Affiliation: Genentech Inc
- Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell lineYichin Liu
Center for Neurologic Diseases, Brigham and Women s Hospital, 65 Landsdowne Street, Cambridge, MA 02139, USA
Chem Biol 10:837-46. 2003..The molecular mechanism of this response remains to be determined...
- High-throughput assays for sirtuin enzymes: a microfluidic mobility shift assay and a bioluminescence assayYichin Liu
Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320 1799, USA
Anal Biochem 378:53-9. 2008..Kinetic parameters of peptide and NAD(+) cosubstrates and IC(50) values of standard reference inhibitors determined in either assay were similar. With robust Z' values (0.7), both assays are amenable to high-throughput screening...
- A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivoJasvinder K Atwal
Neurodegeneration Labs, Department of Neuroscience, Genentech, 1 DNA Way, South San Francisco, CA 94080, USA
Sci Transl Med 3:84ra43. 2011..Nevertheless, therapeutic success with anti-BACE1 will depend on improving antibody uptake into the brain...
- Case studies of minimizing nonspecific inhibitors in HTS campaigns that use assay-ready platesYichin Liu
Biochemical Pharmacology and Early Leads, Genentech, Inc, South San Francisco, CA 90480, USA
J Biomol Screen 17:225-36. 2012..These case studies support a model where a diversity set of compounds should be tested first for hit rates as a function of order of addition, carrier protein, and relevant mechanistic studies prior to launch of the HTS campaign...
- Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitorsDavid Meininger
Protein Sciences, Amgen Inc, Seattle, WA 98119, USA
Biochim Biophys Acta 1814:1947-54. 2011..Docking of Amg-1 and related analogs to the known structure of IDO1 and to homology-modeled IDO2 suggests possible rationales for the different inhibition profiles of IDO1 and IDO2...
- Differential effects of divalent manganese and magnesium on the kinase activity of leucine-rich repeat kinase 2 (LRRK2)Brian Lovitt
Biochemical Pharmacology and Early Leads, Genentech, Inc, One DNA Way, South San Francisco, California 90480, USA
Biochemistry 49:3092-100. 2010....
- Assessment of the integrity of compounds stored in assay-ready plates using a kinase sentinel assayAda Chen
Therapeutic Discovery, Amgen, Inc, 1120 Veterans Blvd, South San Francisco, CA 94080 USA
Comb Chem High Throughput Screen 16:644-51. 2013....
- Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modelingHuifen Chen
Discovery Chemistry Department, Genentech, Inc, 1 DNA Way, South San Francisco, California 94080, United States
J Med Chem 55:5536-45. 2012....
- Discovery of acetyl-coenzyme A carboxylase 2 inhibitors: comparison of a fluorescence intensity-based phosphate assay and a fluorescence polarization-based ADP Assay for high-throughput screeningYichin Liu
Amgen Inc, Thousand Oaks, CA 91320 1799, USA
Assay Drug Dev Technol 5:225-35. 2007..Acetyl-coenzyme A carboxylase inhibitors were identified by these high-throughput screening methods and were confirmed in a radiometric high performance liquid chromatography assay of malonyl-coenzyme A production...