List of works - Charles Eigenbrot

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

scientific article

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

scientific article

A minimized M13 coat protein defines the requirements for assembly into the bacteriophage particle

scientific article

A new regulatory switch in a JAK protein kinase ⬇️

scientific article published on February 1, 2011

A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo

scientific article published on 4 January 2005

A trigger squeezed

scientific article published on 01 March 2008

A two-in-one antibody against HER3 and EGFR has superior inhibitory activity compared with monospecific antibodies

scientific article

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

scientific article

An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma

scientific article published on 01 October 2019

An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma

scientific article published on 01 January 2020

An allosteric switch for pro-HGF/Met signaling using zymogen activator peptides

scientific article

An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors

scientific article (publication date: September 2003)

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

Aspartate isomerization in the complementarity-determining regions of two closely related monoclonal antibodies

scientific article published on 17 January 2007

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations

scientific article

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

scientific article published on 26 August 2016

Conformational lability in serine protease active sites: structures of hepatocyte growth factor activator (HGFA) alone and with the inhibitory domain from HGFA inhibitor-1B

scientific article (publication date: 11 March 2005)

Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates.

scientific article published on 22 January 2012

Convergent recognition of the IgE binding site on the high-affinity IgE receptor

scientific article published in July 2004

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article published on 11 March 2016

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors

scientific article

Design of Organo-Peptides As Bipartite PCSK9 Antagonists

scientific article published on 30 January 2020

Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK)

scientific article

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

scientific article

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors

scientific article

Discovery of GDC-0853, a Potent, Selective, and Non-Covalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development

scientific article published on 19 February 2018

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

scientific article

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

scientific article

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

scientific article

Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.

scientific article published on 21 August 2017

Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

scientific article

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors

scientific article

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

scientific article

Disulfide locked variants of factor VIIa with a restricted beta-strand conformation have enhanced enzymatic activity

scientific article published in May 2005

Diverse somatic mutation patterns and pathway alterations in human cancers

scientific article (publication date: 12 August 2010)

Dual functionality of β-tryptase protomers as both proteases and cofactors in the active tetramer

scientific article published on 16 April 2018

Endocytosis and sorting of ErbB2 and the site of action of cancer therapeutics trastuzumab and geldanamycin

scientific article

Engineering exosite peptides for complete inhibition of factor VIIa using a protease switch with substrate phage

scientific article

Epidermal growth factor receptor in osteosarcoma: expression and mutational analysis

scientific article published on 23 May 2007

Framework selection can influence pharmacokinetics of a humanized therapeutic antibody through differences in molecule charge

scientific article

Function blocking antibodies to neuropilin-1 generated from a designed human synthetic antibody phage library

scientific article

Generation and characterization of a unique reagent that recognizes a panel of recombinant human monoclonal antibody therapeutics in the presence of endogenous human IgG

scientific article

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

Hepatocyte growth factor activator (HGFA): molecular structure and interactions with HGFA inhibitor-1 (HAI-1).

scientific article published on 09 April 2010

High-affinity human antibodies from phage-displayed synthetic Fab libraries with a single framework scaffold

scientific article

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 C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2

scientific article

Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor

scientific article

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.

scientific article published on 12 August 2017

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

Inhibitors of Tissue Factor. Factor VIIa for anticoagulant therapy

scientific article published in September 2004

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

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

scientific article

New insight into how tissue factor allosterically regulates factor VIIa

scientific article

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article

Oncogenic ERBB3 mutations in human cancers

scientific article

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

scientific article

Phage-displayed antibody libraries of synthetic heavy chain complementarity determining regions

scientific article

Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group

scientific article published on 11 April 2019

Pro-urokinase-type plasminogen activator is a substrate for hepsin

scientific article

Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors

scientific article

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

scientific article published on 17 December 2015

Rapid identification of reactive cysteine residues for site-specific labeling of antibody-Fabs

scientific article published on 14 January 2008

Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity

scientific article published on November 2016

Similar molecular interactions of factor VII and factor VIIa with the tissue factor region that allosterically regulates enzyme activity

scientific article published on February 2004

Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity

scientific article published on 13 July 2020

Structural and Functional Analysis of HtrA1 and Its Subdomains ⬇️

scientific article published on May 10, 2012

Structural and functional basis of the serine protease-like hepatocyte growth factor beta-chain in Met binding and signaling

scientific article published on 24 June 2004

Structural and mechanistic insight into how antibodies inhibit serine proteases.

scientific article published on September 2010

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

scientific article

Structural basis of signaling blockade by anti-IL-13 antibody Lebrikizumab

scientific article

Structural basis of the broadly neutralizing anti-interferon-α antibody rontalizumab

scientific article published on 22 June 2015

Structural insight into distinct mechanisms of protease inhibition by antibodies

scientific article

Structural insight into how an anti-idiotypic antibody against D3H44 (anti-tissue factor antibody) restores normal coagulation

