List of works - Michael P. Pollastri

A chemical screen identifies small molecules that regulate hepcidin expression

scientific article

A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes

scientific article (publication date: September 2014)

Anilinoquinoline based inhibitors of trypanosomatid proliferation

scientific article published on 26 November 2018

Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.

scientific article

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

scientific article

Corrigendum to "Optimization of physicochemical properties for 4-Anilinoquinazoline inhibitors of trypanosome proliferation" [Eur. J. Med. Chem. 141 (2017) 446-459]

scientific article published on 10 May 2018

Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis

scientific article

Drug Discovery in the 21St Century ⬇️

scientific article published on December 1, 2011

EVALUATION OF AROMATIC 6-SUBSTITUTED THIENOPYRIMIDINES AS SCAFFOLDS AGAINST PARASITES THAT CAUSE TRYPANOSOMIASIS, LEISHMANIASIS, AND MALARIA.

scientific article

Efficient use of the iron ortho-nitrophenylporphyrin chloride to mimic biological oxidations of dimethylaminoantipyrine

scientific article published in October 2007

Erratum: Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis

scientific article published on 11 January 2017

Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness

scientific article published on 21 May 2014

Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents

scientific article published on 08 February 2019

Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)

scientific article published on May 2015

Fexinidazole: A New Drug for African Sleeping Sickness on the Horizon

scientific article

Finding new collaboration models for enabling neglected tropical disease drug discovery

scientific article (publication date: July 2014)

From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.

scientific article

Glycogen Synthase Kinase 3β Promotes the Endocytosis of Transferrin in the African Trypanosome

scientific article published on 16 June 2016

Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics

scientific article published on 20 November 2019

Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign

scientific article (publication date: October 2014)

Identification and characterization of kava-derived compounds mediating TNF-alpha suppression

scientific article published on 16 June 2009

Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?

scientific article published on 17 January 2016

Identification of cinnabarinic acid as a novel endogenous aryl hydrocarbon receptor ligand that drives IL-22 production.

scientific article published on 03 February 2014

Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development

scientific article published on 10 January 2019

In silico identification of an aryl hydrocarbon receptor antagonist with biological activity in vitro and in vivo

scientific article

Jumping the Industrial-Academia Fence ⬇️

scientific article published on January 1, 2013

Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis

scientific article published on 3 May 2013

Kinases as druggable targets in trypanosomatid protozoan parasites

scientific article

Lapatinib-binding protein kinases in the African trypanosome: identification of cellular targets for kinase-directed chemical scaffolds

scientific article

Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead for Trypanosoma brucei Inhibitors

scientific article published on 13 August 2020

Microwave Synthesis

article

Neutralizing positive charges at the surface of a protein lowers its rate of amide hydrogen exchange without altering its structure or increasing its thermostability.

scientific article

Novel Effects of Lapatinib Revealed in the African Trypanosome by Using Hypothesis-Generating Proteomics and Chemical Biology Strategies

scientific article published on 21 November 2016

Optimization of Physicochemical Properties for 4-Anilinoquinoline Inhibitors of Plasmodium falciparum Proliferation

scientific article published on 4 January 2018

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.

scientific article

Overview on the Rule of Five ⬇️

scientific article published on 01 June 2010

Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness

scientific article published on 8 November 2011

Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery.

scientific article published on 8 July 2015

Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery

scientific article published on May 2014

Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei

scientific article

Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

scientific article

Repurposing strategies for tropical disease drug discovery

scientific article published on 30 March 2016

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors

scientific article published on 10 January 2020

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis

scientific article published on 08 January 2020

Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation

scientific article published on 04 September 2018

Structure-Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni

scientific article published on 10 January 2020

Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

scientific article published on 21 August 2013

Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs

scientific article published on 9 February 2012

Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs.

scientific article published on 9 February 2012

Synthesis, structure, and thermal properties of 1,2-dipalmitoylgalloylglycerol (DPGG), a novel self-adhering lipid

scientific article published on 01 January 2000

Target repurposing for neglected diseases

scientific article

The Future of Drug Repositioning

The Importance of Collaboration between Industry, Academics, and Nonprofits in Tropical Disease Drug Discovery

scientific article published on 14 November 2017

The challenge of developing robust drugs to overcome resistance ⬇️

scientific article published on July 19, 2011

The human Aurora kinase inhibitor danusertib is a lead compound for anti-trypanosomal drug discovery via target repurposing.

scientific article

The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing

scientific article

List of works by Michael P. Pollastri

A chemical screen identifies small molecules that regulate hepcidin expression

A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes

Anilinoquinoline based inhibitors of trypanosomatid proliferation

Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

Corrigendum to "Optimization of physicochemical properties for 4-Anilinoquinazoline inhibitors of trypanosome proliferation" [Eur. J. Med. Chem. 141 (2017) 446-459]

Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis

Drug Discovery in the 21St Century ⬇️

EVALUATION OF AROMATIC 6-SUBSTITUTED THIENOPYRIMIDINES AS SCAFFOLDS AGAINST PARASITES THAT CAUSE TRYPANOSOMIASIS, LEISHMANIASIS, AND MALARIA.

Efficient use of the iron ortho-nitrophenylporphyrin chloride to mimic biological oxidations of dimethylaminoantipyrine

Erratum: Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis

Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness

Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents

Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)

Fexinidazole: A New Drug for African Sleeping Sickness on the Horizon

Finding new collaboration models for enabling neglected tropical disease drug discovery

From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.

Glycogen Synthase Kinase 3β Promotes the Endocytosis of Transferrin in the African Trypanosome

Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics

Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign

Identification and characterization of kava-derived compounds mediating TNF-alpha suppression

Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?

Identification of cinnabarinic acid as a novel endogenous aryl hydrocarbon receptor ligand that drives IL-22 production.

Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development

In silico identification of an aryl hydrocarbon receptor antagonist with biological activity in vitro and in vivo

Jumping the Industrial-Academia Fence ⬇️

Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis

Kinases as druggable targets in trypanosomatid protozoan parasites

Lapatinib-binding protein kinases in the African trypanosome: identification of cellular targets for kinase-directed chemical scaffolds

Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead for Trypanosoma brucei Inhibitors

Microwave Synthesis

Neutralizing positive charges at the surface of a protein lowers its rate of amide hydrogen exchange without altering its structure or increasing its thermostability.

Novel Effects of Lapatinib Revealed in the African Trypanosome by Using Hypothesis-Generating Proteomics and Chemical Biology Strategies

Optimization of Physicochemical Properties for 4-Anilinoquinoline Inhibitors of Plasmodium falciparum Proliferation

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.

Overview on the Rule of Five ⬇️

Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness

Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery.

Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery

Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei

Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

Repurposing strategies for tropical disease drug discovery

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis

Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation

Structure-Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni

Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs

Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs.

Synthesis, structure, and thermal properties of 1,2-dipalmitoylgalloylglycerol (DPGG), a novel self-adhering lipid

Target repurposing for neglected diseases

The Future of Drug Repositioning

The Importance of Collaboration between Industry, Academics, and Nonprofits in Tropical Disease Drug Discovery

The challenge of developing robust drugs to overcome resistance ⬇️

The human Aurora kinase inhibitor danusertib is a lead compound for anti-trypanosomal drug discovery via target repurposing.

The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing