Light-regulated allosteric switch enables temporal and subcellular control of enzyme activity
Engineered allosteric regulation of protein activity provides significant advantages for the development of robust and broadly applicable tools. However, the application of allosteric switches in optogenetics has been scarce and suffers from critical ...
Mark Shaaya +14 more
doaj +1 more source
Allosteres to regulate neurotransmitter sulfonation [PDF]
Catecholamine neurotransmitter levels in the synapses of the brain shape human disposition-cognitive flexibility, aggression, depression, and reward seeking-and manipulating these levels is a major objective of the pharmaceutical industry. Certain neurotransmitters are extensively sulfonated and inactivated by human sulfotransferase 1A3 (SULT1A3).
Kristie, Darrah +5 more
openaire +2 more sources
Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]
Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili +18 more
core +2 more sources
Modeling metabolism is fundamental for cell factory design. Central carbon metabolism (CCM) is particularly important as it provides the energy and precursors for other biological processes.
Daniel eMachado +2 more
doaj +1 more source
Modes of allosteric regulation of the ubiquitination machinery [PDF]
Ubiquitination is a post-translational modification crucial for cellular signaling. A diverse range of enzymes constitute the machinery that mediates attachment of ubiquitin onto target proteins. This diversity allows the targeting of various proteins in a highly regulated fashion.
Rennie, Martin L. +2 more
openaire +2 more sources
Emerging maps of allosteric regulation in cellular networks [PDF]
Allosteric regulation is classically defined as action at a distance, where a perturbation outside of a protein active site affects function. While this definition has motivated many studies of allosteric mechanisms at the level of protein structure ...
Christopher J.P. Mathy +3 more
core +1 more source
Functional selectivity of insulin receptor revealed by aptamer-trapped receptor structures
DNA aptamers can activate insulin receptor as selective agonists or positive allosteric modulators. Here, authors determine structures of the insulin receptor bound to aptamers and provide a basis for the selective activation or allosteric regulation of ...
Junhong Kim +8 more
doaj +1 more source
p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia [PDF]
Background: The t(9;22) translocation leads to the formation of the chimeric breakpoint cluster region/c-abl oncogene 1 (BCR/ABL) fusion gene on der22, the Philadelphia chromosome.
Mahajna, Jamal +12 more
core +1 more source
Engineering and exploiting synthetic allostery of NanoLuc luciferase
Allosteric regulation of proteins allows transduction and interconversion of biochemical signals. Here the authors construct an allosteric version of circular permutated NanoLuc that can be activated by a ligand; they use this to create biosensors to ...
Zhong Guo +10 more
doaj +1 more source
Allosteric regulation of phenylalanine hydroxylase [PDF]
The liver enzyme phenylalanine hydroxylase is responsible for conversion of excess phenylalanine in the diet to tyrosine. Phenylalanine hydroxylase is activated by phenylalanine; this activation is inhibited by the physiological reducing substrate tetrahydrobiopterin.
openaire +2 more sources

