The study, published today in the prestigious journal Angewandte Chemie, presents the concept of a tiny polypeptide consisting of 42 amino acids to which virtually any target-seeking organic molecule can be bound. In the body it then seeks out the designated sites to be treated. What’s unique about the polypeptide is that it dramatically enhances the properties of the little molecule in a simple and very general way.
- This produces superbinders. They bind more strongly and more specifically than other alternatives, says Lars Baltzer, professor of organic chemistry, who believes it will be possible to rapidly develop new drugs much more readily with this new concept.
The whole concept goes against the grain of what is usually done in drug development. Traditionally it’s usually a matter of synthesizing drugs from A to Z, with certain requirements needing to be met in order to succeed. Drugs should be low molecular (500 Da), be highly fat soluble, and have no more than ten binding sites in order to pass through the cell membrane. But the majority are ineffective or toxic, and nowadays there are also ways to get larger molecules through cell membranes. Recently therapeutic antibodies have emerged as an alternative. They’re large (150,000 Da) and bind to the outside of cells, which they then “block.”
The new peptide is 5,000 Da or only 1/30 as large as a typical antibody, which is smaller than was thought possible. But according to Lars Baltzer nature has always signaled that this should work.
- The human growth factor hGH uses 35 amino acids to bind to its receptor, but it turns out that only six of them are critical. The rest can be replaced without significantly changing the function. There’s really nothing very special about placing a general peptide on a small molecule, but nobody has done it before, he says.
In this study the peptide was successfully bound to the inflammation marker CRP, which is an indicator of a risk of premature death in heart patients, among other things. Several other studies are underway and are proving to be equally successful.
These findings are of great importance to industry, and several large companies have shown their interest. The spin-out company that was previously formed out of Baltzer’s research team is now going to further develop the concept to be able to help the drug industry determine at a considerably earlier stage than today whether a drug candidate is worth pursuing or not.
For more information, please contact Lars Baltzer, mobile phone: +46 (0)706-482 595.
Uppsala universitet - kvalitet, kunskap och kreativitet sedan 1477. Forskning i världsklass och högklassig utbildning till global nytta för samhälle, näringsliv och kultur. Uppsala universitet är ett av norra Europas högst rankade lärosäten. www.uu.se
Anneli Waara | Uppsala universitet
Innovative genetic tests for children with developmental disorders and epilepsy
11.07.2018 | Christian-Albrechts-Universität zu Kiel
Oxygen loss in the coastal Baltic Sea is “unprecedentedly severe”
05.07.2018 | European Geosciences Union
For the first time ever, scientists have determined the cosmic origin of highest-energy neutrinos. A research group led by IceCube scientist Elisa Resconi, spokesperson of the Collaborative Research Center SFB1258 at the Technical University of Munich (TUM), provides an important piece of evidence that the particles detected by the IceCube neutrino telescope at the South Pole originate from a galaxy four billion light-years away from Earth.
To rule out other origins with certainty, the team led by neutrino physicist Elisa Resconi from the Technical University of Munich and multi-wavelength...
For the first time a team of researchers have discovered two different phases of magnetic skyrmions in a single material. Physicists of the Technical Universities of Munich and Dresden and the University of Cologne can now better study and understand the properties of these magnetic structures, which are important for both basic research and applications.
Whirlpools are an everyday experience in a bath tub: When the water is drained a circular vortex is formed. Typically, such whirls are rather stable. Similar...
Physicists working with Roland Wester at the University of Innsbruck have investigated if and how chemical reactions can be influenced by targeted vibrational excitation of the reactants. They were able to demonstrate that excitation with a laser beam does not affect the efficiency of a chemical exchange reaction and that the excited molecular group acts only as a spectator in the reaction.
A frequently used reaction in organic chemistry is nucleophilic substitution. It plays, for example, an important role in in the synthesis of new chemical...
Optical spectroscopy allows investigating the energy structure and dynamic properties of complex quantum systems. Researchers from the University of Würzburg present two new approaches of coherent two-dimensional spectroscopy.
"Put an excitation into the system and observe how it evolves." According to physicist Professor Tobias Brixner, this is the credo of optical spectroscopy....
Ultra-short, high-intensity X-ray flashes open the door to the foundations of chemical reactions. Free-electron lasers generate these kinds of pulses, but there is a catch: the pulses vary in duration and energy. An international research team has now presented a solution: Using a ring of 16 detectors and a circularly polarized laser beam, they can determine both factors with attosecond accuracy.
Free-electron lasers (FELs) generate extremely short and intense X-ray flashes. Researchers can use these flashes to resolve structures with diameters on the...
13.07.2018 | Event News
12.07.2018 | Event News
03.07.2018 | Event News
16.07.2018 | Physics and Astronomy
16.07.2018 | Life Sciences
16.07.2018 | Earth Sciences