{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,31]],"date-time":"2026-10-31T11:49:50Z","timestamp":1793447390576,"version":"4.5.0"},"reference-count":50,"publisher":"American Chemical Society (ACS)","issue":"1","license":[{"start":{"date-parts":[[2018,12,16]],"date-time":"2018-12-16T00:00:00Z","timestamp":1544918400000},"content-version":"vor","delay-in-days":27,"URL":"https:\/\/pubs.acs.org\/page\/policy\/authorchoice_termsofuse.html"}],"funder":[{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["DK090316"],"award-info":[{"award-number":["DK090316"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["DK117599"],"award-info":[{"award-number":["DK117599"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["F32DK115109"],"award-info":[{"award-number":["F32DK115109"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["U01DK116101"],"award-info":[{"award-number":["U01DK116101"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["U54DK083912"],"award-info":[{"award-number":["U54DK083912"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000062","name":"National Institute of Diabetes and Digestive and Kidney Diseases","doi-asserted-by":"publisher","award":["UM1DK100846"],"award-info":[{"award-number":["UM1DK100846"]}],"id":[{"id":"10.13039\/100000062","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100006108","name":"National Center for Advancing Translational Sciences","doi-asserted-by":"publisher","award":["1UL1TR000460"],"award-info":[{"award-number":["1UL1TR000460"]}],"id":[{"id":"10.13039\/100006108","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100007013","name":"F. Hoffmann-La Roche","doi-asserted-by":"publisher","award":["NA"],"award-info":[{"award-number":["NA"]}],"id":[{"id":"10.13039\/100007013","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2019,1,18]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>The importance of Discoidin Domain Receptor 1 (DDR1) in renal fibrosis has been shown via gene knockout and use of antisense oligonucleotides; however, these techniques act via a reduction of DDR1 protein, while we prove the therapeutic potential of inhibiting DDR1 phosphorylation with a small molecule. To date, efforts to generate a selective small-molecule to specifically modulate the activity of DDR1 in an in vivo model have been unsuccessful. We performed parallel DNA encoded library screens against DDR1 and DDR2, and discovered a chemical series that is highly selective for DDR1 over DDR2. Structure-guided optimization efforts yielded the potent DDR1 inhibitor 2.45, which possesses excellent kinome selectivity (including 64-fold selectivity over DDR2 in a biochemical assay), a clean in vitro safety profile, and favorable pharmacokinetic and physicochemical properties. As desired, compound 2.45 modulates DDR1 phosphorylation in vitro as well as prevents collagen-induced activation of renal epithelial cells expressing DDR1. Compound 2.45 preserves renal function and reduces tissue damage in Col4a3\u2013\/\u2013 mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo. Our results may have wider significance as Col4a3\u2013\/\u2013 mice also represent a model for chronic kidney disease, a disease which affects 10% of the global population.<\/jats:p>","DOI":"10.1021\/acschembio.8b00866","type":"journal-article","created":{"date-parts":[[2018,11,19]],"date-time":"2018-11-19T12:40:47Z","timestamp":1542631247000},"page":"37-49","source":"Crossref","is-referenced-by-count":118,"title":["DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and\nRenal Function Loss in a Genetic Mouse Model of Alport Syndrome"],"prefix":"10.1021","volume":"14","author":[{"given":"Hans","family":"Richter","sequence":"first","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1284-1977","authenticated-orcid":true,"given":"Alexander L.","family":"Satz","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marc","family":"Bedoucha","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bernd","family":"Buettelmann","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ann