Results 51 to 60 of about 3,716,801 (336)

Construction of Novel Aspartokinase Mutant A380I and Its Characterization by Molecular Dynamics Simulation

open access: yesMolecules, 2018
In this study, a novel monomer aspartokinase (AK) from Corynebacterium pekinense was identified, and its monomer model was constructed. Site 380 was identified by homologous sequencing and monomer model comparison as the key site which was conserved and ...
Caijing Han   +4 more
doaj   +1 more source

Natural products targeting human lactate dehydrogenases for cancer therapy: A mini review

open access: yesFrontiers in Chemistry, 2022
Reprogramming cancer metabolism has become the hallmark of cancer progression. As the key enzyme catalyzing the conversion of pyruvate to lactate in aerobic glycolysis of cancer cells, human lactate dehydrogenase (LDH) has been a promising target in the ...
Huankai Yao, Feng Yang, Yan Li
doaj   +1 more source

FoxO1 signaling in B cell malignancies and its therapeutic targeting

open access: yesFEBS Letters, EarlyView.
FoxO1 has context‐specific tumor suppressor or oncogenic character in myeloid and B cell malignancies. This includes tumor‐promoting properties such as stemness maintenance and DNA damage tolerance in acute leukemias, or regulation of cell proliferation and survival, or migration in mature B cell malignancies.
Krystof Hlavac   +3 more
wiley   +1 more source

Usage of Mitogen-Activated Protein Kinase Small Molecule Inhibitors: More Than Just Inhibition!

open access: yesFrontiers in Pharmacology, 2018
We have identified a phenomenon occurring in the usage of proposed “specific” Mitogen-activated protein kinase (MAPK) inhibitors. We found that especially inhibitors of p38 potentiate the activation of other MAPKs in various cell types. This finding will
Steffen K. Meurer, Ralf Weiskirchen
doaj   +1 more source

Translational Potential of Immune Tolerance Induction by AAV Liver-Directed Factor VIII Gene Therapy for Hemophilia A

open access: yesFrontiers in Immunology, 2020
Hemophilia A (HA) is an X-linked bleeding disorder due to deficiencies in coagulation factor VIII (FVIII). The major complication of current protein-based therapies is the development of neutralizing anti-FVIII antibodies, termed inhibitors, that block ...
Benjamin J. Samelson-Jones   +5 more
doaj   +1 more source

The immunological interface: dendritic cells as key regulators in metabolic dysfunction‐associated steatotic liver disease

open access: yesFEBS Letters, EarlyView.
Metabolic dysfunction‐associated steatotic liver disease (MASLD) affects nearly one‐third of the global population and poses a significant risk of progression to cirrhosis or liver cancer. Here, we discuss the roles of hepatic dendritic cell subtypes in MASLD, highlighting their distinct contributions to disease initiation and progression, and their ...
Camilla Klaimi   +3 more
wiley   +1 more source

Synthesis and Biological Evaluation of 2-Phenoxyacetamide Analogues, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors

open access: yesMolecules, 2014
Monoamine oxidases (EC 1.4.3.4; MAOs), a family of FAD-containing enzymes, is an important target for antidepressant drugs. In this paper, a series of 2-phenoxyacetamide analogues were synthesized, and their inhibitory potency towards monoamine oxidases ...
Wei Shen   +4 more
doaj   +1 more source

Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition

open access: yesBeilstein Journal of Organic Chemistry, 2020
Guided by computational analysis, herein we report the design, synthesis and evaluation of four novel diazine-based histone deacetylase inhibitors (HDACis). The targets of interest (TOI) are analogues of panobinostat, one of the most potent and versatile
Sivaraman Balasubramaniam   +8 more
doaj   +1 more source

Evaluation of Artificial Intelligence in Participating Structure-Based Virtual Screening for Identifying Novel Interleukin-1 Receptor Associated Kinase-1 Inhibitors

open access: yesFrontiers in Oncology, 2020
Interleukin-1 receptor associated kinase-1 (IRAK1) exhibits important roles in inflammation, infection, and autoimmune diseases; however, only a few inhibitors have been discovered.
Jinxin Che   +17 more
doaj   +1 more source

Defining stage-specific activity of potent new inhibitors of Cryptosporidium parvum growth in vitro [PDF]

open access: yes, 2020
Currently, nitazoxanide is the only FDA-approved treatment for cryptosporidiosis; unfortunately, it is ineffective in immunocompromised patients, has varied efficacy in immunocompetent individuals, and is not approved in infants under 1 year of age ...
Funkhouser-Jones, Lisa J   +2 more
core   +2 more sources

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