Halogen chemistry has been exploited by medicinal chemists for nearly 70 years. To date, halogens were regarded useful for optimization of so-called ADMET properties (the acronym stands for absorption, distribution, metabolism, excretion, toxicity) – they improve oral absorption and facilitate crossing biological barriers by prospective drugs, they are useful for filling small hydrophobic cavities present in many protein targets, and they prolong lifetime of the drug.
Left panel: the charge distribution around the bromobenzene molecule. The regions of negative electrostatic potential are in blue, positive regions in grey. The grey disc in the forefront represents the ?-hole. Right panel: the overlay of the predicted binding poses of K17 inhibitor of casein kinase 2 (PDB code 2OXY) with (red) and without (blue) explicit sigma-holes (ESH) and comparison with the crystal structure (grey).
Image: Agnieszka Bronowska / HITS
Dr. Peter Saueressig | idw
Tissue-engineered colon from human cells develop different types of neurons
02.10.2015 | Children's Hospital Los Angeles
Big eyes! – MDC Researchers Identify Cause of Inherited Form of Extreme Nearsightedness
02.10.2015 | Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft
The Laser Zentrum Hannover e.V. (LZH) will present how laser-based technologies can contribute to the laboratory of the future at the LABVOLUTION in Hannover in Hall 9, Stand E67/09, from October 6th to 8th, 2015. As a part of the model lab smartLAB, the LZH is showing how additive manufacturing, better known as 3-D printing, can make experimental setups more flexible.
Twelve partners from science and industry are presenting an intelligent and innovative model lab at the special display smartLAB. A part of this intelligent...
Before embarking on a transcontinental journey, jet airplanes fill up with tens of thousands of gallons of fuel. In the event of a crash, such large quantities of fuel increase the severity of an explosion upon impact.
Researchers at Caltech and JPL have discovered a polymeric fuel additive that can reduce the intensity of postimpact explosions that occur during accidents and...
When surgical residents need to practice a complicated procedure to fashion a new ear for children without one, they typically get a bar of soap, carrot or an apple.
To treat children with a missing or under-developed ear, experienced surgeons harvest pieces of rib cartilage from the child and carve them into the framework...
Walking an obstacle course on Earth is relatively easy. Walking an obstacle course on Earth after being in space for six months is not quite as simple. The...
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