List of works - Andreas Koeberle

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

scientific article published on 4 January 2016

A Multicomponent Carba-Betti Strategy to Alkylidene Heterodimers - Total Synthesis and Structure-Activity Relationships of Arzanol

Acetyl-CoA carboxylase 1 regulates endothelial cell migration by shifting the phospholipid composition

scientific article published on 5 December 2017

Analgesic potential of standardized methanol stem bark extract of Ficus platyphylla in mice: Mechanisms of action

scientific article

Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males

scientific article

Aneuploidy-inducing gene knockdowns overlap with cancer mutations and identify Orp3 as a B-cell lymphoma suppressor

scientific article published on 28 October 2019

Anti-inflammatory and analgesic activity of carnosol and carnosic acid in vivo and in vitro and in silico analysis of their target interactions.

scientific article

Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding ⬇️

scientific article published on January 28, 2013

Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo

scientific article published on 8 October 2010

Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors

scientific article published on 20 November 2015

Carnosol and carnosic acids from Salvia officinalis inhibit microsomal prostaglandin E2 synthase-1.

scientific article

Connecting lysosomes and mitochondria - a novel role for lipid metabolism in cancer cell death

scientific article published on 29 July 2019

Corrigendum to “Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors” [Eur. J. Med. Chem. 101 (2015) 573–583]

scholarly article by Daniela de Lucia et al published October 2015 in European Journal of Medicinal Chemistry

Curcumin blocks prostaglandin E2 biosynthesis through direct inhibition of the microsomal prostaglandin E2 synthase-1.

scientific article

Defined Structure-Activity Relationships of Boswellic Acids Determine Modulation of Ca2+ Mobilization and Aggregation of Human Platelets by Boswellia serrata Extracts

scientific article published on 12 April 2017

Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions

scientific article

Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors

scientific article published on 15 July 2015

Developmental stage-dependent regulation of spine formation by calcium-calmodulin-dependent protein kinase IIα and Rap1.

scientific article published on 17 October 2017

Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.

scientific article published on 31 October 2009

Discovery of new potent molecular entities able to inhibit mPGES-1.

scientific article published on 23 October 2017

Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol

scientific article published on June 2015

Endogenous metabolites of vitamin E limit inflammation by targeting 5-lipoxygenase

scientific article published in Nature Communications

Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation

scientific article published on 19 July 2021

Ginkgolic Acid is a Multi-Target Inhibitor of Key Enzymes in Pro-Inflammatory Lipid Mediator Biosynthesis

scientific article published on 17 July 2019

Green tea epigallocatechin-3-gallate inhibits microsomal prostaglandin E(2) synthase-1.

scientific article published on 6 August 2009

High capacity for leukotriene biosynthesis in peripheral blood during pregnancy ⬇️

scientific article published on July 16, 2013

Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study

scientific article published on 10 November 2015

Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo.

scientific article

Hyperforin, an Anti-Inflammatory Constituent from St. John's Wort, Inhibits Microsomal Prostaglandin E(2) Synthase-1 and Suppresses Prostaglandin E(2) Formation in vivo ⬇️

scientific article published on 18 February 2011

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.

scientific article published on 22 April 2011

Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol

scientific article

Learning from Nature: From a Marine Natural Product to Synthetic Cyclooxygenase-1 Inhibitors by Automated De Novo Design

scientific article published on 27 June 2021

Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1.

