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Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.
Boehm M, Beaumont K, Jones R, Kalgutkar AS, Zhang L, Atkinson K, Bai G, Brown JA, Eng H, Goetz GH, Holder BR, Khunte B, Lazzaro S, Limberakis C, Ryu S, Shapiro MJ, Tylaska L, Yan J, Turner R, Leung SSF, Ramaseshan M, Price DA, Liras S, Jacobson MP, Earp DJ, Lokey RS, Mathiowetz AM, Menhaji-Klotz E. Boehm M, et al. Among authors: jacobson mp. J Med Chem. 2017 Dec 14;60(23):9653-9663. doi: 10.1021/acs.jmedchem.7b01028. Epub 2017 Oct 30. J Med Chem. 2017. PMID: 29045152 Free article.
On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds.
White TR, Renzelman CM, Rand AC, Rezai T, McEwen CM, Gelev VM, Turner RA, Linington RG, Leung SS, Kalgutkar AS, Bauman JN, Zhang Y, Liras S, Price DA, Mathiowetz AM, Jacobson MP, Lokey RS. White TR, et al. Among authors: jacobson mp. Nat Chem Biol. 2011 Sep 25;7(11):810-7. doi: 10.1038/nchembio.664. Nat Chem Biol. 2011. PMID: 21946276 Free PMC article.
Testing physical models of passive membrane permeation.
Leung SS, Mijalkovic J, Borrelli K, Jacobson MP. Leung SS, et al. Among authors: jacobson mp. J Chem Inf Model. 2012 Jun 25;52(6):1621-36. doi: 10.1021/ci200583t. Epub 2012 May 24. J Chem Inf Model. 2012. PMID: 22621168 Free PMC article.
Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target.
Choy JW, Bryant C, Calvet CM, Doyle PS, Gunatilleke SS, Leung SS, Ang KK, Chen S, Gut J, Oses-Prieto JA, Johnston JB, Arkin MR, Burlingame AL, Taunton J, Jacobson MP, McKerrow JM, Podust LM, Renslo AR. Choy JW, et al. Among authors: jacobson mp. Beilstein J Org Chem. 2013;9:15-25. doi: 10.3762/bjoc.9.3. Epub 2013 Jan 4. Beilstein J Org Chem. 2013. PMID: 23400640 Free PMC article.
203 results