Exequiel O. J. Porta
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View article: INTERACT: Interactome Network Targeting via Enzyme Reactivity and Activity-based Chemoproteomic Tools
INTERACT: Interactome Network Targeting via Enzyme Reactivity and Activity-based Chemoproteomic Tools Open
This chapter details an activity-based chemoproteomic methodology, INTERACT (Interactome Network Targeting via Enzyme Reactivity and Activity-based Chemoproteomic Tools), for the functional interrogation of host-pathogen interactions (inte…
View article: Progress and Prospects of Triazoles in Advanced Therapies for Parasitic Diseases
Progress and Prospects of Triazoles in Advanced Therapies for Parasitic Diseases Open
Parasitic diseases represent a severe global burden, with current treatments often limited by toxicity, drug resistance, and suboptimal efficacy in chronic infections. This review examines the emerging role of triazole-based compounds, ori…
View article: Activity-Based Chemoproteomic Profiling Reveals the Active Kinome of Leishmania
Activity-Based Chemoproteomic Profiling Reveals the Active Kinome of Leishmania Open
Background: Leishmania parasites cause neglected tropical diseases such as cutaneous and visceral leishmaniasis, which have limited treatment options and rising drug resistance. Protein kinases are pivotal in Leishmania biology and attract…
View article: Profiling Serine Hydrolases in the <i>Leishmania</i> Host–Pathogen Interactome Using Cell‐Permeable Activity‐Based Fluorophosphonate Probes
Profiling Serine Hydrolases in the <i>Leishmania</i> Host–Pathogen Interactome Using Cell‐Permeable Activity‐Based Fluorophosphonate Probes Open
Leishmaniasis, a vector‐borne neglected tropical disease, caused by the protozoan parasite Leishmania , is a major global public health challenge with millions of new cases annually. Treatment of leishmaniasis is difficult for many reasons…
View article: Simple accessible clemastine fumarate analogues as effective antileishmanials
Simple accessible clemastine fumarate analogues as effective antileishmanials Open
N-linked analogues of clemastine fumarate afford simpler, more accessible, more selective antileishmanials.
View article: Fragment-based drug discovery: A graphical review
Fragment-based drug discovery: A graphical review Open
Three decades after its introduction, fragment-based drug (or lead) discovery (FBDD or FBLD) has become a mature and powerful strategy for generating novel leads, offering distinct advantages for challenging or previously “undruggable” tar…
View article: BONCAT-iTRAQ Labelling Reveals Molecular Markers of Adaptive Responses in Toxoplasma gondii to Pyrimethamine Treatment
BONCAT-iTRAQ Labelling Reveals Molecular Markers of Adaptive Responses in Toxoplasma gondii to Pyrimethamine Treatment Open
We employed a BONCAT-iTRAQ labelling approach to investigate newly synthesised proteins (NSPs) in Toxoplasma gondii subjected to varying concentrations of the antifolate drug pyrimethamine. Our results reveal that numerous NSPs exhibited a…
View article: Microplate-Based Enzymatic Activity Assay Protocol Powered by Activity-Based Probes
Microplate-Based Enzymatic Activity Assay Protocol Powered by Activity-Based Probes Open
Identifying new enzymes and gaining insights into their mode of action (and inhibition) is a critical step in drug discovery. In this chapter, we describe a novel methodology that accelerates this process by combining the precision of Acti…
View article: Microplate-Based Enzymatic Activity Assay Protocol Powered by Activity-Based Probes
Microplate-Based Enzymatic Activity Assay Protocol Powered by Activity-Based Probes Open
In the pursuit of innovative therapeutics, understanding enzyme inhibitors' mechanisms is pivotal. In this chapter, we explore a novel methodology that combines the precision of Activity-Based Protein Profiling (ABPP) with the efficiency o…
View article: Editorial: The evolution in pharmacology of infectious diseases: 2022
Editorial: The evolution in pharmacology of infectious diseases: 2022 Open
This editorial offers an insightful examination and analysis of the significant advancements in the field of infectious diseases from 2022 to 2023, specifically focusing on how these developments have transformed our approaches to combatin…
View article: Inhibition of HSP90 distinctively modulates the global phosphoproteome of <i>Leishmania mexicana</i> developmental stages
Inhibition of HSP90 distinctively modulates the global phosphoproteome of <i>Leishmania mexicana</i> developmental stages Open
Heat shock protein 90 (HSP90) is an evolutionarily conserved chaperone protein that plays a central role in the folding and maturation of a large array of client proteins. In the unicellular parasite Leishmania , the etiological agent of t…
View article: Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities
Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities Open
Chagas disease is a vector-borne illness caused by the protozoan parasite Trypanosoma cruzi ( T. cruzi ). It poses a significant public health burden, particularly in the poorest regions of Latin America. Currently, there is no available v…
View article: Inhibition of HSP90 distinctively modulates the global phosphoproteome of<i>Leishmania mexicana</i>developmental stages
Inhibition of HSP90 distinctively modulates the global phosphoproteome of<i>Leishmania mexicana</i>developmental stages Open
Heat shock protein 90 (HSP90) is an evolutionary conserved chaperone protein that plays a central role in the folding and maturation of a large array of client proteins. In the unicellular parasite Leishmania , the etiological agent of the…
View article: Lipophilic modification of salirasib modulates the antiproliferative and antimigratory activity
Lipophilic modification of salirasib modulates the antiproliferative and antimigratory activity Open
Salirasib, or farnesylthiosalicylic acid (FTS), is a salicylic acid derivative with demonstrated antineoplastic activity. While designed as a competitor of the substrate S-farnesyl cysteine on Ras, it is a potent competitive inhibitor of i…
View article: Mapping the Evolution of Activity-Based Protein Profiling: A Bibliometric Review
Mapping the Evolution of Activity-Based Protein Profiling: A Bibliometric Review Open
Activity-based protein profiling (ABPP) is a chemoproteomic approach that employs small-molecule probes to directly evaluate protein functionality within complex proteomes. This technology has proven to be a potent strategy for mapping lig…
View article: Lipophilic modification of Salirasib modulate the antiproliferative and antimigratory activity.
