List of works - Laszlo Orfi

A closer look at the structure of sterically stabilized liposomes: a small-angle X-ray scattering study.

scientific article published in May 2010

A novel drug discovery concept for tuberculosis: inhibition of bacterial and host cell signalling.

scientific article

A novel normalized retention factor in micellar electrokinetic chromatography

scientific article published on 01 June 1999

AXL is a potential target for therapeutic intervention in breast cancer progression.

scientific article

Acid-base profiling of imatinib (gleevec) and its fragments.

scientific article published in January 2005

Activation of HER3 interferes with antitumor effects of Axl receptor tyrosine kinase inhibitors: suggestion of combination therapy.

scientific article

Anticytolytic screen identifies inhibitors of mycobacterial virulence protein secretion.

scientific article

Binding specificity of the L-arginine transport systems in mouse macrophages and human cells overexpressing the cationic amino acid transporter hCAT-1.

scientific article

Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor

scientific article published on 01 January 2008

Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors.

scientific article

Characterization of binding mode of imatinib to human α1-acid glycoprotein.

scientific article

Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors

scientific article published in January 2005

Comparison of the cytotoxic effects of receptor tyrosine kinase inhibitors on macrophage functions; possible side effects in the immune defense

scientific article published on 18 October 2006

Delivery of the p38 MAPkinase inhibitor SB202190 to angiogenic endothelial cells: development of novel RGD-equipped and PEGylated drug-albumin conjugates using platinum(II)-based drug linker technology

scientific article published on September 2006

Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells

scientific article published on 12 December 2015

Determination of human serum alpha1-acid glycoprotein and albumin binding of various marketed and preclinical kinase inhibitors.

scientific article published on January 2009

Developing FGFR4 Inhibitors As Potential Anti-Cancer Agents Via In Silico Design, Supported by In Vitro and Cell-Based Testing ⬇️

scientific article published on January 1, 2013

Development of a 3D Tissue Culture-Based High-Content Screening Platform That Uses Phenotypic Profiling to Discriminate Selective Inhibitors of Receptor Tyrosine Kinases.

scientific article published on 7 July 2016

Development of a cell-selective and intrinsically active multikinase inhibitor bioconjugate.

scientific article

Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors

scientific article published on 09 July 2018

Drug discovery in the kinase inhibitory field using the Nested Chemical Library technology.

scientific article published in October 2005

Evaluation of lipophilicity and antitumour activity of parallel carboxamide libraries.

scientific article

HER2 Mediates PSMA/mGluR1-Driven Resistance to the DS-7423 Dual PI3K/mTOR Inhibitor in PTEN Wild-type Prostate Cancer Models

scientific article published on 01 April 2022

Heterocondensed quinazolones: synthesis and protein-tyrosine kinase inhibitory activity of 3,4-dihydro-1H,6H-[1,4] oxazino-[3,4-b]quinazolin-6-one derivatives

scientific article published on 01 April 1996

Integrating molecular diagnostics into anticancer drug discovery.

scientific article published on 7 June 2010

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library

scientific article published on 28 February 2015

Leads for antitubercular compounds from kinase inhibitor library screens

scientific journal article

Local inhibition of liver fibrosis by specific delivery of a platelet-derived growth factor kinase inhibitor to hepatic stellate cells

scientific article published on 16 March 2007

Machine learning and docking models for Mycobacterium tuberculosis topoisomerase I.

scientific article

Measurement of SDS Micelle-Peptide Association Using (1)H NMR Chemical Shift Analysis and Pulsed-Field Gradient NMR Spectroscopy

scientific article published on 01 April 1998

Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes

scientific article published on 28 November 2015

Nox4 contributes to the hypoxia-mediated regulation of actin cytoskeleton in cerebrovascular smooth muscle

scientific article published on 21 August 2016

Optimization of important early ADME(T) parameters of NADPH oxidase-4 inhibitor molecules.

scientific article

Optimized conversion of antiproliferative lignans pinoresinol and epipinoresinol: Their simultaneous isolation and identification by centrifugal partition chromatography and high performance liquid chromatography

scientific article published on 31 March 2017

Pharmacophore and binding analysis of known and novel B-RAF kinase inhibitors.

scientific article

Physicochemical characterization of psychosine by 1H nuclear magnetic resonance and electron microscopy ⬇️

scientific article published on October 1, 1997

Prediction oriented QSAR modelling of EGFR inhibition.

scientific article published in January 2006

Pro-apoptotic and anti-apoptotic molecules affecting pathways of signal transduction.

scientific article published in December 2003

Protein kinase inhibitor as a potential candidate for epilepsy treatment

scientific article published on 03 March 2011

Protein kinase inhibitor-induced endothelial cell cytotoxicity and its prediction based on calculated molecular descriptors.

scientific article

Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling.

scientific article published in August 2005

Rational design of RGD-albumin conjugates for targeted delivery of the VEGF-R kinase inhibitor PTK787 to angiogenic endothelium.

scientific article

Screening for MAPK modulators using an in-cell western assay

scientific article

Signalling inhibitors against Mycobacterium tuberculosis--early days of a new therapeutic concept in tuberculosis.

scientific article

Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes

scientific journal article

Small-Molecule Inhibitors of NADPH Oxidase 4 ⬇️

scientific article published on September 23, 2010

Structure -activity relationships of PDE5 inhibitors.

scientific article published on January 2008

Synthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines.

scientific article

Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases

scientific article published on 01 January 2008

Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.

scientific article published on 2 May 2014

Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.

scientific article published in July 2005

TP53 mutation-correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53-mutated breast cancers.