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 Crenezumab Complex with Aβ Shows Loss of β-Hairpin

scientific article published on 20 December 2016

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

scientific article

Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor

scientific article

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

scientific article

Structure, function, and activation of coagulation factor VII.

scientific article

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

scientific article published on 22 December 2016

Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK)

scientific article

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

scientific article

Structures of neutrophil serine protease 4 reveal an unusual mechanism of substrate recognition by a trypsin-fold protease

scientific article

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo

scientific article

The ErbB4 extracellular region retains a tethered-like conformation in the absence of the tether

scientific article

The trimeric serine protease HtrA1 forms a cage-like inhibition complex with an anti-HtrA1 antibody

scientific article published on 18 September 2015

Tissue expression, protease specificity, and Kunitz domain functions of hepatocyte growth factor activator inhibitor-1B (HAI-1B), a new splice variant of HAI-1

scientific article (publication date: 19 September 2003)

Two-in-One antibodies with dual action Fabs

scientific article published on 14 May 2013

Unraveling the allosteric mechanism of serine protease inhibition by an antibody

scientific article

Unveiling a glycation hot spot in a recombinant humanized monoclonal antibody

scientific article

Utilizing the activation mechanism of serine proteases to engineer hepatocyte growth factor into a Met antagonist

scholarly article

Water molecules in protein-ligand interfaces. Evaluation of software tools and SAR comparison

scientific article published on 12 February 2019

List of works by Charles Eigenbrot

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

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

A minimized M13 coat protein defines the requirements for assembly into the bacteriophage particle

A new regulatory switch in a JAK protein kinase ⬇️

A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo

A trigger squeezed

A two-in-one antibody against HER3 and EGFR has superior inhibitory activity compared with monospecific antibodies

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma

An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma

An allosteric switch for pro-HGF/Met signaling using zymogen activator peptides

An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors

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

Aspartate isomerization in the complementarity-determining regions of two closely related monoclonal antibodies

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

Conformational lability in serine protease active sites: structures of hepatocyte growth factor activator (HGFA) alone and with the inhibitory domain from HGFA inhibitor-1B

Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates.

Convergent recognition of the IgE binding site on the high-affinity IgE receptor

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors

Design of Organo-Peptides As Bipartite PCSK9 Antagonists

Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK)

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

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors

Discovery of GDC-0853, a Potent, Selective, and Non-Covalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.

Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Disulfide locked variants of factor VIIa with a restricted beta-strand conformation have enhanced enzymatic activity

Diverse somatic mutation patterns and pathway alterations in human cancers

Dual functionality of β-tryptase protomers as both proteases and cofactors in the active tetramer

Endocytosis and sorting of ErbB2 and the site of action of cancer therapeutics trastuzumab and geldanamycin

Engineering exosite peptides for complete inhibition of factor VIIa using a protease switch with substrate phage

Epidermal growth factor receptor in osteosarcoma: expression and mutational analysis

Framework selection can influence pharmacokinetics of a humanized therapeutic antibody through differences in molecule charge

Function blocking antibodies to neuropilin-1 generated from a designed human synthetic antibody phage library

Generation and characterization of a unique reagent that recognizes a panel of recombinant human monoclonal antibody therapeutics in the presence of endogenous human IgG

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

Hepatocyte growth factor activator (HGFA): molecular structure and interactions with HGFA inhibitor-1 (HAI-1).

High-affinity human antibodies from phage-displayed synthetic Fab libraries with a single framework scaffold

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 C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2

Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.

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

Inhibitors of Tissue Factor. Factor VIIa for anticoagulant therapy

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

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

New insight into how tissue factor allosterically regulates factor VIIa

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Oncogenic ERBB3 mutations in human cancers

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

Phage-displayed antibody libraries of synthetic heavy chain complementarity determining regions

Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group

Pro-urokinase-type plasminogen activator is a substrate for hepsin

Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Rapid identification of reactive cysteine residues for site-specific labeling of antibody-Fabs

Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity

Similar molecular interactions of factor VII and factor VIIa with the tissue factor region that allosterically regulates enzyme activity

Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity

Structural and Functional Analysis of HtrA1 and Its Subdomains ⬇️

Structural and functional basis of the serine protease-like hepatocyte growth factor beta-chain in Met binding and signaling

Structural and mechanistic insight into how antibodies inhibit serine proteases.

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

Structural basis of signaling blockade by anti-IL-13 antibody Lebrikizumab

Structural basis of the broadly neutralizing anti-interferon-α antibody rontalizumab

Structural insight into distinct mechanisms of protease inhibition by antibodies