Lipophilic modification of Salirasib modulate the antiproliferative and antimigratory activity. Open
Salirasib, or farnesylthiosalicylic acid (FTS), is a salicylic acid derivative with demonstrated antineoplastic activity. While designed as a competitor of the substrate S-farnesyl cysteine on Ras, it is a potent competitive inhibitor of i…
View article: Systematic study of 1,2,3-triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases
Systematic study of 1,2,3-triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases Open
A series of thirty 1,2,3-triazolylsterols, inspired by azasterols with proven antiparasitic activity, were prepared by a stereocontrolled synthesis. Ten of these compounds constitute chimeras/hybrids of 22,26-azasterol (AZA) and 1,2,3-tria…
View article: Activity-Based Protein Profiling: A Graphical Review
Activity-Based Protein Profiling: A Graphical Review Open
View article: Lipophilic Modification of Salirasib Modulates the Antiproliferative and Antimigratory Activity
Lipophilic Modification of Salirasib Modulates the Antiproliferative and Antimigratory Activity Open
View article: Activity-based protein profiling: A graphical review
Activity-based protein profiling: A graphical review Open
Activity-based protein profiling (ABPP) is a chemoproteomic technology that employs small chemical probes to directly interrogate protein function within complex proteomes. Since its initial application almost 25 years ago, ABPP has proven…
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols, inspired by azasterols with proven antiparasitic activity, were prepared by a stereocontrolled synthesis. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols. …
View article: Discovery of Leishmania Druggable Serine Proteases by Activity-Based Protein Profiling
Discovery of Leishmania Druggable Serine Proteases by Activity-Based Protein Profiling Open
Leishmaniasis are a group of diseases caused by parasitic protozoa of the genus Leishmania . Current treatments are limited by difficult administration, high cost, poor efficacy, toxicity, and growing resistance. New agents, with new mecha…
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols were prepared by a stereocontrolled synthesis and inspired by azasterols with proven antiparasitic activity. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols…
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols were prepared by a stereocontrolled synthesis and inspired by azasterols with proven antiparasitic activity. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols…
View article: Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines
Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines Open
Aim: We proposed to determine the antiproliferative activity of a series of synthetic salirasib analogs, presenting or not a 1,2,3-triazole linker, against five different cancer cell lines. Results: Bioassay, cheminformatic, and in silico …
View article: Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines
Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines Open
Aim: We proposed to determine the antiproliferative activity of a series of synthetic salirasib analogs, presenting or not a 1,2,3-triazole linker, against five different cancer cell lines. Results: Bioassay, cheminformatic, and in silico …
View article: Synthesis and interaction of terminal unsaturated chemical probes with Mycobacterium tuberculosis CYP124A1
Synthesis and interaction of terminal unsaturated chemical probes with Mycobacterium tuberculosis CYP124A1 Open
A series of C15-C20 isoprenyl derivatives bearing terminal alkenyl and alkynyl groups were synthesized as possible substrates of the methyl-branched lipid ω-hydroxylase CYP124A1 from Mycobacterium tuberculosis. The interactions of each com…
View article: Repositioning Salirasib as a new antimalarial agent
Repositioning Salirasib as a new antimalarial agent Open
Repurposing strategies present an enormous advantage for drug discovery, especially in malaria, where resources are scarce.
View article: Repositioning Salirasib as New Antimalarial Agent
Repositioning Salirasib as New Antimalarial Agent Open
The antiplasmodial activity assay was performed using a simple, high-sensitivity methodology based on nanoluciferase (nLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromol…
View article: Repositioning Salirasib as New Antimalarial Agent
Repositioning Salirasib as New Antimalarial Agent Open
The antiplasmodial activity assay was performed using a simple, high-sensitivity methodology based on nanoluciferase (nLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromolar conc…