List of works - James W. Janetka

A FimH inhibitor prevents acute bladder infection and treats chronic cystitis caused by multidrug-resistant uropathogenic Escherichia coli ST131.

scientific article published on 03 June 2013

A cyclic side-chain-linked biphenyl ether tripeptide: H3N(+)-cyclo-[Phe(4-O)Phe-Phe(3-O)]-OMe.Cl-

scientific article published on 01 December 1996

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies

scientific article

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

scientific article

Antivirulence C-Mannosides as Antibiotic-Sparing, Oral Therapeutics for Urinary Tract Infections

scientific article published on 30 September 2016

Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI.

scientific article published on 26 January 2016

Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through Iterative Rational Drug Design

scientific article published on 02 January 2019

Characterization of parasite-specific indels and their proposed relevance for selective anthelminthic drug targeting.

scientific article published on 29 January 2016

Checkpoint kinase inhibitors: a review of the patent literature

scientific article published on February 2009

Click Chemistry Reagent for Identification of Sites of Covalent Ligand Incorporation in Integral Membrane Proteins.

scientific article

Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice.

scientific article

Death by releasing the breaks: CHK1 inhibitors as cancer therapeutics

scientific article

Diaryldimethylpiperazine ligands with mu- and delta-opioid receptor affinity: Synthesis of (+)-4-[(alphaR)-alpha-(4-allyl-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide and (-)-4-[(alphaR)-alpha-(2S,5S)-dimethylpi

scientific article

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology

scientific article published on 04 January 2019

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

scientific article published on 6 May 2008

Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration

scientific article

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas

scientific article

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

scientific article published on 30 April 2012

Distinguishing the contribution of type 1 pili from that of other QseB-misregulated factors when QseC is absent during urinary tract infection.

scientific article

Enantioconvergent synthesis of (-)-(2R,5S)-1-allyl-2,5-dimethylpiperazine, an intermediate to delta-opioid receptor ligands

scientific article

Evolutionary fine-tuning of conformational ensembles in FimH during host-pathogen interactions.

scientific article

Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors

scientific article

Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment

scientific article published on 17 April 2017

Human Urine Decreases Function and Expression of Type 1 Pili in Uropathogenic Escherichia coli.

scientific article published on 30 June 2015

Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics

scientific article published on 24 June 2019

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

scientific article published on 28 December 2015

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

scientific article published on 21 September 2017

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer

scientific article published on 9 October 2014

Keeping checkpoint kinases in line: new selective inhibitors in clinical trials

scientific article published in September 2008

Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides

scientific article

MFN2 agonists reverse mitochondrial defects in preclinical models of Charcot-Marie-Tooth disease type 2A.

scientific article published in April 2018

Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn's disease.

scientific article

Photoaffinity labeling with cholesterol analogues precisely maps a cholesterol-binding site in voltage-dependent anion channel-1.

scientific article

Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin

scientific article published on 18 July 2019

Precision antimicrobial therapeutics: the path of least resistance?

scientific article

Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn's disease

scientific article

Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist.

scientific article published on 14 June 2017

Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics

scientific article published on 14 May 2018

Structure-based discovery of glycomimetic FmlH ligands as inhibitors of bacterial adhesion during urinary tract infection.

scientific article

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.

scientific article published on 4 April 2015

Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation.

scientific article published on 29 May 2017

Treatment and Prevention of Urinary Tract Infection with Orally Active FimH Inhibitors ⬇️

scientific article published on November 16, 2011

α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer

scientific article published on 17 February 2016

List of works by James W. Janetka

A FimH inhibitor prevents acute bladder infection and treats chronic cystitis caused by multidrug-resistant uropathogenic Escherichia coli ST131.

A cyclic side-chain-linked biphenyl ether tripeptide: H3N(+)-cyclo-[Phe(4-O)Phe-Phe(3-O)]-OMe.Cl-

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Antivirulence C-Mannosides as Antibiotic-Sparing, Oral Therapeutics for Urinary Tract Infections

Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI.

Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through Iterative Rational Drug Design

Characterization of parasite-specific indels and their proposed relevance for selective anthelminthic drug targeting.

Checkpoint kinase inhibitors: a review of the patent literature

Click Chemistry Reagent for Identification of Sites of Covalent Ligand Incorporation in Integral Membrane Proteins.

Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice.

Death by releasing the breaks: CHK1 inhibitors as cancer therapeutics

Diaryldimethylpiperazine ligands with mu- and delta-opioid receptor affinity: Synthesis of (+)-4-[(alphaR)-alpha-(4-allyl-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide and (-)-4-[(alphaR)-alpha-(2S,5S)-dimethylpi

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

Distinguishing the contribution of type 1 pili from that of other QseB-misregulated factors when QseC is absent during urinary tract infection.

Enantioconvergent synthesis of (-)-(2R,5S)-1-allyl-2,5-dimethylpiperazine, an intermediate to delta-opioid receptor ligands

Evolutionary fine-tuning of conformational ensembles in FimH during host-pathogen interactions.

Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors

Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment

Human Urine Decreases Function and Expression of Type 1 Pili in Uropathogenic Escherichia coli.

Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer

Keeping checkpoint kinases in line: new selective inhibitors in clinical trials

Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides

MFN2 agonists reverse mitochondrial defects in preclinical models of Charcot-Marie-Tooth disease type 2A.

Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn's disease.

Photoaffinity labeling with cholesterol analogues precisely maps a cholesterol-binding site in voltage-dependent anion channel-1.

Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin

Precision antimicrobial therapeutics: the path of least resistance?

Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn's disease

Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist.

Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics

Structure-based discovery of glycomimetic FmlH ligands as inhibitors of bacterial adhesion during urinary tract infection.

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.

Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation.

Treatment and Prevention of Urinary Tract Infection with Orally Active FimH Inhibitors ⬇️

α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer