Kris A. Borzilleri

发表

Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.

R. Kurumbail, M. Harris, Hong Wang, 2014, Structure.

Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.

Kaihong Zhou, Spiros Liras, Meihua Tu, 2018, Journal of the American Chemical Society.

Delineating the role of cooperativity in the design of potent PROTACs for BTK

Graham M. West, James Smith, V. Shanmugasundaram, 2018, Proceedings of the National Academy of Sciences.

Spontaneous alpha-N-6-phosphogluconoylation of a "His tag" in Escherichia coli: the cause of extra mass of 258 or 178 Da in fusion proteins.

P. Lemotte, K. Geoghegan, H. Dixon, 1999, Analytical biochemistry.

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

R. Kurumbail, A. Kalgutkar, B. Feng, 2018, Journal of medicinal chemistry.

Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro.

M. Ammirati, D. Craik, David A. Price, 2014, Chemistry & biology.

Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).

G. S. Walker, R. Kurumbail, Jake E. Delmore, 2018, Journal of medicinal chemistry.

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.

Jessica Ward, Jun Xiao, David Hepworth, 2016, Journal of medicinal chemistry.

Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK).

J. Pandit, J. Culp, K. Parris, 2017, Journal of medicinal chemistry.

Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.

É. Hajós‐Korcsok, Claude Ambroise, K. Borzilleri, 2012, Journal of medicinal chemistry.

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

Stephen Brown, R. Horst, Yilin Meng, 2020, Nature Chemical Biology.

Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.

M. Mansour, S. Sakya, K. Borzilleri, 2009, Journal of medicinal chemistry.

Driving Drug Discovery with Biophysical Information

G. Karam, V. Shanmugasundaram, A. Palmer, 2017 .

Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design.

M. Mansour, J. Pandit, BinQing Wei, 2012, Journal of medicinal chemistry.

Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.

R. Kurumbail, M. Harris, Hong Wang, 2014, Structure.

A covalent BTK ternary complex compatible with targeted protein degradation

R. Horst, K. Borzilleri, M. Calabrese, 2023, Nature Communications.