List of works - Mark Ultsch

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

scientific article

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

scientific article

A new regulatory switch in a JAK protein kinase ⬇️

scientific article published on February 1, 2011

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

scientific article

Antibodies specific for a segment of human membrane IgE deplete IgE-producing B cells in humanized mice

scientific article

Antiparallel conformation of knob and hole aglycosylated half-antibody homodimers is mediated by a CH2-CH3 hydrophobic interaction

scientific article

Bcl10 activates the NF-kappaB pathway through ubiquitination of NEMO

scientific article

Development and preclinical characterization of a humanized antibody targeting CXCL12

scientific article

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2

scientific article

Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors ⬇️

scientific article published on October 24, 2012

Generation of a high-fidelity antibody against nerve growth factor using library scanning mutagenesis and validation with structures of the initial and optimized Fab-antigen complexes

scientific article

Glycan Shifting on Hepatitis C Virus (HCV) E2 Glycoprotein Is a Mechanism for Escape from Broadly Neutralizing Antibodies ⬇️

scientific article published on February 28, 2013

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

scientific article

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

scientific article

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors

scientific article

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

scientific article

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

scientific article

Lead identification of novel and selective TYK2 inhibitors

scientific article

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors

scientific article

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

scientific article

Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta ⬇️

scientific article published on August 21, 2012

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf ⬇️

scientific article published on May 17, 2012

Structural Basis of Signaling Blockade by Anti-IL-13 Antibody Lebrikizumab ⬇️

scientific article published on January 25, 2013

Structural and Functional Analysis of HtrA1 and Its Subdomains ⬇️

scientific article published on May 10, 2012

Structural basis for high-affinity HER2 receptor binding by an engineered protein

scientific article

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479

scientific article

Structure of a phage display-derived variant of human growth hormone complexed to two copies of the extracellular domain of its receptor: evidence for strong structural coupling between receptor binding sites

scientific article

Structure of the complex between HER2 and an antibody paratope formed by side chains from tryptophan and serine

scientific article

Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition

scientific article

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2

scientific article

List of works by Mark Ultsch

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

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

A new regulatory switch in a JAK protein kinase ⬇️

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

Antibodies specific for a segment of human membrane IgE deplete IgE-producing B cells in humanized mice

Antiparallel conformation of knob and hole aglycosylated half-antibody homodimers is mediated by a CH2-CH3 hydrophobic interaction

Bcl10 activates the NF-kappaB pathway through ubiquitination of NEMO

Development and preclinical characterization of a humanized antibody targeting CXCL12

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2

Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors ⬇️

Generation of a high-fidelity antibody against nerve growth factor using library scanning mutagenesis and validation with structures of the initial and optimized Fab-antigen complexes

Glycan Shifting on Hepatitis C Virus (HCV) E2 Glycoprotein Is a Mechanism for Escape from Broadly Neutralizing Antibodies ⬇️

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

Lead identification of novel and selective TYK2 inhibitors

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta ⬇️

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf ⬇️

Structural Basis of Signaling Blockade by Anti-IL-13 Antibody Lebrikizumab ⬇️

Structural and Functional Analysis of HtrA1 and Its Subdomains ⬇️

Structural basis for high-affinity HER2 receptor binding by an engineered protein

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479

Structure of a phage display-derived variant of human growth hormone complexed to two copies of the extracellular domain of its receptor: evidence for strong structural coupling between receptor binding sites

Structure of the complex between HER2 and an antibody paratope formed by side chains from tryptophan and serine

Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2