scientific article published on 11 June 2008

Lipid Mediator Profiles Predict Response to Therapy with an Oral Frankincense Extract in Relapsing-Remitting Multiple Sclerosis

scientific article published on 29 May 2020

Lipophilic extracts of Leucas zeylanica, a multi-purpose medicinal plant in the tropics, inhibit key enzymes involved in inflammation and gout

scientific article published in May 2018

Lysophosphatidylcholine acyltransferase 3 is the key enzyme for incorporating arachidonic acid into glycerophospholipids during adipocyte differentiation

scientific article published on 3 December 2012

MK-886, an inhibitor of the 5-lipoxygenase-activating protein, inhibits cyclooxygenase-1 activity and suppresses platelet aggregation

scientific article

Machine intelligence decrypts β-lapachone as an allosteric 5-lipoxygenase inhibitor

scientific article published on 17 July 2018

Matrix-based Molecular Descriptors for Prospective Virtual Compound Screening

scientific article

Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy

scientific article published on 30 January 2017

Multi-target approach for natural products in inflammation

scientific article

Munronia pinnata (Wall.) Theob.: unveiling phytochemistry and dual inhibition of 5-lipoxygenase and microsomal prostaglandin E2 synthase (mPGES)-1.

scientific article published on 4 December 2013

Myrtucommulone from Myrtus communis exhibits potent anti-inflammatory effectiveness in vivo

scientific article

Myxochelins target human 5-lipoxygenase

scientific article published on 16 February 2015

Natural products as inhibitors of prostaglandin E2 and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis

scientific article published on 15 February 2018

Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid

scientific article published on 19 August 2008

PI(18:1/18:1) is a SCD1-derived lipokine that limits stress signaling

scientific article published on 27 May 2022

Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol

scientific article

Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders

scientific article published on 26 June 2015

Pharmacological targeting of membrane rigidity: implications on cancer cell migration and invasion

scholarly article by Simone Braig et al published 5 August 2015 in New Journal of Physics

Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase

scientific article

Polyunsaturated fatty acids are incorporated into maturating male mouse germ cells by lysophosphatidic acid acyltransferase 3 ⬇️

scientific article published on 03 October 2011

Predictive Bioinformatic Assignment of Methyl-Bearing Stereocenters, Total Synthesis, and an Additional Molecular Target of Ajudazol B.

scientific article published on 21 January 2016

Protective Effect of Casperome®, an Orally Bioavailable Frankincense Extract, on Lipopolysaccharide- Induced Systemic Inflammation in Mice.

scientific article

Regeneration in starved planarians depends on TRiC/CCT subunits modulating the unfolded protein response

scientific article published on 30 June 2021

Revealing the macromolecular targets of complex natural products

scientific article published on 2 November 2014

Role of lysophosphatidic acid acyltransferase 3 for the supply of highly polyunsaturated fatty acids in TM4 Sertoli cells

scientific article published on 12 August 2010

Role of p38 mitogen-activated protein kinase in linking stearoyl-CoA desaturase-1 activity with endoplasmic reticulum homeostasis

scientific article published on 12 February 2015

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor ⬇️

scientific article published on December 25, 2011

Stearoyl-CoA desaturase-1 and adaptive stress signaling

scientific article

Structure-Based Design of Microsomal Prostaglandin E2 Synthase-1 (mPGES-1) Inhibitors using a Virtual Fragment Growing Optimization Scheme

scientific article

Structure-Function Relationship Studies In Vitro Reveal Distinct and Specific Effects of Long-Chain Metabolites of Vitamin E.

scientific article

Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents

scientific article published on 29 September 2016

Target identification and lead discovery by functional lipidomics

scientific article published on 15 November 2016

Targeting de novo lipogenesis as a novel approach in anti-cancer therapy

scientific article published on 7 November 2017

The 5‐lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages ⬇️

scientific article published on October 1, 2010

The Anti-Inflammatory and Antimicrobial Potential of Selected Ethnomedicinal Plants from Sri Lanka

scientific article published on 20 April 2020

The Bibenzyl Canniprene Inhibits the Production of Pro-Inflammatory Eicosanoids and Selectively Accumulates in Some Cannabis sativa Strains

scientific article published on 6 February 2017

The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase

scientific article

The role of diacylglyceride generation by phospholipase D and phosphatidic acid phosphatase in the activation of 5-lipoxygenase in polymorphonuclear leukocytes

scientific article published on 24 January 2008

The standardized herbal combination BNO 2103 contained in Canephron® N alleviates inflammatory pain in experimental cystitis and prostatitis

scientific article published on 10 June 2019

The vitamin E derivative garcinoic acid from Garcinia kola nut seeds attenuates the inflammatory response

scientific article published on 12 March 2019

Tnfaip2/exoc3-driven lipid metabolism is essential for stem cell differentiation and organ homeostasis

scientific article published on 10 December 2020

Total synthesis of myrtucommulone A.

