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5N-Bicalutamide | Wikipedia audio article

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This is an audio version of the Wikipedia Article: 5N-Bicalutamide Listening is a more natural way of learning, when compared to reading. Written language only began at around 3200 BC, but spoken language has existed long ago. Learning by listening is a great way to: - increases imagination and understanding - improves your listening skills - improves your own spoken accent - learn while on the move - reduce eye strain Now learn the vast amount of general knowledge available on Wikipedia through audio (audio article). You could even learn subconsciously by playing the audio while you are sleeping! If you are planning to listen a lot, you could try using a bone conduction headphone, or a standard speaker instead of an earphone. You can find other Wikipedia audio articles too at: https://www.youtube.com/channel/UCuKfABj2eGyjH3ntPxp4YeQ In case you don't find one that you were looking for, put a comment. This video uses Google TTS en-US-Standard-D voice. SUMMARY ======= 5N-Bicalutamide, or 5-azabicalutamide, is a highly potent nonsteroidal antiandrogen (NSAA) which was discovered in 2016. It is a structural modification of bicalutamide differing it from it only by the replacement of a carbon atom with a nitrogen atom in one of its phenyl rings. Similarly to bicalutamide, the drug acts as a selective antagonist of the androgen receptor (AR). However, unlike bicalutamide, it is a reversible covalent antagonist and stays bound to the receptor for a far longer amount of time. As a result of this difference, 5N-bicalutamide has markedly improved potency relative to bicalutamide, with approximately 150-fold higher affinity for the AR (Ki = 0.15 nM versus 22.3 nM) and about 20-fold greater functional inhibition (IC50 = 15 nM versus 310 nM) of the AR. Future studies of 5N-bicalutamide in normal and mutated prostate cancer cells are planned or underway and it is anticipated that N-bicalutamide may be able to overcome resistance to current antiandrogens that are used in the treatment of prostate cancer.Enzalutamide and related second-generation NSAAs like RD-162 and apalutamide were derived from bicalutamide and as a result are similar to it in chemical structure. They have up to about 10-fold higher affinity for the AR than does bicalutamide and hence are comparatively more potent and efficacious antiandrogens. However, their structures are rigidified such that the analogous structural modification that was done with bicalutamide to create 5N-bicalutamide could not be used to increase affinity or potency with them. Enzalutamide was described in 2013 as "the emperor of all antiandrogens" and other second-generation NSAAs have similar potency to it, so 5N-bicalutamide would appear to be the most potent AR antagonist to have been developed thus far.
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