4.7 Article

Giardia lamblia G6PD::6PGL Fused Protein Inhibitors Decrease Trophozoite Viability: A New Alternative against Giardiasis

Related references

Note: Only part of the references are listed.
Article Biochemistry & Molecular Biology

Kinetic and Molecular Docking Studies to Determine the Effect of Inhibitors on the Activity and Structure of Fused G6PD::6PGL Protein from Trichomonas vaginalis

Victor Martinez-Rosas et al.

Summary: Trichomoniasis is a globally prevalent sexually transmitted disease, affecting 270 million people worldwide. This study investigated the impact of a library of compounds on the activity of a crucial protein involved in the energy production of Trichomonas vaginalis. Four compounds were found to inhibit the protein by more than 50%. Further analysis revealed the mechanism of inhibition and demonstrated the potential of these compounds as selective inhibitors. These findings provide new insights and potential treatment options for trichomoniasis.

MOLECULES (2022)

Article Chemistry, Medicinal

Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPARγ Modulators: An In Combo Study

Blanca Colin-Lozano et al.

Summary: This study synthesized and characterized four isobutyric acid derivatives. The results showed that these compounds increased the mRNA concentration of PPAR gamma and GLUT-4, and had antihyperglycemic effects. Nitrocompound 2 was identified as the most promising candidate.

PHARMACEUTICALS (2022)

Review Biology

The Multiple Roles of Glucose-6-Phosphate Dehydrogenase in Tumorigenesis and Cancer Chemoresistance

Jiaqi Song et al.

Summary: The pentose phosphate pathway (PPP) is an important metabolic pathway that provides crucial substances such as NADPH and nucleotides for cellular activities. G6PD, the rate-limiting enzyme of PPP, is upregulated in various cancers and its dysfunction influences cancer cell growth, invasion, and chemotherapeutic resistance. Targeting G6PD has shown promise as a strategy in treating cancer and reversing chemoresistance.

LIFE-BASEL (2022)

Article Pharmacology & Pharmacy

Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes

Zirui Lu et al.

Summary: Nitazoxanide and related thiazolides are effective against protozoan parasites, bacteria, and viruses, and have also shown potential in inducing cell cycle arrest and apoptosis in cancer cells. This study reveals that the 20S proteasome is a direct target of these compounds, leading to cell cycle arrest and cell death in colon cancer cells. The binding mode of these compounds in the 20S proteasome is different from existing proteasome inhibitors, providing insights for the design of novel anti-tumor agents.

BIOCHEMICAL PHARMACOLOGY (2022)

Article Biochemical Research Methods

ColabFold: making protein folding accessible to all

Milot Mirdita et al.

Summary: ColabFold combines fast homology search and optimized model utilization to offer accelerated prediction of protein structures and complexes, with a processing speed that is 40-60 times faster. It serves as a free and accessible platform for protein folding, capable of predicting close to 1,000 structures per day.

NATURE METHODS (2022)

Article Chemistry, Medicinal

Synthesis, in vitro, in silico and in vivo hypoglycemic and lipid-lowering effects of 4-benzyloxy-5-benzylidene-1,3-thiazolidine-2,4-diones mediated by dual PPAR α/γ modulation

Jose Luis Madrigal-Angulo et al.

Summary: In this study, a series of nine compounds were synthesized and tested for their effects on proteins related to diabetes. Compounds 1-3 were identified as dual PPARα/γ modulators and showed potential therapeutic effects for both diabetes and dyslipidemia.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

Article Biochemistry & Molecular Biology

Novel inhibitors of human glucose-6-phosphate dehydrogenase (HsG6PD) affect the activity and stability of the protein

Edson Jiovany Ramirez-Nava et al.

Summary: In vitro studies identified two new compounds (CNZ-3 and JMM-2) as inhibitors of HsG6PD, showing different mechanisms of inhibition compared to previously known inhibitors. These compounds affect the protein's structure and thermal stability, highlighting their potential as future pharmacological approaches for cancer research and treatment.

BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS (2021)

Article Chemistry, Medicinal

Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors

Zirui Lu et al.

Summary: Nitazoxanide was identified as a moderate inhibitor of the STAT3 pathway, leading to the design and synthesis of a series of thiazolide derivatives with enhanced potency. Two derivatives, 15 and 24, showed greater efficacy than the positive control WP1066, indicating a potential broad-spectrum effect of thiazolides as antitumor agents targeting STAT3.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

Review Microbiology

Giardia duodenalis: Biology and Pathogenesis

Rodney D. Adam

Summary: Giardia duodenalis, initially observed by Leeuwenhoek in 1681, gained attention as a human pathogen in the 1960s. Advances in technology have provided insights into its biology and immunology, revealing the importance of a balanced host immune response and the role of the Th17 response. Infection with Giardia can result in a wide range of symptoms, highlighting the complexity of host-parasite interactions.

