List of works - Giancarlo Biagini

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

scientific article published on 18 April 2016

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

scientific article

A comprehensive model of purine uptake by the malaria parasite Plasmodium falciparum: identification of four purine transport activities in intraerythrocytic parasites

scientific article published in April 2008

A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs.

scientific article

A novel drug for uncomplicated malaria: targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNdh2) of Plasmodium falciparum.

scientific article

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

scientific article published on 24 May 2017

A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials.

scientific article published on 20 December 2016

A yeast expression system for functional and pharmacological studies of the malaria parasite Ca²⁺/H⁺ antiporter.

scientific article

Acridinediones: selective and potent inhibitors of the malaria parasite mitochondrial bc1 complex

scientific article

An acid-loading chloride transport pathway in the intraerythrocytic malaria parasite, Plasmodium falciparum

scientific article

Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1

scientific article

Antimalarial activity of primaquine operates via a two-step biochemical relay

scientific article published on 19 July 2019

Antimalarial chemotherapy: young guns or back to the future? ⬇️

scientific article published on November 1, 2003

Antimalarial pharmacology and therapeutics of atovaquone

scientific article

Antitubercular pharmacodynamics of phenothiazines

scientific article published on 9 December 2012

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7.

scientific article published on 8 February 2016

Bacterial-like energy metabolism in the amitochondriate protozoon Hexamita inflata

scientific article published in April 2003

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century

scientific article published on March 2009

Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials

scientific article published on 29 July 2015

Carbohydrate and Amino Acid Fermentation in the Free-Living Primitive Protozoon Hexamita sp.

scientific article published on January 1998

Chapter 17 Type II NADH: quinone oxidoreductases of Plasmodium falciparum and Mycobacterium tuberculosis kinetic and high-throughput assays.

scientific article

Characterization of the choline carrier of Plasmodium falciparum: a route for the selective delivery of novel antimalarial drugs.

scientific article

Continued cytoadherence of Plasmodium falciparum infected red blood cells after antimalarial treatment

scientific article published in October 2009

Corrigendum: A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

scientific article

Current drug development portfolio for antimalarial therapies.

scientific article

Cytochrome b mutation Y268S conferring atovaquone resistance phenotype in malaria parasite results in reduced parasite bc1 catalytic turnover and protein expression

scientific article published on 26 January 2012

Detection of adenovirus and rotavirus antigens by an immuno-gold lateral flow test and ultrasound-enhanced latex agglutination assay

scientific article published on 01 February 2001

Development of a novel drug for uncomplicated malaria targeting the mitochondrial NADH:quinone oxidoreductase.

scientific article published on 20 October 2010

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay

scientific article

Dose prediction for repurposing nitazoxanide in SARS-CoV-2 treatment or chemoprophylaxis

scientific article published on 06 May 2020

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity

scientific article published on 27 October 2010

Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs.

scientific article

Evolution of the hydrogenosome ⬇️

scientific article published on October 15, 1997

Functional characterization and target validation of alternative complex I of Plasmodium falciparum mitochondria

scientific article (publication date: May 2006)

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria

scientific article

Glycerol: an unexpected major metabolite of energy metabolism by the human malaria parasite.

scientific article published on 06 March 2009

HDQ, a potent inhibitor of Plasmodium falciparum proliferation, binds to the quinone reduction site of the cytochrome bc1 complex.

scientific article

Heme Binding Contributes to Antimalarial Activity of Bis-Quaternary Ammoniums

scientific article published in 2003

Identification of new antimalarial leads by use of virtual screening against cytochrome bc₁.

scientific article published on 10 September 2011

Identification of novel antimalarial chemotypes via chemoinformatic compound selection methods for a high-throughput screening program against the novel malarial target, PfNDH2: increasing hit rate via virtual screening methods.

scientific article

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

scientific article published on 24 February 2012

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

scientific article

Intracellular PD Modelling (PDi) for the Prediction of Clinical Activity of Increased Rifampicin Dosing

scientific article published on 13 June 2019

Intracellular Pharmacodynamic Modeling Is Predictive of the Clinical Activity of Fluoroquinolones against Tuberculosis

scientific article published on 20 December 2019

Loss of pH control in Plasmodium falciparum parasites subjected to oxidative stress

scientific article

Malaria parasite transporters as a drug-delivery strategy.

scientific article

Malaria-parasite mitochondrial dehydrogenases as drug targets: too early to write the obituary.

scientific article

Modelling of Systemic versus Pulmonary Chloroquine Exposure in Man for COVID-19 Dose Selection

scientific article published on 30 April 2020

Mutations conferring drug resistance in malaria parasite drug transporters Pgh1 and PfCRT do not affect steady-state vacuolar Ca2+.