C.","family":"Petersen","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anja","family":"Harmeier","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ricardo","family":"Hermosilla","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Remo","family":"Hochstrasser","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dominique","family":"Burger","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bernard","family":"Gsell","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rodolfo","family":"Gasser","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sylwia","family":"Huber","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Melanie N.","family":"Hug","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Buelent","family":"Kocer","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bernd","family":"Kuhn","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Martin","family":"Ritter","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Markus G.","family":"Rudolph","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Franziska","family":"Weibel","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]},{"name":"Ridgeline Therapeutics GmbH , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Judith","family":"Molina-David","sequence":"additional","affiliation":[{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]},{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jin-Ju","family":"Kim","sequence":"additional","affiliation":[{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]},{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Javier Varona","family":"Santos","sequence":"additional","affiliation":[{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]},{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Martine","family":"Stihle","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guy J.","family":"Georges","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Munich, Germany, 82377"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R. Daniel","family":"Bonfil","sequence":"additional","affiliation":[{"name":"Nova Southeastern University , , , ,","place":["Fort Lauderdale, Florida, United States, 33328"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rafael","family":"Fridman","sequence":"additional","affiliation":[{"name":"Wayne State University , , , ,","place":["Detroit, Michigan, United States, 48202"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sabine","family":"Uhles","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Solange","family":"Moll","sequence":"additional","affiliation":[{"name":"University Hospital of Geneva , ,","place":["Geneva, Switzerland, 1205"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Christian","family":"Faul","sequence":"additional","affiliation":[{"name":"University of Alabama at Birmingham , , 35294,","place":["Birmingham, Alabama, United States"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alessia","family":"Fornoni","sequence":"additional","affiliation":[{"name":"University of Miami Miller School of Medicine , , , ,","place":["Miami, Florida, United States, 33136"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marco","family":"Prunotto","sequence":"additional","affiliation":[{"name":"Roche Pharma Research and Early Development, Roche Innovation Center , ,","place":["Basel, Switzerland, 4070"]},{"name":"Roche and Genentech Late Stage Development , , ,","place":["Basel, Switzerland, 4070"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2018,11,19]]},"reference":[{"key":"2026090213583234200_cit1","doi-asserted-by":"publisher","first-page":"199","DOI":"10.1002\/path.2277","article-title":"Cellular and molecular mechanisms\nof fibrosis","volume":"214","author":"Wynn","year":"2008","journal-title":"J. Pathol."},{"key":"2026090213583234200_cit2","doi-asserted-by":"publisher","first-page":"159","DOI":"10.7326\/0003-4819-152-3-201002020-00007","article-title":"Narrative\nreview: fibrotic diseases: cellular and molecular mechanisms and novel\ntherapies","volume":"152","author":"Rosenbloom","year":"2010","journal-title":"Ann. Intern. Med."