Search Results - "Li, Xaria X"
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The Complement Receptor C5aR2: A Powerful Modulator of Innate and Adaptive Immunity
Published in The Journal of immunology (1950) (15-06-2019)“…Complement activation generates the core effector protein C5a, a potent immune molecule that is linked to multiple inflammatory diseases. Two C5a receptors,…”
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C5aR2 Activation Broadly Modulates the Signaling and Function of Primary Human Macrophages
Published in The Journal of immunology (1950) (15-08-2020)“…The complement activation fragment C5a is a potent proinflammatory mediator that is increasingly recognized as an immune modulator. C5a acts through two C5a…”
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Protocol for cell-based screening assay to measure ERK1/2 phosphorylation as a readout for complement receptor activation
Published in STAR protocols (15-12-2023)“…The complement receptors C3aR and C5aR1 are promising therapeutic targets. Here, we present a protocol to screen the effects of different agonists and…”
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The "C3aR Antagonist" SB290157 is a Partial C5aR2 Agonist
Published in Frontiers in pharmacology (21-01-2021)“…Innate immune complement activation generates the C3 and C5 protein cleavage products C3a and C5a, defined classically as anaphylatoxins. C3a activates C3aR,…”
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TLQP-21 is a low potency partial C3aR activator on human primary macrophages
Published in Frontiers in immunology (26-01-2023)“…TLQP-21 is a 21-amino acid neuropeptide derived from the VGF precursor protein. TLQP-21 is expressed in the nervous system and neuroendocrine glands, and…”
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Complement receptor C3aR1 controls neutrophil mobilization following spinal cord injury through physiological antagonism of CXCR2
Published in JCI insight (02-05-2019)“…Traumatic spinal cord injury (SCI) triggers an acute-phase response that leads to systemic inflammation and rapid mobilization of bone marrow (BM) neutrophils…”
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Emerging Insights into the Structure and Function of Complement C5a Receptors
Published in Trends in biochemical sciences (Amsterdam. Regular ed.) (01-08-2020)“…Complement factor C5a is an integral constituent of the complement cascade critically involved in the innate immune response, and it exerts its functions via…”
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Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors
Published in Molecular cell (18-11-2021)“…G-protein-coupled receptors (GPCRs), also known as seven transmembrane receptors (7TMRs), typically interact with two distinct signal-transducers, i.e., G…”
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SARS-CoV-2 drives NLRP3 inflammasome activation in human microglia through spike protein
Published in Molecular psychiatry (01-07-2023)“…Coronavirus disease-2019 (COVID-19) is primarily a respiratory disease, however, an increasing number of reports indicate that SARS-CoV-2 infection can also…”
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Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function
Published in Biochemical pharmacology (01-10-2020)“…[Display omitted] The complement fragment C5a is a core effector of complement activation. C5a, acting through its major receptor C5aR1, exerts powerful…”
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Cell-intrinsic C5a synergizes with Dectin-1 in macrophages to mediate fungal killing
Published in Proceedings of the National Academy of Sciences - PNAS (30-01-2024)“…The complement factor C5a is a core effector product of complement activation. C5a, acting through its receptors C5aR1 and C5aR2, exerts pleiotropic…”
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Anaphylatoxin receptor promiscuity for commonly used complement C5a peptide agonists
Published in International immunopharmacology (01-11-2021)“…•Peptides EP54, EP67 and C5apep are widely used in complement C5a research.•EP54, EP67 and C5apep have off-target activities at C5aR2 and C3aR.•EP54 and EP67…”
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New concepts on the therapeutic control of complement anaphylatoxin receptors
Published in Molecular immunology (01-09-2017)“…•Complement underlies the pathogenesis of a vast number of inflammatory disorders.•Driving the complement inflammatory response are the anaphylatoxins, C5a and…”
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Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors
Published in Cell (26-10-2023)“…The complement system is a critical part of our innate immune response, and the terminal products of this cascade, anaphylatoxins C3a and C5a, exert their…”
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Partial ligand-receptor engagement yields functional bias at the human complement receptor, C5aR1
Published in The Journal of biological chemistry (14-06-2019)“…The human complement component, C5a, binds two different seven-transmembrane receptors termed C5aR1 and C5aR2. C5aR1 is a prototypical G-protein–coupled…”
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Unexpected Off-Target Activities for Recombinant C5a in Human Macrophages
Published in The Journal of immunology (1950) (01-01-2022)“…The anaphylatoxin C5a is core effector of complement activation. C5a exerts potent proinflammatory and immunomodulatory actions through interacting with its…”
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Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity
Published in Journal of medicinal chemistry (25-11-2021)“…The anaphylatoxin C5a is a complement peptide associated with immune-related disorders. C5a binds with equal potency to two GPCRs, C5aR1 and C5aR2. Multiple…”
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C5a receptors C5aR1 and C5aR2 mediate opposing pathologies in a mouse model of melanoma
Published in The FASEB journal (01-10-2019)“…ABSTRACT The canonical complement component 5a (C5a) receptor (C5aR) 1 has well‐described roles in tumorigenesis but the contribution of the second receptor,…”
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Development of Synthetic Human and Mouse C5a: Application to Binding and Functional Assays In Vitro and In Vivo
Published in ACS pharmacology & translational science (10-12-2021)“…The complement activation peptide C5a is a key mediator of inflammation that is associated with numerous immune disorders. C5a binds and activates two…”
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THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors
Published in British journal of pharmacology (01-10-2021)“…The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular…”
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