scientific article

Na(+)-dependent pH regulation by the amitochondriate protozoan parasite Giardia intestinalis

scientific article published on 10 April 2001

Novel inhibitors of the Plasmodium falciparum electron transport chain

scientific article published on January 2014

Open-label comparative clinical study of chlorproguanil-dapsone fixed dose combination (Lapdap) alone or with three different doses of artesunate for uncomplicated Plasmodium falciparum malaria

scientific article

OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens

scientific article

Oxygen uptake and antioxidant responses of the free-living diplomonad Hexamita sp

scientific article published on 01 September 1997

PfCRT and the trans-vacuolar proton electrochemical gradient: regulating the access of chloroquine to ferriprotoporphyrin IX.

scientific article published on 31 August 2006

Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration

scientific article

Potent Antimalarial 2-Pyrazolyl Quinolone bc 1 (Qi) Inhibitors with Improved Drug-like Properties

scientific article published on 19 October 2018

Potent antihematozoan activity of novel bisthiazolium drug T16: evidence for inhibition of phosphatidylcholine metabolism in erythrocytes infected with Babesia and Plasmodium spp.

scientific article

Primitive anaerobic protozoa: a false concept?

scientific article published on 01 May 2000

Prioritisation of potential anti-SARS-CoV-2 drug repurposing opportunities based on ability to achieve adequate target site concentrations derived from their established human pharmacokinetics

scientific article published on 22 April 2020

Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential

scientific article published on 12 December 2013

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis

scholarly article

Role of K+ and amino acids in osmoregulation by the free-living microaerophilic protozoon Hexamita inflata

scientific article published on 01 February 2000

Sex, power and drugs: the murky world of malaria parasite mitochondria.

scientific article

Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability

scientific article published on 30 September 2013

Synthesis and antimalarial activities of a diverse set of triazole-containing furamidine analogues

scientific article published on 8 September 2011

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria

scientific article published on 17 May 2018

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

scientific article published on April 2009

Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era.

scientific article

The antioxidant potential of pyruvate in the amitochondriate diplomonads Giardia intestinalis and Hexamita inflata

scientific article published in December 2001

The digestive food vacuole of the malaria parasite is a dynamic intracellular Ca2+ store.

scientific article

The malaria parasite type II NADH:quinone oxidoreductase: an alternative enzyme for an alternative lifestyle

scientific article published on 10 May 2007

The membrane potential of Giardia intestinalis

scientific article published on 01 November 2000

The microaerophilic flagellate Giardia intestinalis: oxygen and its reaction products collapse membrane potential and cause cytotoxicity

scientific article published in December 2000

The molecular basis of folate salvage in Plasmodium falciparum: characterization of two folate transporters

scientific article (publication date: 30 December 2011)

The plasma membrane of microaerophilic protists: oxidative and nitrosative stress.

scientific article

The proliferating cell hypothesis: a metabolic framework for Plasmodium growth and development

scientific article published on 11 March 2014

The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest

scientific article published on 01 February 2020

Transforming rhinacanthin analogues from potent anticancer agents into potent antimalarial agents

scientific article published in February 2010

Treatment responses to Azithromycin and Ciprofloxacin in uncomplicated Salmonella Typhi infection: A comparison of Clinical and Microbiological Data from a Controlled Human Infection Model

scientific article published on 26 December 2019

Trichomonas vaginalis and Giardia intestinalis produce nitric oxide and display NO-synthase activity

scientific article published on 01 January 2006

Ultrasound enhanced detection of individual meningococcal serogroups by latex immunoassay.

scientific article

List of works by Giancarlo Biagini

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

A comprehensive model of purine uptake by the malaria parasite Plasmodium falciparum: identification of four purine transport activities in intraerythrocytic parasites

A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs.

A novel drug for uncomplicated malaria: targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNdh2) of Plasmodium falciparum.

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials.

A yeast expression system for functional and pharmacological studies of the malaria parasite Ca²⁺/H⁺ antiporter.

Acridinediones: selective and potent inhibitors of the malaria parasite mitochondrial bc1 complex

An acid-loading chloride transport pathway in the intraerythrocytic malaria parasite, Plasmodium falciparum

Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1

Antimalarial activity of primaquine operates via a two-step biochemical relay

Antimalarial chemotherapy: young guns or back to the future? ⬇️

Antimalarial pharmacology and therapeutics of atovaquone

Antitubercular pharmacodynamics of phenothiazines

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7.

Bacterial-like energy metabolism in the amitochondriate protozoon Hexamita inflata

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century

Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials

Carbohydrate and Amino Acid Fermentation in the Free-Living Primitive Protozoon Hexamita sp.

