{"id":4825,"date":"2025-10-06T14:02:09","date_gmt":"2025-10-06T05:02:09","guid":{"rendered":"https:\/\/bionauts.jp\/?p=4825"},"modified":"2025-10-06T14:04:41","modified_gmt":"2025-10-06T05:04:41","slug":"derivative-screening-technology-for-peptide-drug-development","status":"publish","type":"post","link":"https:\/\/bionauts.jp\/?p=4825","title":{"rendered":"Derivative Screening Technology  for Peptide Drug Development"},"content":{"rendered":"<h3>Advantages<\/h3>\n<ul>\n<li><strong>Proven in derivative discovery for infectious disease drugs such as polymyxin B<\/strong><\/li>\n<li><strong>Seamless integration process of \u201cstructure exploration\u201d and \u201ccompound evaluation\u201d<\/strong><\/li>\n<li><strong>Two patterns of \u201coriginal amino acid units\u201d and \u201cmodified peptide libraries\u201d can be selected based on application<\/strong><\/li>\n<\/ul>\n<h3>Background &amp; Technology<\/h3>\n<p>Peptide drug development requires the examination of structural modifications to enhance activity or confer stability, but the current challenge is the enormous time and cost involved in the development process. Conventionally, the process involves first identifying the modifiable sites on the parent peptide, then preparing selectively chemically modified peptides at the identified sites, and finally evaluating them separately.<br \/>\nThe researchers have developed an amino acid unit that allows for both the identification of modifiable sites on the parent peptide and selective chemical modification at those sites. Two patterns of this amino acid unit are available:<\/p>\n<p><strong>Process <\/strong><strong>1<\/strong>: After peptide scanning, the alcohol side chain of this amino acid unit undergoes <strong>serine\/threonine ligation<\/strong> (54 synthesized compounds already created), enabling continuous evaluation of scanning and peptide chemical modification.<br \/>\n<strong>Process <\/strong><strong>2<\/strong>: Using the original amino acid unit, a wide range of commercially available aldehyde compounds can be screened and evaluated in a <strong>single step<\/strong> on the same plate where the modification site was scanned.<br \/>\nBoth processes 1 and 2 allow chemical modification to be performed on a <strong>micro-scale (hundreds of nmol)<\/strong>, achieving reductions in time and cost for synthesizing numerous peptides. This technology is believed to contribute significantly to future peptide drug discovery.<\/p>\n<h3>Data<\/h3>\n<p>For polymyxin B, a broad substrate range was discovered through the reaction in Process 2. From 50 derivatives, the synthesis and evaluation of the derivatives were carried out with a scan of only a few milligrams using in situ screening.<br \/>\nThe library contained many compounds exhibiting antimicrobial activity against two or more bacterial strains. Among these, P03 demonstrated antimicrobial activity against <em>E. coli<\/em> plus three other bacterial species, and P09 showed antimicrobial activity against <em>E. coli<\/em> plus <strong>six<\/strong> other bacterial species.<br \/>\nThese results demonstrated that this process can be used to search for compounds with<br \/>\nhigher antimicrobial activity than the parent peptide, as well as compounds exhibiting antimicrobial activity against a variety of bacterial species, and those showing antimicrobial activity against a large number of bacterial species.<\/p>\n<table style=\"border-collapse: collapse; width: 88.4991%;\">\n<tbody>\n<tr>\n<td style=\"width: 100%;\"><a href=\"http:\/\/bionauts.jp\/wp-content\/uploads\/2025\/10\/ON-05366_lower_EN-1.png\"><img decoding=\"async\" loading=\"lazy\" class=\"alignleft size-full wp-image-4827\" src=\"http:\/\/bionauts.jp\/wp-content\/uploads\/2025\/10\/ON-05366_lower_EN-1.png\" alt=\"\" width=\"578\" height=\"373\" srcset=\"https:\/\/bionauts.jp\/wp-content\/uploads\/2025\/10\/ON-05366_lower_EN-1.png 578w, https:\/\/bionauts.jp\/wp-content\/uploads\/2025\/10\/ON-05366_lower_EN-1-300x194.png 300w\" sizes=\"(max-width: 578px) 85vw, 578px\" \/><\/a><\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<h3>Patent<\/h3>\n<p>Pending\u3000Process1: international phase, Process2: domestic phase<\/p>\n<h3>Researcher<\/h3>\n<p>Hokkaido University \u00a0Center for research for education on drug discovery<br \/>\nProfessor Satoshi Ichikawa, Lecturer Akira Katsuyama<\/p>\n<h3>Development Phase<\/h3>\n<p>Current Stage: Concept validation completed for two patterns of \u201cOriginal Amino Acid Unit + Library-Based Exploration Process.\u201d<br \/>\nNext Phase:<\/p>\n<ol>\n<li>Development and evaluation of compounds identified through the search process<\/li>\n<li>Broad-range derivative search and evaluation using target peptides via this process<\/li>\n<li>Kit development and automation of this process<\/li>\n<\/ol>\n<p>We are seeking partner companies interested in technology licensing or development collaboration\/commercialization regarding the above. We would be pleased to begin with a detailed technical explanation and discussion.<\/p>\n<p>&nbsp;<\/p>\n<p>Project ID:ON-05366<\/p>\n","protected":false},"excerpt":{"rendered":"<p>A novel peptide scanning process capable of significantly reducing the time<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_mi_skip_tracking":false,"_monsterinsights_sitenote_active":false,"_monsterinsights_sitenote_note":"","_monsterinsights_sitenote_category":0},"categories":[1],"tags":[],"categories_of_inventions":[46],"disease_categories___indication":[],"asset_type":[],"development_phase":[],"medicine":[],"other_than_medicine":[],"material":[],"engineering":[],"software_it":[],"aioseo_notices":[],"_links":{"self":[{"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/posts\/4825"}],"collection":[{"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=4825"}],"version-history":[{"count":4,"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/posts\/4825\/revisions"}],"predecessor-version":[{"id":4831,"href":"https:\/\/bionauts.jp\/index.php?rest_route=\/wp\/v2\/posts\/4825\/revisions\/4831"}],"wp:attachment":[{"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=4825"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=4825"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=4825"},{"taxonomy":"categories_of_inventions","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories_of_inventions&post=4825"},{"taxonomy":"disease_categories___indication","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fdisease_categories___indication&post=4825"},{"taxonomy":"asset_type","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fasset_type&post=4825"},{"taxonomy":"development_phase","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fdevelopment_phase&post=4825"},{"taxonomy":"medicine","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fmedicine&post=4825"},{"taxonomy":"other_than_medicine","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fother_than_medicine&post=4825"},{"taxonomy":"material","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fmaterial&post=4825"},{"taxonomy":"engineering","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fengineering&post=4825"},{"taxonomy":"software_it","embeddable":true,"href":"https:\/\/bionauts.jp\/index.php?rest_route=%2Fwp%2Fv2%2Fsoftware_it&post=4825"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}