scientific article published in March 2010

Triterpene Acids from Frankincense and Semi-Synthetic Derivatives That Inhibit 5-Lipoxygenase and Cathepsin G.

scientific article published on 24 February 2018

V-ATPase inhibition increases cancer cell stiffness and blocks membrane related Ras signaling - a new option for HCC therapy

scientific article published on 28 December 2016

Vitamin A regulates Akt signaling through the phospholipid fatty acid composition

scientific article

α-Tocopherol long-chain metabolite α-13'-COOH affects the inflammatory response of lipopolysaccharide-activated murine RAW264.7 macrophages

scientific article published on 12 June 2015

List of works by Andreas Koeberle

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

A Multicomponent Carba-Betti Strategy to Alkylidene Heterodimers - Total Synthesis and Structure-Activity Relationships of Arzanol

Acetyl-CoA carboxylase 1 regulates endothelial cell migration by shifting the phospholipid composition

Analgesic potential of standardized methanol stem bark extract of Ficus platyphylla in mice: Mechanisms of action

Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males

Aneuploidy-inducing gene knockdowns overlap with cancer mutations and identify Orp3 as a B-cell lymphoma suppressor

Anti-inflammatory and analgesic activity of carnosol and carnosic acid in vivo and in vitro and in silico analysis of their target interactions.

Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding ⬇️

Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo

Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors

Carnosol and carnosic acids from Salvia officinalis inhibit microsomal prostaglandin E2 synthase-1.

Connecting lysosomes and mitochondria - a novel role for lipid metabolism in cancer cell death

Corrigendum to “Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors” [Eur. J. Med. Chem. 101 (2015) 573–583]

Curcumin blocks prostaglandin E2 biosynthesis through direct inhibition of the microsomal prostaglandin E2 synthase-1.

Defined Structure-Activity Relationships of Boswellic Acids Determine Modulation of Ca2+ Mobilization and Aggregation of Human Platelets by Boswellia serrata Extracts

Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions

Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors

Developmental stage-dependent regulation of spine formation by calcium-calmodulin-dependent protein kinase IIα and Rap1.

Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.

Discovery of new potent molecular entities able to inhibit mPGES-1.

Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol

Endogenous metabolites of vitamin E limit inflammation by targeting 5-lipoxygenase

Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation

Ginkgolic Acid is a Multi-Target Inhibitor of Key Enzymes in Pro-Inflammatory Lipid Mediator Biosynthesis

Green tea epigallocatechin-3-gallate inhibits microsomal prostaglandin E(2) synthase-1.

High capacity for leukotriene biosynthesis in peripheral blood during pregnancy ⬇️

Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study

Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo.

Hyperforin, an Anti-Inflammatory Constituent from St. John's Wort, Inhibits Microsomal Prostaglandin E(2) Synthase-1 and Suppresses Prostaglandin E(2) Formation in vivo ⬇️

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.

Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol

Learning from Nature: From a Marine Natural Product to Synthetic Cyclooxygenase-1 Inhibitors by Automated De Novo Design

Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1.

