Biochemistry – Page 2

University of Oklahoma researcher leads efforts to unravel mysteries of cognitive decline

An estimated 76,000 Oklahomans are living with Alzheimer’s disease, a number that has surged by 13% in just five years. Yet, despite the increasing need for effective treatments, therapies for age-related dementia have largely failed to slow or halt the disease’s progression. Now, a University of Oklahoma researcher, backed by $2.2 million in federal funding,… Continue reading University of Oklahoma researcher leads efforts to unravel mysteries of cognitive decline

Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of Acute Myeloid Leukemia

Acute myeloid leukemia (AML) is the most prevalent form of acute leukemia in adults, representing a substantial medical need, as the standard of care has not changed for the past two decades, and long-term outcome remains dismal for a large fraction of patients. Approximately 30% of AMLs carry activating mutations of the FLT3 kinase. Unfortunately,… Continue reading Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of Acute Myeloid Leukemia

Antimicrobial triazinedione inhibitors of the translocase MraY-protein E interaction site: synergistic effects with bacitracin imply a new mechanism of action

Escherichia coli translocase MraY is the target for bacteriolytic protein E from bacteriophage φX174, interacting at a site close to Phe-288 on helix 9, on the extracellular face of the protein. A peptide motif Arg-Trp-x-x-Trp from protein E was used to design a set of triazinedione peptidomimetics, which inhibit particulate MraY (6d IC50 48 µM),… Continue reading Antimicrobial triazinedione inhibitors of the translocase MraY-protein E interaction site: synergistic effects with bacitracin imply a new mechanism of action

Design, Synthesis and Evaluation of Pyrimidinobenzylamide and Pyrimidinothiophenamide Derivatives as Inhibitors of DOT1L and Related Epigenetic Targets DNMT3a, PRMT4 and other HMTs

The histone methyltransferase DOT1L (DOT1 like, disruptor of telomeric silencing) is responsible of methylation of H3K79, leading to oncogene transcription, and its involved in the development of different types of cancers such as MLL-rearranged leukemia (MLL-r, Myeloid-Lymphoid Leukemia). Inhibitors of DOT1L have a therapeutic potential. Thus, we present herein the in silico based design and… Continue reading Design, Synthesis and Evaluation of Pyrimidinobenzylamide and Pyrimidinothiophenamide Derivatives as Inhibitors of DOT1L and Related Epigenetic Targets DNMT3a, PRMT4 and other HMTs

Chemical looping turns environmental waste into fuel

Turning environmental waste into useful chemical resources could solve many of the inevitable challenges of our growing amounts of discarded plastics, paper and food waste, according to new research.

Scientists ‘mimic real biological processes’ using synthetic neurons

A new collaboration has unlocked new potential for the field by creating a novel high-performance organic electrochemical neuron that responds within the frequency range of human neurons.