MIT News Office

Massachusetts Institute of Technology

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