},{"key":"2026090213583234200_cit3","doi-asserted-by":"publisher","first-page":"95","DOI":"10.1056\/NEJMc1504848","article-title":"Fibrosis--A\nCommon Pathway to Organ Injury and Failure","volume":"373","author":"Rockey","year":"2015","journal-title":"N. Engl. J. Med."},{"key":"2026090213583234200_cit4","doi-asserted-by":"publisher","first-page":"1340","DOI":"10.1016\/j.ajpath.2012.02.004","volume":"180","author":"Hinz","year":"2012","journal-title":"Am. J. Pathol."},{"key":"2026090213583234200_cit5","doi-asserted-by":"publisher","first-page":"309","DOI":"10.1146\/annurev-physiol-022516-034227","article-title":"Mechanisms of Renal Fibrosis","volume":"80","author":"Humphreys","year":"2018","journal-title":"Annu. Rev. Physiol."},{"key":"2026090213583234200_cit6","doi-asserted-by":"publisher","first-page":"861","DOI":"10.1056\/NEJMoa011161","article-title":"Effects of losartan\non renal and cardiovascular outcomes in patients with type 2 diabetes\nand nephropathy","volume":"345","author":"Brenner","year":"2001","journal-title":"N. Engl. J. Med."},{"key":"2026090213583234200_cit7","doi-asserted-by":"publisher","first-page":"1034","DOI":"10.1681\/ASN.2013010012","article-title":"Integrins in Kidney\nDisease","volume":"24","author":"Pozzi","year":"2013","journal-title":"J. Am. Soc. Nephrol."},{"key":"2026090213583234200_cit8","doi-asserted-by":"publisher","first-page":"185","DOI":"10.1016\/j.matbio.2013.12.002","article-title":"Discoidin domain receptors\nin disease","volume":"34","author":"Borza","year":"2014","journal-title":"Matrix Biol."},{"key":"2026090213583234200_cit9","doi-asserted-by":"publisher","first-page":"52","DOI":"10.3389\/fmed.2017.00052","article-title":"Periostin\nand Discoidin Domain Receptor 1: New Biomarkers or Targets for Therapy\nof Renal Disease","volume":"4","author":"Prakoura","year":"2017","journal-title":"Front. Med."},{"key":"2026090213583234200_cit10","doi-asserted-by":"publisher","first-page":"318","DOI":"10.1016\/j.matbio.2017.12.013","article-title":"Renal fibrosis: Recent translational aspects","volume":"68-69","author":"Francois","year":"2018","journal-title":"Matrix Biol."},{"key":"2026090213583234200_cit11","doi-asserted-by":"publisher","first-page":"13","DOI":"10.1016\/S1097-2765(00)80003-9","article-title":"The discoidin\ndomain receptor tyrosine kinases are activated by collagen","volume":"1","author":"Vogel","year":"1997","journal-title":"Mol. Cell"},{"key":"2026090213583234200_cit12","doi-asserted-by":"publisher","first-page":"7430","DOI":"10.1074\/jbc.R112.444158","article-title":"Discoidin Domain Receptors: Unique Receptor Tyrosine\nKinases in Collagen-mediated Signaling","volume":"288","author":"Fu","year":"2013","journal-title":"J. Biol.\nChem."},{"key":"2026090213583234200_cit13","doi-asserted-by":"publisher","first-page":"785","DOI":"10.3892\/ijmm_00000405","article-title":"Linkage and association\nstudy of discoidin domain receptor 1 as a novel susceptibility gene\nfor childhood IgA nephropathy","volume":"25","author":"Hahn","year":"2010","journal-title":"Int. J. Mol.\nMed."},{"key":"2026090213583234200_cit14","doi-asserted-by":"publisher","first-page":"3374","DOI":"10.1681\/ASN.2006060677","article-title":"Discoidin Domain Receptor 1 Null\nMice Are Protected against Hypertension-Induced Renal Disease","volume":"17","author":"Flamant","year":"2006","journal-title":"J. Am. Soc. Nephrol."},{"key":"2026090213583234200_cit15","doi-asserted-by":"publisher","first-page":"83","DOI":"10.1016\/j.ajpath.2011.03.023","article-title":"Discoidin domain receptor 1 is a major mediator of\ninflammation and fibrosis in obstructive nephropathy","volume":"179","author":"Guerrot","year":"2011","journal-title":"Am. J. Pathol."},{"key":"2026090213583234200_cit16","doi-asserted-by":"publisher","first-page":"21262","DOI":"10.1038\/srep21262","article-title":"Protective effects of genetic inhibition\nof Discoidin Domain Receptor 1 in experimental renal disease","volume":"6","author":"Kerroch","year":"2016","journal-title":"Sci. Rep."