Translations:Discovery and development of angiotensin receptor blockers/36/en: Difference between revisions

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Message definition (Discovery and development of angiotensin receptor blockers)
===Pharmacophore and structure-activity relationship===
'''Pharmacophore'''<br />
There are three functional groups that are the most important parts for the [[bioactivity]] of ARBs, see figure 1 for details.<br />
The first one is the imidazole ring that binds to amino acids in helix 7 ([[Asparagine|Asn]]<sup>295</sup>). The second group is the biphenyl-methyl group that binds to amino acids in both helices 6 and 7 ([[Phenylalanine|Phe]]<sup>301</sup>, [[Phenylalanine|Phe]]<sup>300</sup>, [[Tryptophan|Trp]]<sup>253</sup> and [[Histidine|His]]<sup>256</sup>). The third one is the [[tetrazole]] group that interacts with amino acids in helices 4 and 5 ([[Arginine|Arg]]<sup>167</sup> and [[Lysine|Lys]]<sup>199</sup>). <br />
The tetrazole group has been successfully replaced by a carboxylic acid group as is the case with telmisartan.

Pharmacophore and structure-activity relationship

Pharmacophore
There are three functional groups that are the most important parts for the bioactivity of ARBs, see figure 1 for details.
The first one is the imidazole ring that binds to amino acids in helix 7 (Asn295). The second group is the biphenyl-methyl group that binds to amino acids in both helices 6 and 7 (Phe301, Phe300, Trp253 and His256). The third one is the tetrazole group that interacts with amino acids in helices 4 and 5 (Arg167 and Lys199).
The tetrazole group has been successfully replaced by a carboxylic acid group as is the case with telmisartan.

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