T. Kleinheinz

发表

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

C. Li, R. Rowntree, BinQing Wei, 2019, Bioorganic & medicinal chemistry letters.

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2012, Journal of medicinal chemistry.

A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.

Jennafer Dotson, Christian Wiesmann, Jason Drummond, 2009, Journal of medicinal chemistry.

Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.

Siew K. Yeap, N. C. Ray, Jun Liang, 2019, Bioorganic & medicinal chemistry letters.

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2014, Journal of medicinal chemistry.

Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2013, ACS medicinal chemistry letters.

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2020, ChemMedChem.

Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2020, ACS medicinal chemistry letters.

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Karen E Gascoigne, Fei Wang, S. Kharbanda, 2016, Journal of medicinal chemistry.

Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.

Matthew S. Johnson, M. Ultsch, J. Veal, 2022, Journal of medicinal chemistry.

A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.

Guy Georges, Elizabeth Blackwood, Christian Wiesmann, 2008, Journal of medicinal chemistry.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility

Mamie Yu, A. Daemen, R. Houtman, 2019, Cell.

USP7 small-molecule inhibitors interfere with ubiquitin binding

Florian Gnad, Scott E. Martin, Michelle R. Arkin, 2017, Nature.

Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.

A. Beresford, A. Medhurst, Xingrong Liu, 2019, Bioorganic & medicinal chemistry letters.

Ser1292 Autophosphorylation Is an Indicator of LRRK2 Kinase Activity and Contributes to the Cellular Effects of PD Mutations

K. Scearce-Levie, M. P. van der Brug, Xingrong Liu, 2012, Science Translational Medicine.

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Siew K. Yeap, N. C. Ray, Jun Liang, 2021, Journal of medicinal chemistry.

A Simple High-Content Cell Cycle Assay Reveals Frequent Discrepancies between Cell Number and ATP and MTS Proliferation Assays

Grace Ka Yan Chan, David A. Peterson, John G. Moffat, 2013, PloS one.

Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2021, Bioorganic & medicinal chemistry letters.

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2021, Journal of medicinal chemistry.

Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.

Jun Liang, J. Nwachukwu, K. Nettles, 2019, Bioorganic & medicinal chemistry letters.

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.

Melinda M. Mulvihill, R. Rowntree, Wentao Wei, 2021, Journal of medicinal chemistry.

Abstract 1648: Discovery and evolution of orally bioavailable selective estrogen receptor degraders for ER+ breast cancer: From GDC-0810 to GDC-0927

Jun Liang, A. Daemen, Andiliy G. Lai, 2018, Cancer Chemistry.

Targeted degradation via direct 26S proteasome recruitment

C. Ciferri, N. Popovych, I. Wertz, 2022, Nature Chemical Biology.

Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.

I. Wertz, P. Di Lello, L. Kategaya, 2017, Journal of medicinal chemistry.