Computational investigation of turmeric phytochemicals targeting PTR1 enzyme of Leishmania species [PDF]
HeliyonIn this study, we used in silico techniques to identify available parasite treatments, representing a promising therapeutic avenue. Building upon our computational initiatives aimed at discovering natural inhibitors for various target enzymes from ...
Wasia Ullah +9 more
doaj +6 more sources
Inhibition of Leishmania Major PTR1 Gene Expression by Anti-sense in Escherichia Coli [PDF]
Iranian Journal of Public Health, 2012 Background:Protozoa related to Trypanosome family including Leishmania,synthesize enzymes to escape from drug therapy.One of them is PTR1 that its enzymatic activity is similar to dihydrofolate reductase(DHFR)Dihydrofolate reductase - thymidylate ...
M Mohebali +5 more
doaj +7 more sources
Design of 2-Aminobenzothiazole Derivatives Targeting Trypanosomatid PTR1 by a Multidisciplinary Fragment Hybridization Approach. [PDF]
J Med ChemPteridine reductase 1 (PTR1) is a key folate pathway enzyme of pathogenic trypanosomatids that reduces biopterin to dihydro- and tetrahydrobiopterin. It is a promising target for drug design against diseases such as sleeping sickness or leishmaniasis. Amongst known PTR1 inhibitors, 2-aminobenzothiazole derivatives that target the PTR1 biopterin pocket ...
Panecka-Hofman J +18 more
europepmc +9 more sources
Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasi [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2019 Leishmaniasis is a tropical disease found in more than 90 countries. The drugs available to treat this disease have nonspecific action and high toxicity.
Bárbara Velame Ferreira Teixeira +7 more
doaj +4 more sources
Spiro heterocycles bearing piperidine moiety as potential scaffold for antileishmanial activity: synthesis, biological evaluation, and in silico studies [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023 New spiro-piperidine derivatives were synthesised via the eco-friendly ionic liquids in a one-pot fashion. The in vitro antileishmanial activity against Leishmania major promastigote and amastigote forms highlighted promising antileishmanial activity for
Mounir A. A. Mohamed +7 more
doaj +2 more sources
Kaurane-Type Diterpenoids as Potential Inhibitors of Dihydrofolate Reductase-Thymidylate Synthase in New World Leishmania Species [PDF]
Antibiotics, 2023 The bifunctional enzyme Dihydrofolate reductase-thymidylate synthase (DHFR-TS) plays a crucial role in the survival of the Leishmania parasite, as folates are essential cofactors for purine and pyrimidine nucleotide biosynthesis. However, DHFR inhibitors
Chonny Herrera-Acevedo +5 more
doaj +2 more sources
Protozoan Neglected Tropical Diseases (NTDs) Target Inhibition of Alkaloids from Croton linearis Jacq Leaves: A Molecular Docking and ADMET Approach [PDF]
PharmaceuticalsBackground/Objectives: Neglected tropical diseases (NTDs) caused by protozoan parasites such as Trypanosoma cruzi, Trypanosoma brucei, Leishmania spp., and Plasmodium falciparum remain a global health challenge due to limited therapies and increasing ...
Julio A. Rojas-Vargas +6 more
doaj +2 more sources
Design and Synthesis of New Anthranyl Phenylhydrazides: Antileishmanial Activity and Structure–Activity Relationship [PDF]
Pharmaceuticals, 2023 Leishmaniasis is a neglected tropical disease affecting millions of people worldwide. A centenary approach to antimonial-based drugs was first initiated with the synthesis of urea stibamine by Upendranath Brahmachari in 1922.
Claudia do Carmo Maquiaveli +12 more
doaj +2 more sources
HAPLN1 confers multiple myeloma cell resistance to several classes of therapeutic drugs. [PDF]
PLoS ONE, 2022 Multiple myeloma (MM), a malignant plasma cell infiltration of the bone marrow, is generally considered incurable: resistance to multiple therapeutic drugs inevitably arises from tumor cell-intrinsic and tumor microenvironment (TME)-mediated mechanisms ...
Mailee Huynh +6 more
doaj +2 more sources
Drug Repurposing for Kala-Azar [PDF]
PharmaceuticsObjective: Visceral leishmaniasis (VL), a Neglected Tropical Disease caused by Leishmania donovani, remains insufficiently addressed by current therapies due to high toxicity, poor efficacy, and immunosuppressive complications.
Biljana Arsić +6 more
doaj +2 more sources