E. Vangrevelinghe

发表

A Small-Molecule Dengue Virus Entry Inhibitor

E. Jacoby, S. Vasudevan, W. Schul, 2009, Antimicrobial Agents and Chemotherapy.

Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking.

D. Fabbro, P. Furet, R. Portmann, 2003, Journal of medicinal chemistry.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition

Eric Vangrevelinghe, Andrew L. Kung, James E. Bradner, 2011, The Journal of experimental medicine.

An Integrated Approach for Fragment‐Based Lead Discovery: Virtual, NMR, and High‐Throughput Screening Combined with Structure‐Guided Design. Application to the Aspartyl Protease Renin.

Eric Vangrevelinghe, E. Vangrevelinghe, S. Rüdisser, 2016 .

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

A. Letai, S. Sallan, M. Harris, 2015, Cancer cell.

Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805

D. Erdmann, J. Brueggen, P. Furet, 2010, Molecular Cancer Therapeutics.

A Small-Molecule Dengue Virus Entry Inhibitor (cid:1) †

E. Jacoby, S. Vasudevan, W. Schul, 2009 .

Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.

E. Vangrevelinghe, J. Wagner, W. Schuler, 2017, Bioorganic & medicinal chemistry letters.

Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist.

T. Junt, P. Loetscher, E. Vangrevelinghe, 2022, ACS medicinal chemistry letters.

Identification and characterization of a phenyl-thiazolyl-benzoic acid derivative as a novel RAR/RXR agonist

T. Honda, S. Hatakeyama, T. Kanazawa, 2019, Heliyon.

Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.

T. Junt, P. Loetscher, E. Vangrevelinghe, 2020, Journal of Medicinal Chemistry.

3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology.

L Morin-Allory, P. Renard, C. Marot, 2000, Journal of medicinal chemistry.

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Eric Vangrevelinghe, Clive McCarthy, Pascal Furet, 2010, Bioorganic & medicinal chemistry letters.

Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.

L. Meijer, P. Furet, B. Chaudhuri, 2002, Journal of medicinal chemistry.

2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.

G. Rummel, S. Cowan-Jacob, E. Vangrevelinghe, 2011, Bioorganic & medicinal chemistry letters.

Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.

W. Sellers, R. Levine, F. Hofmann, 2012, Cancer discovery.

Genetic resistance to JAK 2 enzymatic inhibitors is overcome by HSP 90 inhibition

D. Erdmann, M. McKeown, J. Bradner, 2012 .

Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

S. Hintermann, R. Wolf, A. Vulpetti, 2018, Journal of medicinal chemistry.

An Activating Janus Kinase-3 Mutation Is Associated with Cytotoxic T Lymphocyte Antigen-4-Dependent Immune Dysregulation Syndrome

B. Linghu, E. Oakeley, M. Beibel, 2017, Front. Immunol..

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.

N. Waters, E. Vangrevelinghe, G. Hollingworth, 2014, Bioorganic & medicinal chemistry letters.

Discovery and profiling of a selective and efficacious Syk inhibitor.

Eric Vangrevelinghe, E. Vangrevelinghe, Christian C. Lee, 2015, Journal of medicinal chemistry.

A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.

Eric Vangrevelinghe, Markus Krömer, Edgar Jacoby, 2013, Journal of medicinal chemistry.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

C. Dekker, P. Chène, M. Eck, 2019, ACS chemical biology.

Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.

Eric Vangrevelinghe, E. Vangrevelinghe, R. Falchetto, 2011, Journal of medicinal chemistry.

Syk inhibitors with high potency in presence of blood.

Jianwei Che, E. Vangrevelinghe, Christian C. Lee, 2014, Bioorganic & medicinal chemistry letters.

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Eric Vangrevelinghe, Marc Lang, Pascal Furet, 2010, Bioorganic & medicinal chemistry letters.

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.

E. Vangrevelinghe, Christian C. Lee, G. Thoma, 2015, Bioorganic & medicinal chemistry letters.

Computational Approaches for Fragment Optimization

Eric Vangrevelinghe, Simon Rüdisser, E. Vangrevelinghe, 2007 .

2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.

G. Rummel, S. Cowan-Jacob, E. Vangrevelinghe, 2011, Bioorganic & medicinal chemistry letters.

Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.

E. Vangrevelinghe, G. Thoma, H. Zerwes, 2023, Journal of medicinal chemistry.

A Small-Molecule Dengue Virus Entry Inhibitor

E. Jacoby, S. Vasudevan, W. Schul, 2009, Antimicrobial Agents and Chemotherapy.