CLINICAL MICROBIOLOGY REVIEWS (2021)

Article Multidisciplinary Sciences

Highly accurate protein structure prediction with AlphaFold

John Jumper et al.

Summary: Proteins are essential for life, and accurate prediction of their structures is a crucial research problem. Current experimental methods are time-consuming, highlighting the need for accurate computational approaches to address the gap in structural coverage. Despite recent progress, existing methods fall short of atomic accuracy in protein structure prediction.

NATURE (2021)

Review Infectious Diseases

Giardiasis treatment: an update with a focus on refractory disease

Kristine Morch et al.

CURRENT OPINION IN INFECTIOUS DISEASES (2020)

Article Chemistry, Medicinal

Anti-Giardia Drug Discovery: Current Status and Gut Feelings

Andrew Riches et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Biochemistry & Molecular Biology

Enhanced Antigiardial Effect of Omeprazole Analog Benzimidazole Compounds

Beatriz Hernandez-Ochoa et al.

MOLECULES (2020)

Article Medicine, General & Internal

Anti-amoebic activity of a cecropin-melittin hybrid peptide (CM11) against trophozoites of Entamoeba histolytica

Fatemeh Mahdavi Abhari et al.

WIENER KLINISCHE WOCHENSCHRIFT (2019)

Article Chemistry, Medicinal

Nitro-Group-Containing Drugs

Kunal Nepali et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Nutrition & Dietetics

Giardia intestinalis and Fructose Malabsorption: A Frequent Association

Maria Trelis et al.

NUTRIENTS (2019)

Article Biochemistry & Molecular Biology

MolProbity: More and better reference data for improved all-atom structure validation

Christopher J. Williams et al.

PROTEIN SCIENCE (2018)

Review Infectious Diseases

Nitroimidazole-refractory giardiasis: a growing problem requiring rational solutions

E. R. Carter et al.

CLINICAL MICROBIOLOGY AND INFECTION (2018)

Article Biochemistry & Molecular Biology

Biochemical Characterization and Structural Modeling of Fused Glucose-6-Phosphate Dehydrogenase-Phosphogluconolactonase from Giardia lamblia

Laura Morales-Luna et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2018)

Article Microbiology

Five facts about Giardia lamblia

Lenka Cernikova et al.

PLOS PATHOGENS (2018)

Article Biochemistry & Molecular Biology

The multicatalytic compartment of propionyl-CoA synthase sequesters a toxic metabolite

Iria Bernhardsgruetter et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biotechnology & Applied Microbiology

A comprehensive map of molecular drug targets

Rita Santos et al.

NATURE REVIEWS DRUG DISCOVERY (2017)

Review Chemistry, Medicinal

Therapeutic journey of 2,4-thiazolidinediones as a versatile scaffold: An insight into structure activity relationship

Mohd. Javed Naim et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Chemistry, Medicinal

Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum

Blanca Colin-Lozano et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

Review Biochemistry & Molecular Biology

Thiazolidine-2,4-dione derivatives: Programmed chemical weapons for key protein targets of various pathological conditions

Navriti Chadha et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2015)

Article Biochemistry & Molecular Biology

Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase is a potential drug target

Stacey M. Allen et al.

FEBS JOURNAL (2015)

Article Oncology

Glucose-6-phosphate Dehydrogenase: a Biomarker and Potential Therapeutic Target for Cancer

Chunhua Zhang et al.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2014)

Review Parasitology

Nitro drugs for the treatment of trypanosomatid diseases: past, present, and future prospects

Stephen Patterson et al.

TRENDS IN PARASITOLOGY (2014)

Article Multidisciplinary Sciences

Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity

Yukiko Miyamoto et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

Article Pharmacology & Pharmacy

Synthesis, in vitro aerobic and hypoxic cytotoxicity and radiosensitizing activity of novel metronidazole tethered 5-fluorouracil

Khosrou Abdi et al.

DARU-JOURNAL OF PHARMACEUTICAL SCIENCES (2013)

Review Microbiology

Zoonotic Potential and Molecular Epidemiology of Giardia Species and Giardiasis

Yaoyu Feng et al.

CLINICAL MICROBIOLOGY REVIEWS (2011)

Article Infectious Diseases

Characterization of Giardia lamblia WBC6 clones resistant to nitazoxanide and to metronidazole

Joachim Mueller et al.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2007)

Article Microbiology

A novel Giardia lamblia nitroreductase, GlNR1, interacts with nitazoxanide and other thiazolides

Joachim Muller et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2007)

Article Biochemical Research Methods

Structural studies of glucose-6-phosphate and NADP+ binding to human glucose-6-phosphate dehydrogenase

M Kotaka et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2005)

Article Chemistry, Multidisciplinary

UCSF chimera - A visualization system for exploratory research and analysis

EF Pettersen et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2004)