scientific article published on 5 January 2014

TT232, a novel signal transduction inhibitory compound in the therapy of cancer and inflammatory diseases.

scientific article

Targeting of a platinum-bound sunitinib analog to renal proximal tubular cells ⬇️

scientific article published on January 31, 2012

Targeting of the VEGF-kinase inhibitor PTK787 to angiogenic vasculature using RGD-equipped albumin carrier molecules

scientific article published on 01 November 2006

Two antithrombotic quinazolone derivatives

scientific article published in April 1995

Tyrphostin induces non-apoptotic programmed cell death in colon tumor cells

scientific article published on 01 November 1995

Validation subset selections for extrapolation oriented QSPAR models.

scientific article published in January 2003

List of works by Laszlo Orfi

A closer look at the structure of sterically stabilized liposomes: a small-angle X-ray scattering study.

A novel drug discovery concept for tuberculosis: inhibition of bacterial and host cell signalling.

A novel normalized retention factor in micellar electrokinetic chromatography

AXL is a potential target for therapeutic intervention in breast cancer progression.

Acid-base profiling of imatinib (gleevec) and its fragments.

Activation of HER3 interferes with antitumor effects of Axl receptor tyrosine kinase inhibitors: suggestion of combination therapy.

Anticytolytic screen identifies inhibitors of mycobacterial virulence protein secretion.

Binding specificity of the L-arginine transport systems in mouse macrophages and human cells overexpressing the cationic amino acid transporter hCAT-1.

Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor

Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors.

Characterization of binding mode of imatinib to human α1-acid glycoprotein.

Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors

Comparison of the cytotoxic effects of receptor tyrosine kinase inhibitors on macrophage functions; possible side effects in the immune defense

Delivery of the p38 MAPkinase inhibitor SB202190 to angiogenic endothelial cells: development of novel RGD-equipped and PEGylated drug-albumin conjugates using platinum(II)-based drug linker technology

Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells

Determination of human serum alpha1-acid glycoprotein and albumin binding of various marketed and preclinical kinase inhibitors.

Developing FGFR4 Inhibitors As Potential Anti-Cancer Agents Via In Silico Design, Supported by In Vitro and Cell-Based Testing ⬇️

Development of a 3D Tissue Culture-Based High-Content Screening Platform That Uses Phenotypic Profiling to Discriminate Selective Inhibitors of Receptor Tyrosine Kinases.

Development of a cell-selective and intrinsically active multikinase inhibitor bioconjugate.

Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors

Drug discovery in the kinase inhibitory field using the Nested Chemical Library technology.

Evaluation of lipophilicity and antitumour activity of parallel carboxamide libraries.

HER2 Mediates PSMA/mGluR1-Driven Resistance to the DS-7423 Dual PI3K/mTOR Inhibitor in PTEN Wild-type Prostate Cancer Models

Heterocondensed quinazolones: synthesis and protein-tyrosine kinase inhibitory activity of 3,4-dihydro-1H,6H-[1,4] oxazino-[3,4-b]quinazolin-6-one derivatives

Integrating molecular diagnostics into anticancer drug discovery.

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library

Leads for antitubercular compounds from kinase inhibitor library screens

Local inhibition of liver fibrosis by specific delivery of a platelet-derived growth factor kinase inhibitor to hepatic stellate cells

Machine learning and docking models for Mycobacterium tuberculosis topoisomerase I.

Measurement of SDS Micelle-Peptide Association Using (1)H NMR Chemical Shift Analysis and Pulsed-Field Gradient NMR Spectroscopy

Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes

Nox4 contributes to the hypoxia-mediated regulation of actin cytoskeleton in cerebrovascular smooth muscle

Optimization of important early ADME(T) parameters of NADPH oxidase-4 inhibitor molecules.

Optimized conversion of antiproliferative lignans pinoresinol and epipinoresinol: Their simultaneous isolation and identification by centrifugal partition chromatography and high performance liquid chromatography

Pharmacophore and binding analysis of known and novel B-RAF kinase inhibitors.

Physicochemical characterization of psychosine by 1H nuclear magnetic resonance and electron microscopy ⬇️

Prediction oriented QSAR modelling of EGFR inhibition.

Pro-apoptotic and anti-apoptotic molecules affecting pathways of signal transduction.

Protein kinase inhibitor as a potential candidate for epilepsy treatment

Protein kinase inhibitor-induced endothelial cell cytotoxicity and its prediction based on calculated molecular descriptors.

Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling.

Rational design of RGD-albumin conjugates for targeted delivery of the VEGF-R kinase inhibitor PTK787 to angiogenic endothelium.

Screening for MAPK modulators using an in-cell western assay

Signalling inhibitors against Mycobacterium tuberculosis--early days of a new therapeutic concept in tuberculosis.

Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes

Small-Molecule Inhibitors of NADPH Oxidase 4 ⬇️

Structure -activity relationships of PDE5 inhibitors.

Synthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines.

Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases

Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.

Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.

TP53 mutation-correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53-mutated breast cancers.

TT232, a novel signal transduction inhibitory compound in the therapy of cancer and inflammatory diseases.

Targeting of a platinum-bound sunitinib analog to renal proximal tubular cells ⬇️

Targeting of the VEGF-kinase inhibitor PTK787 to angiogenic vasculature using RGD-equipped albumin carrier molecules

Two antithrombotic quinazolone derivatives

Tyrphostin induces non-apoptotic programmed cell death in colon tumor cells

Validation subset selections for extrapolation oriented QSPAR models.