},{"key":"2026090213583234200_cit17","doi-asserted-by":"publisher","first-page":"1965","DOI":"10.1093\/ndt\/gfv074","article-title":"Discoidin\ndomain receptor-1 and periostin: new players in chronic kidney disease","volume":"30","author":"Alfieri","year":"2015","journal-title":"Nephrol., Dial., Transplant."},{"key":"2026090213583234200_cit18","doi-asserted-by":"publisher","first-page":"4079","DOI":"10.1096\/fj.11-194902","article-title":"Genetic inhibition of discoidin domain receptor 1 protects\nmice against crescentic glomerulonephritis","volume":"26","author":"Kerroch","year":"2012","journal-title":"FASEB J."},{"key":"2026090213583234200_cit19","doi-asserted-by":"publisher","first-page":"420","DOI":"10.1111\/cbdd.12863","volume":"89","author":"Liu","year":"2017","journal-title":"Chem. Biol. Drug\nDes."},{"key":"2026090213583234200_cit20","doi-asserted-by":"publisher","first-page":"798","DOI":"10.1021\/acsmedchemlett.5b00143","article-title":"Fragment-Based Discovery\nof Potent and Selective DDR1\/2 Inhibitors","volume":"6","author":"Murray","year":"2015","journal-title":"ACS\nMed. Chem. Lett."},{"key":"2026090213583234200_cit21","doi-asserted-by":"publisher","first-page":"1540","DOI":"10.1039\/C5MB00911A","article-title":"Identification of novel inhibitors of DDR1 against idiopathic pulmonary\nfibrosis by integrative transcriptome meta-analysis, computational\nand experimental screening","volume":"12","author":"Chen","year":"2016","journal-title":"Mol. BioSyst."},{"key":"2026090213583234200_cit22","doi-asserted-by":"publisher","first-page":"2875","DOI":"10.2174\/138161212800672697","article-title":"Recent\nadvances in designing substrate-competitive protein kinase inhibitors","volume":"18","author":"Han","year":"2012","journal-title":"Curr. Pharm. Des."},{"issue":"6","key":"2026090213583234200_cit23","doi-asserted-by":"publisher","first-page":"2894","DOI":"10.1016\/j.ajpath.2011.09.002","article-title":"Loss of\ndiscoidin domain receptor 2 promotes hepatic fibrosis after chronic\ncarbon tetrachloride through altered paracrine interactions between\nhepatic stellate cells and liver-associated macrophages","volume":"179","author":"Olaso","year":"2011","journal-title":"Am. J. Pathol."},{"key":"2026090213583234200_cit24","doi-asserted-by":"publisher","first-page":"1403","DOI":"10.1083\/jcb.135.5.1403","article-title":"Molecular and functional\ndefects in kidneys of mice lacking collagen alpha 3(IV): implications\nfor Alport syndrome","volume":"135","author":"Miner","year":"1996","journal-title":"J. Cell Biol."},{"key":"2026090213583234200_cit25","doi-asserted-by":"publisher","first-page":"13","DOI":"10.1016\/j.matbio.2014.01.006","article-title":"Collagen receptors integrin alpha2beta1\nand discoidin domain receptor 1 regulate maturation of the glomerular\nbasement membrane and loss of integrin alpha2beta1 delays kidney fibrosis\nin COL4A3 knockout mice","volume":"34","author":"Rubel","year":"2014","journal-title":"Matrix Biol."},{"key":"2026090213583234200_cit26","doi-asserted-by":"publisher","first-page":"346","DOI":"10.1016\/j.matbio.2010.03.002","article-title":"Loss of collagen-receptor DDR1 delays renal fibrosis in hereditary\ntype IV collagen disease","volume":"29","author":"Gross","year":"2010","journal-title":"Matrix Biol."},{"key":"2026090213583234200_cit27","doi-asserted-by":"publisher","first-page":"1323","DOI":"10.1039\/C6MD00221H","article-title":"Analysis of the\nproductivity of DNA encoded libraries","volume":"7","author":"Eidam","year":"2016","journal-title":"MedChemComm"},{"key":"2026090213583234200_cit28","doi-asserted-by":"publisher","first-page":"2237","DOI":"10.1021\/acschembio.5b00378","article-title":"DNA Encoded Library Selections and\nInsights Provided by Computational Simulations","volume":"10","author":"Satz","year":"2015","journal-title":"ACS Chem. Biol."