Results 71 to 80 of about 5,417,177 (410)

Synthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2023
A series of 20 newly designed (E)-1-(4-sulphamoylphenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones was synthesised and assessed as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors towards four human isoforms of pharmaceutical interest, that is, hCA I ...
Farhat Ramzan   +10 more
doaj   +1 more source

Synthetic Routes to a Library of Novel Methionine Synthase Inhibitors [PDF]

open access: yes, 2020
Fungal infections are of continuous concern, especially with regard to immunocompromised patients. In an effort to develop new potential anti-fungal agents, we have begun synthesizing a library of potential inhibitors of the fungal Methionine Synthase ...
Bennett, Zachary   +4 more
core   +1 more source

Ornithine decarboxylase activity, a clinical biomarker for evaluating cancer chemopreventive efficacy of phytomolecules [PDF]

open access: yes, 2011
Biomarkers of cancer have made a strong traipse in predicting the disease pattern and contributed significantly to the understanding of tumour state, progression, characteristics and response to therapies.
Nusrat Masood   +2 more
core   +2 more sources

Making tau amyloid models in vitro: a crucial and underestimated challenge

open access: yesFEBS Letters, EarlyView.
This review highlights the challenges of producing in vitro amyloid assemblies of the tau protein. We review how accurately the existing protocols mimic tau deposits found in the brain of patients affected with tauopathies. We discuss the important properties that should be considered when forming amyloids and the benchmarks that should be used to ...
Julien Broc, Clara Piersson, Yann Fichou
wiley   +1 more source

Unraveling Mycobacterium tuberculosis acid resistance and pH homeostasis mechanisms

open access: yesFEBS Letters, EarlyView.
Mycobacterium tuberculosis exhibits a remarkable resilience to acid stress. In this Review, we discuss some of the molecular mechanisms and metabolic pathways used by the tubercle bacilli to adapt and resist host‐mediated acid stress. Mycobacterium tuberculosis (Mtb) is a successful pathogen that has developed a variety of strategies to survive and ...
Janïs Laudouze   +3 more
wiley   +1 more source

Natural Inhibitors of the Aromatase Enzyme

open access: yesMolecules, 2000
The results of three years of search for natural aromatase inhibitors will be presented.
Roberto R. Gil
doaj   +1 more source

Virtual screening of Microalgal compounds as potential inhibitors of Type 2 Human Transmembrane serine protease (TMPRSS2) [PDF]

open access: yesarXiv, 2021
More than 198 million cases of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been reported that result in no fewer than 4.2 million deaths globally. The rapid spread of the disease coupled with the lack of specific registered drugs for its treatment pose a great challenge that necessitate the development of therapeutic agents from a ...
arxiv  

Refining the NaV1.7 pharmacophore of a class of venom‐derived peptide inhibitors via a combination of in silico screening and rational engineering

open access: yesFEBS Letters, EarlyView.
Venom peptides have shown promise in treating pain. Our study uses computer screening to identify a peptide that targets a sodium channel (NaV1.7) linked to chronic pain. We produced the peptide in the laboratory and refined its design, advancing the search for innovative pain therapies.
Gagan Sharma   +8 more
wiley   +1 more source

The structural basis for the selectivity of sulfonamido dicarbaboranes toward cancer-associated carbonic anhydrase IX

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2020
Human carbonic anhydrase IX (CA IX), a protein specifically expressed on the surface of solid tumour cells, represents a validated target both for anticancer therapy and diagnostics.
Michael Kugler   +10 more
doaj   +1 more source

Substrate-Specific Inhibition Constants for Phospholipase A2 Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics. [PDF]

open access: yes, 2019
Assaying lipolytic enzymes is extremely challenging because they act on water-insoluble lipid substrates, which are normally components of micelles, vesicles, and cellular membranes.
Armando, Aaron   +2 more
core   +6 more sources

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