The Discovery of Tropane‐derived CCR5 Receptor Antagonists [PDF]
Chemical Biology & Drug Design, 2006 The development of compound 1, a piperidine‐based CCR5 receptor antagonist with Type I CYP2D6 inhibition, into the tropane‐derived analogue 5, is described. This compound, which is devoid of CYP2D6 liabilities, is a highly potent ligand for the CCR5 receptor and has broad‐spectrum activity against a range of clinically relevant HIV isolates.
Duncan R, Armour +6 more
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Localization-Specific Expression of CCR1 and CCR5 by Mast Cell Progenitors
Frontiers in Immunology, 2020 Mast cells are powerful immune cells found predominately in barrier tissues. They play an important role in immune surveillance and act as effector cells in allergic reactions.
Maya Salomonsson +3 more
doaj +1 more source
The G protein coupled receptor CCR5 in cancer [PDF]
, 2020 The G coupled protein receptor CC chemokine receptor type 5 (CCR5) has the unusual characteristic in humans of being a developmentally non-essential gene that participates in several pathological processes including infection with HIV (Dean et al., 1996; Gupta et al., 2019; Samson et al., 1996), progression of stroke (Joy et al., 2019), osteoporosis ...
Chandan, Upadhyaya +5 more
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Upregulation of surface feline CXCR4 expression following ectopic expression of CCR5: implications for studies of the cell tropism of feline immunodeficiency virus [PDF]
, 2002 Feline CXCR4 and CCR5 were expressed in feline cells as fusion proteins with enhanced green fluorescent protein (EGFP). Expression of the EGFP fusion proteins was localized to the cell membrane, and surface expression of CXCR4 was confirmed by using a ...
Hosie, M.J., Willett, B.J., Cannon, C.A.
core +1 more source
Evolution of CCR5 and CCR2 Genes in Bats Showed Multiple Independent Gene Conversion Events
Viruses, 2022 Chemokine receptors are an important determinant for the infectiousness of different pathogens, which are able to target the host cells by binding to the extracellular domains of these proteins.
Alexandre P. Fernandes +4 more
doaj +1 more source
Blockade of attachment and fusion receptors inhibits HIV-1 infection of human cervical tissue [PDF]
, 2004 Identification of cellular factors involved in HIV-1 entry and transmission at mucosal surfaces is critical for understanding viral pathogenesis and development of effective prevention strategies. Here we describe the evaluation of HIV-1 entry inhibitors
Ines Frank +26 more
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HIV-1 Tropism Determines Different Mutation Profiles in Proviral DNA. [PDF]
PLoS ONE, 2015 In order to establish new infections HIV-1 particles need to attach to receptors expressed on the cellular surface. HIV-1 particles interact with a cell membrane receptor known as CD4 and subsequently with another cell membrane molecule known as a co ...
Sieberth Nascimento-Brito +9 more
doaj +1 more source
Retrovirology, 2004 Background CCR5 and CXCR4 are the two main coreceptors essential for HIV entry. Therefore, these chemokine receptors have become important targets in the search for anti-HIV agents.
De Clercq Erik +4 more
doaj +1 more source
Investigation into imbalance of Th1/Th2 cells in cirrhotic, hypersplenic rats
Journal of International Medical Research, 2020 Objectives To evaluate the Th1/Th2 cell profile in spleens of cirrhotic and hypersplenic rats by investigating the expression of Th1-associated chemokine receptors CXCR3, CCR5 and Th2-associated chemokine receptor CCR3.
Yunfu Lv +4 more
doaj +1 more source
Potent Anti-HIV Chemokine Analogs Direct Post-Endocytic Sorting of CCR5. [PDF]
PLoS ONE, 2015 G protein-coupled receptors (GPCRs) are desensitized and internalized following activation. They are then subjected to post-endocytic sorting (degradation, slow recycling or fast recycling).
Claudia Bönsch +4 more
doaj +1 more source