Results 51 to 60 of about 702,558 (291)
Scientific Reports, 2017 As class C GPCRs and regulators of synaptic activity, human metabotropic glutamate receptors (mGluRs) 4 and 5 are prime targets for allosteric modulation, with mGlu5 inhibition or mGlu4 stimulation potentially treating conditions like chronic pain and ...
James A. R. Dalton +2 more
doaj +1 more source
Frontiers in Pharmacology, 2018 The A2A adenosine (A2AR) and D2 dopamine (D2R) receptors form oligomers in the cell membrane and allosteric interactions across the A2AR–D2R heteromer represent a target for development of drugs against central nervous system disorders.
Dasiel O. Borroto-Escuela +8 more
doaj +1 more source
The mesenchymal stem cell differentiation to osteoblasts is potentiate by the allosteric modulation of A2B adenosine receptors. [PDF]
, 2015 The A2B adenosine receptor (A2BAR) has been recently emerged as the major adenosine receptor involved in the mesenchymal stem cell differentiation to osteoblast and bone formation, highlighting this receptor as a new target in bone diseases.
GIACOMELLI, CHIARA +9 more
core
Membrane composition and thermodynamic identity as boundaries of life for synthetic cell research
FEBS Letters, EarlyView.What makes a cell a cell? The boundary of a living cell is not just a wall. Read as a Markov blanket, the membrane separates internal from external states, generating identity and non‐equilibrium order. Can this identity be rebuilt from scratch in a synthetic cell?
Caterina Presutti, Bert Poolman
wiley +1 more source
Allosteric Modulators: A Side Door [PDF]
Journal of Medicinal Chemistry, 2015 Allosteric modulators of the cannabinoid CB1 receptor were first discovered in 2005. Since then, although both negative and positive allosteric modulators have been uncovered, many questions remain about their site(s) of action, as well as the basis of their signaling.
openaire +2 more sources
Molecular Oncology, EarlyView.Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla +9 more
wiley +1 more source
Molecular sites for the positive allosteric modulation of glycine receptors by endocannabinoids.
PLoS ONE, 2011 Glycine receptors (GlyRs) are transmitter-gated anion channels of the Cys-loop superfamily which mediate synaptic inhibition at spinal and selected supraspinal sites.
Gonzalo E Yévenes +1 more
doaj +1 more source
The Structural Basis of ATP as an Allosteric Modulator [PDF]
PLoS Computational Biology, 2014 Adenosine-5'-triphosphate (ATP) is generally regarded as a substrate for energy currency and protein modification. Recent findings uncovered the allosteric function of ATP in cellular signal transduction but little is understood about this critical behavior of ATP.
Shaoyong Lu +6 more
openaire +4 more sources
Filamentation modulates allosteric regulation of PRPS
eLife, 2022 Phosphoribosyl pyrophosphate (PRPP) is a key intermediate in the biosynthesis of purine and pyrimidine nucleotides, histidine, tryptophan, and cofactors NAD and NADP. Abnormal regulation of PRPP synthase (PRPS) is associated with human disorders, including Arts syndrome, retinal dystrophy, and gouty arthritis.
Chia-Chun Chang +9 more
openaire +3 more sources
Loss of proton‐sensing TDAG8 increases tumor progression in mouse models of colon cancer
Molecular Oncology, EarlyView.Loss of the pH‐sensing receptor TDAG8 accelerates colorectal cancer progression in mice. Animals lacking TDAG8 expression had increased tumor growth, DNA damage, and recruitment of tumor‐associated immune cells, including macrophages, neutrophils, and monocytes.
Ermanno Malagola +11 more
wiley +1 more source