List of works - Andreas Kuglstatter

3-Amido Pyrrolopyrazine JAK Kinase Inhibitors: Development of a JAK3 vs JAK1 Selective Inhibitor and Evaluation in Cellular and in Vivo Models ⬇️

scientific article published on December 19, 2012

A Real-World Perspective on Molecular Design

scientific article

Crystal structure of SRP19 in complex with the S domain of SRP RNA and its implication for the assembly of the signal recognition particle

scientific article

Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation

scientific article

Cutting Edge: IL-1 receptor-associated kinase 4 structures reveal novel features and multiple conformations

scientific article

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead

scientific article

Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties ⬇️

scientific article published on April 21, 2013

Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys

scientific article

Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors ⬇️

scientific article published on March 14, 2013

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold

scientific article

Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds

scientific article

Induced structural changes of 7SL RNA during the assembly of human signal recognition particle

scientific article

Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures ⬇️

scientific article published on February 1, 2011

Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones

scientific article

Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors ⬇️

scientific article published on February 12, 2013

Rational design of highly selective spleen tyrosine kinase inhibitors

scientific article

Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines

scientific article

Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome ⬇️

scientific article published on February 13, 2013

Structural basis for the cyclophilin A binding affinity and immunosuppressive potency ofE-ISA247 (voclosporin) ⬇️

scientific article published on January 15, 2011

Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes

scientific article

Structure and assembly of the spliceosomal snRNPs. Novartis Medal Lecture

scientific article (publication date: May 2001)

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis

scientific article

The crystal structure of JNK2 reveals conformational flexibility in the MAP kinase insert and indicates its involvement in the regulation of catalytic activity

scientific article

Tyramine fragment binding to BACE-1

scientific article

X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors

scientific article

X-ray structure analyses of photosynthetic reaction center variants from Rhodobacter sphaeroides: structural changes induced by point mutations at position L209 modulate electron and proton transfer

scientific article

β-Secretase (BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer’s Disease ⬇️

scientific article published on May 2, 2013

List of works by Andreas Kuglstatter

3-Amido Pyrrolopyrazine JAK Kinase Inhibitors: Development of a JAK3 vs JAK1 Selective Inhibitor and Evaluation in Cellular and in Vivo Models ⬇️

A Real-World Perspective on Molecular Design

Crystal structure of SRP19 in complex with the S domain of SRP RNA and its implication for the assembly of the signal recognition particle

Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation

Cutting Edge: IL-1 receptor-associated kinase 4 structures reveal novel features and multiple conformations

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead

Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties ⬇️

Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys

Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors ⬇️

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold

Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds

Induced structural changes of 7SL RNA during the assembly of human signal recognition particle

Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures ⬇️

Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones

Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors ⬇️

Rational design of highly selective spleen tyrosine kinase inhibitors

Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines

Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome ⬇️

Structural basis for the cyclophilin A binding affinity and immunosuppressive potency ofE-ISA247 (voclosporin) ⬇️

Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes

Structure and assembly of the spliceosomal snRNPs. Novartis Medal Lecture

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis

The crystal structure of JNK2 reveals conformational flexibility in the MAP kinase insert and indicates its involvement in the regulation of catalytic activity

Tyramine fragment binding to BACE-1

X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors

X-ray structure analyses of photosynthetic reaction center variants from Rhodobacter sphaeroides: structural changes induced by point mutations at position L209 modulate electron and proton transfer

β-Secretase (BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer’s Disease ⬇️