Chapter 17 Type II NADH: quinone oxidoreductases of Plasmodium falciparum and Mycobacterium tuberculosis kinetic and high-throughput assays.

Characterization of the choline carrier of Plasmodium falciparum: a route for the selective delivery of novel antimalarial drugs.

Continued cytoadherence of Plasmodium falciparum infected red blood cells after antimalarial treatment

Corrigendum: A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

Current drug development portfolio for antimalarial therapies.

Cytochrome b mutation Y268S conferring atovaquone resistance phenotype in malaria parasite results in reduced parasite bc1 catalytic turnover and protein expression

Detection of adenovirus and rotavirus antigens by an immuno-gold lateral flow test and ultrasound-enhanced latex agglutination assay

Development of a novel drug for uncomplicated malaria targeting the mitochondrial NADH:quinone oxidoreductase.

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay

Dose prediction for repurposing nitazoxanide in SARS-CoV-2 treatment or chemoprophylaxis

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity

Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs.

Evolution of the hydrogenosome ⬇️

Functional characterization and target validation of alternative complex I of Plasmodium falciparum mitochondria

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria

Glycerol: an unexpected major metabolite of energy metabolism by the human malaria parasite.

HDQ, a potent inhibitor of Plasmodium falciparum proliferation, binds to the quinone reduction site of the cytochrome bc1 complex.

Heme Binding Contributes to Antimalarial Activity of Bis-Quaternary Ammoniums

Identification of new antimalarial leads by use of virtual screening against cytochrome bc₁.

Identification of novel antimalarial chemotypes via chemoinformatic compound selection methods for a high-throughput screening program against the novel malarial target, PfNDH2: increasing hit rate via virtual screening methods.

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Intracellular PD Modelling (PDi) for the Prediction of Clinical Activity of Increased Rifampicin Dosing

Intracellular Pharmacodynamic Modeling Is Predictive of the Clinical Activity of Fluoroquinolones against Tuberculosis

Loss of pH control in Plasmodium falciparum parasites subjected to oxidative stress

Malaria parasite transporters as a drug-delivery strategy.

Malaria-parasite mitochondrial dehydrogenases as drug targets: too early to write the obituary.

Modelling of Systemic versus Pulmonary Chloroquine Exposure in Man for COVID-19 Dose Selection

Mutations conferring drug resistance in malaria parasite drug transporters Pgh1 and PfCRT do not affect steady-state vacuolar Ca2+.

Na(+)-dependent pH regulation by the amitochondriate protozoan parasite Giardia intestinalis

Novel inhibitors of the Plasmodium falciparum electron transport chain

Open-label comparative clinical study of chlorproguanil-dapsone fixed dose combination (Lapdap) alone or with three different doses of artesunate for uncomplicated Plasmodium falciparum malaria

OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens

Oxygen uptake and antioxidant responses of the free-living diplomonad Hexamita sp

PfCRT and the trans-vacuolar proton electrochemical gradient: regulating the access of chloroquine to ferriprotoporphyrin IX.

Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration

Potent Antimalarial 2-Pyrazolyl Quinolone bc 1 (Qi) Inhibitors with Improved Drug-like Properties

Potent antihematozoan activity of novel bisthiazolium drug T16: evidence for inhibition of phosphatidylcholine metabolism in erythrocytes infected with Babesia and Plasmodium spp.

Primitive anaerobic protozoa: a false concept?

Prioritisation of potential anti-SARS-CoV-2 drug repurposing opportunities based on ability to achieve adequate target site concentrations derived from their established human pharmacokinetics

Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis

Role of K+ and amino acids in osmoregulation by the free-living microaerophilic protozoon Hexamita inflata

Sex, power and drugs: the murky world of malaria parasite mitochondria.

Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability

Synthesis and antimalarial activities of a diverse set of triazole-containing furamidine analogues

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era.

The antioxidant potential of pyruvate in the amitochondriate diplomonads Giardia intestinalis and Hexamita inflata

The digestive food vacuole of the malaria parasite is a dynamic intracellular Ca2+ store.

The malaria parasite type II NADH:quinone oxidoreductase: an alternative enzyme for an alternative lifestyle

The membrane potential of Giardia intestinalis

The microaerophilic flagellate Giardia intestinalis: oxygen and its reaction products collapse membrane potential and cause cytotoxicity

The molecular basis of folate salvage in Plasmodium falciparum: characterization of two folate transporters

The plasma membrane of microaerophilic protists: oxidative and nitrosative stress.

The proliferating cell hypothesis: a metabolic framework for Plasmodium growth and development

The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest

Transforming rhinacanthin analogues from potent anticancer agents into potent antimalarial agents