Lipid Mediator Profiles Predict Response to Therapy with an Oral Frankincense Extract in Relapsing-Remitting Multiple Sclerosis

Lipophilic extracts of Leucas zeylanica, a multi-purpose medicinal plant in the tropics, inhibit key enzymes involved in inflammation and gout

Lysophosphatidylcholine acyltransferase 3 is the key enzyme for incorporating arachidonic acid into glycerophospholipids during adipocyte differentiation

MK-886, an inhibitor of the 5-lipoxygenase-activating protein, inhibits cyclooxygenase-1 activity and suppresses platelet aggregation

Machine intelligence decrypts β-lapachone as an allosteric 5-lipoxygenase inhibitor

Matrix-based Molecular Descriptors for Prospective Virtual Compound Screening

Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy

Multi-target approach for natural products in inflammation

Munronia pinnata (Wall.) Theob.: unveiling phytochemistry and dual inhibition of 5-lipoxygenase and microsomal prostaglandin E2 synthase (mPGES)-1.

Myrtucommulone from Myrtus communis exhibits potent anti-inflammatory effectiveness in vivo

Myxochelins target human 5-lipoxygenase

Natural products as inhibitors of prostaglandin E2 and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis

Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid

PI(18:1/18:1) is a SCD1-derived lipokine that limits stress signaling

Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol

Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders

Pharmacological targeting of membrane rigidity: implications on cancer cell migration and invasion

Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase

Polyunsaturated fatty acids are incorporated into maturating male mouse germ cells by lysophosphatidic acid acyltransferase 3 ⬇️

Predictive Bioinformatic Assignment of Methyl-Bearing Stereocenters, Total Synthesis, and an Additional Molecular Target of Ajudazol B.

Protective Effect of Casperome®, an Orally Bioavailable Frankincense Extract, on Lipopolysaccharide- Induced Systemic Inflammation in Mice.

Regeneration in starved planarians depends on TRiC/CCT subunits modulating the unfolded protein response

Revealing the macromolecular targets of complex natural products

Role of lysophosphatidic acid acyltransferase 3 for the supply of highly polyunsaturated fatty acids in TM4 Sertoli cells

Role of p38 mitogen-activated protein kinase in linking stearoyl-CoA desaturase-1 activity with endoplasmic reticulum homeostasis

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor ⬇️

Stearoyl-CoA desaturase-1 and adaptive stress signaling

Structure-Based Design of Microsomal Prostaglandin E2 Synthase-1 (mPGES-1) Inhibitors using a Virtual Fragment Growing Optimization Scheme

Structure-Function Relationship Studies In Vitro Reveal Distinct and Specific Effects of Long-Chain Metabolites of Vitamin E.

Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents

Target identification and lead discovery by functional lipidomics

Targeting de novo lipogenesis as a novel approach in anti-cancer therapy

The 5‐lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages ⬇️

The Anti-Inflammatory and Antimicrobial Potential of Selected Ethnomedicinal Plants from Sri Lanka

The Bibenzyl Canniprene Inhibits the Production of Pro-Inflammatory Eicosanoids and Selectively Accumulates in Some Cannabis sativa Strains

The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase

The role of diacylglyceride generation by phospholipase D and phosphatidic acid phosphatase in the activation of 5-lipoxygenase in polymorphonuclear leukocytes

The standardized herbal combination BNO 2103 contained in Canephron® N alleviates inflammatory pain in experimental cystitis and prostatitis

The vitamin E derivative garcinoic acid from Garcinia kola nut seeds attenuates the inflammatory response

Tnfaip2/exoc3-driven lipid metabolism is essential for stem cell differentiation and organ homeostasis

Total synthesis of myrtucommulone A.

Triterpene Acids from Frankincense and Semi-Synthetic Derivatives That Inhibit 5-Lipoxygenase and Cathepsin G.

V-ATPase inhibition increases cancer cell stiffness and blocks membrane related Ras signaling - a new option for HCC therapy

Vitamin A regulates Akt signaling through the phospholipid fatty acid composition

α-Tocopherol long-chain metabolite α-13'-COOH affects the inflammatory response of lipopolysaccharide-activated murine RAW264.7 macrophages