{"id":231346,"date":"2026-02-14T05:24:57","date_gmt":"2026-02-14T11:24:57","guid":{"rendered":"https:\/\/lifeboat.com\/blog\/2026\/02\/how-a-key-receptor-tells-apart-two-nearly-identical-drug-molecules"},"modified":"2026-02-14T05:24:57","modified_gmt":"2026-02-14T11:24:57","slug":"how-a-key-receptor-tells-apart-two-nearly-identical-drug-molecules","status":"publish","type":"post","link":"https:\/\/lifeboat.com\/blog\/2026\/02\/how-a-key-receptor-tells-apart-two-nearly-identical-drug-molecules","title":{"rendered":"How a key receptor tells apart two nearly identical drug molecules"},"content":{"rendered":"<p><a class=\"aligncenter blog-photo\" href=\"https:\/\/lifeboat.com\/blog.images\/how-a-key-receptor-tells-apart-two-nearly-identical-drug-molecules2.jpg\"><\/a><\/p>\n<p>G-protein-coupled receptors (GPCRs) are one of the largest families of cell surface proteins in the human body that recognize hormones, neurotransmitters, and drugs. These receptors regulate a wide range of physiological processes and are the targets of more than 30% of currently marketed drugs. The histamine H<sub>1<\/sub> receptor (H<sub>1<\/sub>R) is one such GPCR subtype that plays a key role in mediating allergic reactions, inflammation, vascular permeability, airway constriction, wakefulness, and cognitive functions in the human body. While antihistamines primarily target H<sub>1<\/sub>R, current drugs can exhibit limited therapeutic efficacy, prompting researchers to look at H<sub>1<\/sub>R ligands from new perspectives.<\/p>\n<p>Recently, the importance of drug design based not only on the affinity or binding energy between a compound and its target protein, but also on its components, enthalpy, and entropy, has been recognized as crucial for rational drug design. In particular, enthalpy\u2013entropy compensation has emerged as a key concept for understanding ligand selectivity and isomer specificity. However, direct experimental measurement of these thermodynamic parameters has been limited to cell surface proteins, such as GPCRs.<\/p>\n<p>Addressing this gap, a research team led by Professor Mitsunori Shiroishi from the Department of Life System Engineering, Tokyo University of Science (TUS), Japan, systematically investigated the binding thermodynamics of the H<sub>1<\/sub>R. The team included Mr. Hiroto Kaneko (first-year doctoral student) and Associate Professor Tadashi Ando from TUS, among others. Their study was published online in <a href=\"https:\/\/doi.org\/10.1021\/acsmedchemlett.5c00696\" target=\"_blank\"><i>ACS Medicinal Chemistry Letters<\/i><\/a> on January 26, 2026.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>G-protein-coupled receptors (GPCRs) are one of the largest families of cell surface proteins in the human body that recognize hormones, neurotransmitters, and drugs. These receptors regulate a wide range of physiological processes and are the targets of more than 30% of currently marketed drugs. The histamine H1 receptor (H1R) is one such GPCR subtype that [\u2026]<\/p>\n","protected":false},"author":427,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[1902,11,19,47],"tags":[],"class_list":["post-231346","post","type-post","status-publish","format-standard","hentry","category-bioengineering","category-biotech-medical","category-chemistry","category-neuroscience"],"_links":{"self":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/231346","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/users\/427"}],"replies":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/comments?post=231346"}],"version-history":[{"count":0,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/231346\/revisions"}],"wp:attachment":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/media?parent=231346"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/categories?post=231346"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/tags?post=231346"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}