@article{6973bf13d9424c43a216109d896ec50a,
title = "Quinoline and thiazolopyridine allosteric inhibitors of MALT1",
abstract = "Quinolines and thiazolopyridines were developed as allosteric inhibitors of MALT1, with good cellular potency and exquisite selectivity. Mouse pharmacokinetic (PK) profiling showed these to have low in vivo clearance, and moderate oral exposure. The thiazolopyridines were less lipophilic than the quinolines, and one thiazolopyridine example was active in our hIL10 mouse pharmacodynamic (PD) model upon oral dosing.",
keywords = "Allosteric, B-cell lymphomas, MALT1, Protease inhibitors",
author = "Scott, {David A.} and Hatcher, {John M.} and Hongyan Liu and Mingpeng Fu and Guangyan Du and Lorena Font{\'a}n and Ilkay Us and Gabriella Casalena and Qi Qiao and Hao Wu and Ari Melnick and Gray, {Nathanael S.}",
note = "Funding Information: Synthetic chemistry was partially conducted by Peptech Corporation (Shanghai). Microsome stability, aqueous solubility and PPB measurements were conducted by Janssen Pharmaceuticals. Mouse PK studies were conducted at the Drug Metabolism and Pharmacokinetics laboratory at The Scripps Research Institute, under the supervision of Dr Mike Cameron. Protease profiling was conducted at Genscript USA. This work was supported by funding from Janssen Pharmaceuticals and the NIH (R01 CA182736). We thank Milka Kostic for assistance with the manuscript. Funding Information: Synthetic chemistry was partially conducted by Peptech Corporation (Shanghai). Microsome stability, aqueous solubility and PPB measurements were conducted by Janssen Pharmaceuticals. Mouse PK studies were conducted at the Drug Metabolism and Pharmacokinetics laboratory at The Scripps Research Institute, under the supervision of Dr Mike Cameron. Protease profiling was conducted at Genscript USA. This work was supported by funding from Janssen Pharmaceuticals and the NIH ( R01 CA182736 ). We thank Milka Kostic for assistance with the manuscript. Publisher Copyright: {\textcopyright} 2019 Elsevier Ltd",
year = "2019",
month = jul,
day = "15",
doi = "10.1016/j.bmcl.2019.05.040",
language = "English (US)",
volume = "29",
pages = "1694--1698",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "14",
}