J. Kallen

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Structural States of Hdm2 and HdmX: X‐ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes

Joseph Schoepfer, Joerg Kallen, Pascal Furet, 2019, ChemMedChem.

The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.

P. Furet, A. de Pover, P. Chène, 2012, Bioorganic & Medicinal Chemistry Letters.

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

S. Urwyler, W. Froestl, K. Lingenhoehl, 2012, Bioorganic & medicinal chemistry letters.

Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.

B. Fournier, J. Renaud, C. Halleux, 2003, Journal of medicinal chemistry.

X-Ray Structure of the hROR LBD at 1 . 63 Å : Structural and Functional Data that Cholesterol or a Cholesterol Derivative Is the Natural Ligand of ROR

M. Geiser, S. Geisse, B. Fournier, 2002 .

Effect of the acylation of TEAD4 on its interaction with co‐activators YAP and TAZ

D. Erdmann, P. Chène, T. Schmelzle, 2017, Protein science : a publication of the Protein Society.

Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface.

D. Erdmann, P. Furet, P. Chène, 2018 .

Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface

D. Erdmann, P. Furet, P. Chène, 2018, Protein science : a publication of the Protein Society.

Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.

M. Geiser, B. Fournier, J. Renaud, 2005, Journal of medicinal chemistry.

Conformational control of cyclosporin through substitution of the N-5 position. A new class of cyclosporin antagonists.

J. Kallen, J. France, C. Papageorgiou, 1997, Bioorganic & medicinal chemistry.

Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury.

Stephen M. Canham, John A. Tallarico, J. Tallarico, 2021, Cell chemical biology.

Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site

Joerg Kallen, Volker Brinkmann, Christian Bruns, 2001, Nature Medicine.

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.

A. Sauter, J. Díaz, A. Schmitz, 2004, Bioorganic & medicinal chemistry letters.

The X‐ray structure of a tetrapeptide bound to the active site of human cyclophilin A

M. Walkinshaw, J. Kallen, 1992, FEBS letters.

Sanglifehrins A, B, C and D, novel cyclophilin-binding compounds isolated from Streptomyces sp. A92-308110. II. Structure elucidation, stereochemistry and physico-chemical properties.

J. Kallen, J. Sanglier, L. Oberer, 1999, The Journal of antibiotics.

X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha.

M. Geiser, S. Geisse, B. Fournier, 2002, Structure.

Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.

C. Ehrhardt, J. Kallen, C Ehrhardt, 1998, Journal of medicinal chemistry.

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Joerg Kallen, Pascal Furet, Keiichi Masuya, 2015, Journal of medicinal chemistry.

Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.

P. Furet, G. Bold, A. de Pover, 2014, Bioorganic & medicinal chemistry letters.

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

A. Picard, S. Urwyler, K. Lingenhoehl, 2017, ChemMedChem.

Improved Lymphocyte Function-associated Antigen-1 (LFA-1) Inhibition by Statin Derivatives

J. Kallen, G. Weitz-Schmidt, J. Dawson, 2004, Journal of Biological Chemistry.

Structure of Human Cyclophilin A in Complex with the Novel Immunosuppressant Sanglifehrin A at 1.6 Å Resolution*

R. Sedrani, J. Kallen, J. Wagner, 2005, Journal of Biological Chemistry.

Three‐dimensional structure and actions of immunosuppressants and their immunophilins

K. Wüthrich, W. Braun, M. Walkinshaw, 1995, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

Evidence for ligand-independent transcriptional activation of the human estrogen-related receptor alpha (ERRalpha): crystal structure of ERRalpha ligand binding domain in complex with peroxisome proliferator-activated receptor coactivator-1alpha.

M. Geiser, Alain Schilb, V. Riou, 2004, The Journal of biological chemistry.

p53 dynamics vary between tissues and are linked with radiation sensitivity

Miles A. Miller, R. Weissleder, Y. Iwamoto, 2021, Nature Communications.

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Eric Y. Durand, W. Sellers, Philipp Holzer, 2018, Cancer research.

A distinct p53 target gene set predicts for response to the selective p53–HDM2 inhibitor NVP-CGM097

Hans Bitter, Joerg Kallen, Pascal Furet, 2015, eLife.

Structure-based and property-driven optimization of N-aryl imidazoles towards potent and selective oral RORγt inhibitors.

S. Hintermann, P. Ertl, M. Streiff, 2019, Journal of medicinal chemistry.

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.

Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.