},{"key":"2026090213583234200_cit29","doi-asserted-by":"publisher","first-page":"4443","DOI":"10.1021\/acs.jmedchem.5b01409","article-title":"Analysis of Past and Present Synthetic\nMethodologies on Medicinal Chemistry: Where Have All the New Reactions\nGone?","volume":"59","author":"Brown","year":"2016","journal-title":"J. Med. Chem."},{"key":"2026090213583234200_cit30","doi-asserted-by":"publisher","first-page":"318","DOI":"10.1016\/S0022-2143(97)90180-3","article-title":"Cell lines\nwith extended in vitro growth potential from human renal proximal\ntubule: Characterization, response to inducers, and comparison with\nestablished cell lines","volume":"129","author":"Racusen","year":"1997","journal-title":"J. Lab. Clin. Med."},{"key":"2026090213583234200_cit31","doi-asserted-by":"publisher","first-page":"148","DOI":"10.1186\/s12967-018-1524-5","article-title":"Selective pharmacological inhibition of DDR1 prevents\nexperimentally-induced glomerulonephritis in prevention and therapeutic\nregime","volume":"16","author":"Moll","year":"2018","journal-title":"J. Transl. Med."},{"key":"2026090213583234200_cit32","doi-asserted-by":"publisher","first-page":"e01149","DOI":"10.7554\/eLife.01149","article-title":"Nanoscale protein architecture\nof the kidney glomerular basement membrane","volume":"2","author":"Suleiman","year":"2013","journal-title":"eLife"},{"key":"2026090213583234200_cit33","doi-asserted-by":"publisher","first-page":"3287","DOI":"10.1021\/jm5012319","article-title":"Small molecule discoidin domain receptor kinase inhibitors and potential\nmedical applications","volume":"58","author":"Li","year":"2015","journal-title":"J. Med. Chem."},{"key":"2026090213583234200_cit34","doi-asserted-by":"publisher","first-page":"2145","DOI":"10.1021\/cb400430t","article-title":"Discovery of a potent and selective DDR1 receptor tyrosine\nkinase inhibitor","volume":"8","author":"Kim","year":"2013","journal-title":"ACS Chem. Biol."},{"key":"2026090213583234200_cit35","doi-asserted-by":"publisher","first-page":"44","DOI":"10.1016\/j.ejphar.2008.10.014","article-title":"Inhibition of collagen-induced discoidin\ndomain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib","volume":"599","author":"Day","year":"2008","journal-title":"Eur. J. Pharmacol."},{"key":"2026090213583234200_cit36","doi-asserted-by":"publisher","first-page":"2730","DOI":"10.1021\/acschembio.7b00708","article-title":"Isoform-Selective\nATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode\nof Action","volume":"12","author":"Ferna\u0301ndez-Montalva\u0301n","year":"2017","journal-title":"ACS Chem. Biol."},{"key":"2026090213583234200_cit37","doi-asserted-by":"publisher","first-page":"7299","DOI":"10.1021\/acs.jmedchem.6b00746","article-title":"Discovery and Characterization of\na Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate\nSynthase","volume":"59","author":"Concha","year":"2016","journal-title":"J. Med. Chem."},{"key":"2026090213583234200_cit38","doi-asserted-by":"publisher","first-page":"234","DOI":"10.1021\/acscombsci.7b00023","article-title":"Analysis of Current DNA Encoded Library Screening Data\nIndicates Higher False Negative Rates for Numerically Larger Libraries","volume":"19","author":"Satz","year":"2017","journal-title":"ACS Comb. Sci."},{"key":"2026090213583234200_cit39","doi-asserted-by":"publisher","first-page":"131","DOI":"10.1038\/nrd.2016.213","article-title":"DNA-encoded\nchemistry: enabling the deeper sampling of chemical space","volume":"16","author":"Goodnow","year":"2017","journal-title":"Nat. Rev. Drug Discovery"},{"key":"2026090213583234200_cit40","doi-asserted-by":"publisher","first-page":"864","DOI":"10.1002\/cbic.201600573","article-title":"Discovery of a Potent BTK Inhibitor with a Novel Binding\nMode by Using Parallel Selections with a DNA-Encoded Chemical Library","volume":"18","author":"Cuozzo","year":"2017","journal-title":"ChemBioChem"},{"key":"2026090213583234200_cit41","doi-asserted-by":"publisher","first-page":"8014","DOI":"10.1039\/C5CC01230A","article-title":"Interrogating target-specificity\nby parallel screening of a DNA-encoded chemical library against closely\nrelated proteins","volume":"51","author":"Franzini","year":"2015","journal-title":"Chem. Commun."