S. Geisse, B. Fournier, J. Kallen, 2003, Analytical biochemistry.

Crystal Structure of Human Estrogen-related Receptor α in Complex with a Synthetic Inverse Agonist Reveals Its Novel Molecular Mechanism*

M. Geiser, M. Blommers, B. Fournier, 2007, Journal of Biological Chemistry.

Crystal Structure of the Human RORα Ligand Binding Domain in Complex with Cholesterol Sulfate at 2.2 Å*

B. Fournier, J. Kallen, F. Bitsch, 2004, Journal of Biological Chemistry.

Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo

S. Hintermann, K. Kaupmann, J. Kallen, 2017, PloS one.

X-Ray Structure of the hRORα LBD at 1.63 Å

M. Geiser, S. Geisse, B. Fournier, 2002 .

The x-ray crystal structure of the first RNA recognition motif and site-directed mutagenesis suggest a possible HuR redox sensing mechanism.

Manfred Auer, Joerg Kallen, Christian Ostermeier, 2010, Journal of molecular biology.

X‐ray Structures and Feasibility Assessment of CLK2 Inhibitors for Phelan–McDermid Syndrome

N. Stiefl, A. Elhajouji, Ivan Galimberti, 2018, ChemMedChem.

Cyclosporin A—cyclophilin complex formation A model based on X‐ray and NMR data

G. Wider, K. Wüthrich, W. Braun, 1992, FEBS letters.

Crystallisation and preliminary X‐ray diffraction studies of cyclophilin‐tetrapeptide and cyclophilin‐cyclosporin complexes

M. Walkinshaw, J. Jansonius, M. Zurini, 1990, FEBS letters.

Molecular and structural characterization of a TEAD mutation at the origin of Sveinsson's chorioretinal atrophy

D. Erdmann, P. Furet, P. Chène, 2019, The FEBS journal.

Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.

Y. Auberson, I. Vranesic, S. Urwyler, 2011, Bioorganic & medicinal chemistry letters.

Crystal Structures of Human MdmX (HdmX) in Complex with p53 Peptide Analogues Reveal Surprising Conformational Changes*

M. Geiser, P. Furet, A. Goepfert, 2009, Journal of Biological Chemistry.

Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

Philipp Holzer, P. Furet, P. Chène, 2016, Bioorganic & medicinal chemistry letters.

Structural States of RORγt: X‐ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds

S. Hintermann, K. Kaupmann, J. Kallen, 2017, ChemMedChem.

Synthesis and Biological Evaluation of New Triazolo‐ and Imidazolopyridine RORγt Inverse Agonists

S. Hintermann, A. Vulpetti, K. Kaupmann, 2016, ChemMedChem.

The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition

P. Furet, P. Chène, T. Schmelzle, 2022, ChemMedChem.

Abstract LB319: IAG933, a selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor with pre-clinical activity in monotherapy and combinations

P. Furet, F. Hofmann, Laurent Sansregret, 2023, Cancer Research.

Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP‐TEAD Protein‐Protein Interaction Inhibitors

P. Furet, P. Chène, T. Schmelzle, 2023, ChemMedChem.

Biochemical and Structural Characterization of a Peptidic Inhibitor of the YAP:TEAD Interaction That Binds to the α-Helix Pocket on TEAD.

P. Chène, Hanspeter Gubler, F. Villard, 2023, ACS chemical biology.

In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Philipp Holzer, P. Furet, S. Ferretti, 2018, Bioorganic & medicinal chemistry letters.

Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.

P. Furet, P. Chène, T. Schmelzle, 2019, Bioorganic & medicinal chemistry letters.

1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.

M. Sabio, C. Ehrhardt, U. Hommel, 2005, Bioorganic & medicinal chemistry letters.

Evidence for Ligand-independent Transcriptional Activation of the Human Estrogen-related Receptor α (ERRα)

M. Geiser, Alain Schilb, V. Riou, 2004, Journal of Biological Chemistry.

A distinct p53 target gene set predicts for response to the selective p53–HDM2 inhibitor NVP-CGM097

W. Sellers, Philipp Holzer, P. Furet, 2015, eLife.

Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.

E. Jacoby, Philipp Holzer, P. Furet, 2015, Bioorganic & medicinal chemistry letters.

Conformational polymorphism of cyclosporin A.

K Wüthrich, D Altschuh, K. Wüthrich, 1994, Structure.

Knowledge-based virtual screening: application to the MDM4/p53 protein-protein interaction.

Nathan Brown, Edgar Jacoby, Caroline Engeloch, 2009, Methods in molecular biology.