},{"key":"2026090213583234200_cit42","doi-asserted-by":"publisher","first-page":"172","DOI":"10.1038\/ki.2012.20","article-title":"Targeted\nproximal tubule injury triggers interstitial fibrosis and glomerulosclerosis","volume":"82","author":"Grgic","year":"2012","journal-title":"Kidney Int."},{"key":"2026090213583234200_cit43","doi-asserted-by":"publisher","first-page":"632","DOI":"10.2353\/ajpath.2010.091012","article-title":"Tubular overexpression\nof transforming growth factor-beta1 induces autophagy and fibrosis\nbut not mesenchymal transition of renal epithelial cells","volume":"177","author":"Koesters","year":"2010","journal-title":"Am. J. Pathol."},{"key":"2026090213583234200_cit44","unstructured":"Rubel, R. G. D., Mueller, G. A., and Gross, O. Paper presented at the ASN Kidney\nWeek 2017, New Orleans, LA, USA, 2017."},{"key":"2026090213583234200_cit45","doi-asserted-by":"publisher","first-page":"5","DOI":"10.1007\/s00467-012-2138-4","article-title":"Clinical practice recommendations\nfor the treatment of Alport syndrome: a statement of the Alport Syndrome\nResearch Collaborative","volume":"28","author":"Kashtan","year":"2013","journal-title":"Pediatr. Nephrol."},{"key":"2026090213583234200_cit46","doi-asserted-by":"publisher","first-page":"436046","DOI":"10.5402\/2012\/436046","article-title":"Safety and\nEfficacy of the ACE-Inhibitor Ramipril in Alport Syndrome: The Double-Blind,\nRandomized, Placebo-Controlled, Multicenter Phase III EARLY PRO-TECT\nAlport Trial in Pediatric Patients","volume":"2012","author":"Gross","year":"2012","journal-title":"ISRN Pediatr."},{"key":"2026090213583234200_cit47","doi-asserted-by":"publisher","first-page":"205","DOI":"10.1016\/j.ejphar.2015.03.026","article-title":"Translational\nvalue of animal models of kidney failure","volume":"759","author":"Ortiz","year":"2015","journal-title":"Eur.\nJ. Pharmacol."},{"key":"2026090213583234200_cit48","doi-asserted-by":"publisher","first-page":"F375","DOI":"10.1152\/ajprenal.00266.2016","article-title":"A perspective on\nchronic kidney disease progression","volume":"312","author":"Zhong","year":"2017","journal-title":"Am. J. Physiol."},{"key":"2026090213583234200_cit49","doi-asserted-by":"publisher","first-page":"266","DOI":"10.1038\/sj.ki.5002033","article-title":"Tandem mass spectrometry measurements of creatinine\nin mouse plasma and urine for determining glomerular filtration rate","volume":"71","author":"Takahashi","year":"2007","journal-title":"Kidney Int."},{"key":"2026090213583234200_cit50","doi-asserted-by":"publisher","first-page":"15","DOI":"10.1006\/cbir.1996.0004","article-title":"Structural\nbiology of the fibres of the collagenous and elastic systems","volume":"20","author":"Montes","year":"1996","journal-title":"Cell. Biol. Int."}],"container-title":["ACS Chemical Biology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/pubs.acs.org\/doi\/pdf\/10.1021\/acschembio.8b00866","content-type":"application\/pdf","content-version":"vor","intended-application":"unspecified"},{"URL":"https:\/\/pubs.acs.org\/acbcct\/article-pdf\/14\/1\/37\/66949316\/acschembio.8b00866.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/pubs.acs.org\/acbcct\/article-pdf\/14\/1\/37\/66949316\/acschembio.8b00866.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,9,2]],"date-time":"2026-09-02T17:58:39Z","timestamp":1788371919000},"score":1,"resource":{"primary":{"URL":"https:\/\/pubs.acs.org\/acbcct\/article\/14\/1\/37\/797871\/DNA-Encoded-Library-Derived-DDR1-Inhibitor"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2018,11,19]]},"references-count":50,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2018,11,19]]},"published-print":{"date-parts":[[2019,1,18]]}},"URL":"https:\/\/doi.org\/10.1021\/acschembio.8b00866","relation":{},"ISSN":["1554-8929","1554-8937"],"issn-type":[{"value":"1554-8929","type":"print"},{"value":"1554-8937","type":"electronic"}],"subject":[],"published":{"date-parts":[[2018,11,19]]}}}