PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 21464424-1 2011 Fingolimod is a functional antagonist of the sphingosine-1-phosphate receptor 1 and thereby inhibits sphingosine-1-phosphate-dependent lymphocyte egress from secondary lymphoid tissues, resulting in a pronounced lymphopenia in the peripheral blood. Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 45-79 19814729-4 2009 The S1P mimetic FTY720-phosphate causes internalization and degradation of cell membrane-expressed S1P1, thereby antagonizing S1P action at the receptor. Fingolimod Hydrochloride 16-22 sphingosine-1-phosphate receptor 1 Homo sapiens 99-103 20413685-9 2010 Using S1P receptor specific agonists and antagonists, we determined that fingolimod-induced effects on remyelination and astrogliosis were mediated primarily through S1P3 and S1P5, whereas enhanced microgliosis was mediated through S1P1 and S1P5. Fingolimod Hydrochloride 73-83 sphingosine-1-phosphate receptor 1 Homo sapiens 232-236 24900328-3 2011 It has been postulated that fingolimod"s efficacy is due to S1P1 agonism, while its cardiovascular side effects (transient bradycardia and hypertension) are due to S1P3 agonism. Fingolimod Hydrochloride 28-38 sphingosine-1-phosphate receptor 1 Homo sapiens 60-64 21710707-12 2011 Fingolimod acts on sphingosine 1-phosphate receptors-1 (S1P1). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 19-60 18474015-4 2008 The sphingosine analogue, FTY720 (fingolimod), a high affinity agonist of sphingosine-1-phosphate type-1 receptor (S1P-1), acts primarily by sequestering lymphocytes within peripheral lymphoid organs rendering them incapable of migrating to the sites of inflammation. Fingolimod Hydrochloride 26-32 sphingosine-1-phosphate receptor 1 Homo sapiens 74-113 18474015-4 2008 The sphingosine analogue, FTY720 (fingolimod), a high affinity agonist of sphingosine-1-phosphate type-1 receptor (S1P-1), acts primarily by sequestering lymphocytes within peripheral lymphoid organs rendering them incapable of migrating to the sites of inflammation. Fingolimod Hydrochloride 26-32 sphingosine-1-phosphate receptor 1 Homo sapiens 115-120 18474015-4 2008 The sphingosine analogue, FTY720 (fingolimod), a high affinity agonist of sphingosine-1-phosphate type-1 receptor (S1P-1), acts primarily by sequestering lymphocytes within peripheral lymphoid organs rendering them incapable of migrating to the sites of inflammation. Fingolimod Hydrochloride 34-44 sphingosine-1-phosphate receptor 1 Homo sapiens 74-113 18474015-4 2008 The sphingosine analogue, FTY720 (fingolimod), a high affinity agonist of sphingosine-1-phosphate type-1 receptor (S1P-1), acts primarily by sequestering lymphocytes within peripheral lymphoid organs rendering them incapable of migrating to the sites of inflammation. Fingolimod Hydrochloride 34-44 sphingosine-1-phosphate receptor 1 Homo sapiens 115-120 35158767-3 2022 FTY720 (Fingolimod), which targets SphK1 and S1P1, prevented HIF-1alpha accumulation, and also inhibited cell proliferation in both normoxia and hypoxia unlike conventional chemotherapy. Fingolimod Hydrochloride 8-18 sphingosine-1-phosphate receptor 1 Homo sapiens 45-49 16549044-10 2006 Thus, it is presumed that FTY720-induced lymphocyte sequestration is due to the inhibition of S1P/S1P1-dependent lymphocyte egress from secondary lymphoid tissues and thymus by its active metabolite (S)-FTY720-P. Fingolimod Hydrochloride 26-32 sphingosine-1-phosphate receptor 1 Homo sapiens 98-102 16393960-4 2006 We showed that sphingosine 1-phosphate receptor-1 agonist FTY720 induces relocation of circulating memory CD4 T cells into secondary lymphoid organs. Fingolimod Hydrochloride 58-64 sphingosine-1-phosphate receptor 1 Homo sapiens 15-49 16365393-1 2006 FTY720 is a high-affinity agonist at the sphingosine 1-phosphate receptor 1 that prevents lymphocyte egress from lymphoid tissue and prolongs allograft survival in several animal models of solid organ transplantation. Fingolimod Hydrochloride 0-6 sphingosine-1-phosphate receptor 1 Homo sapiens 41-75 30083262-9 2018 FTY720 in combination with gemcitabine breached the mitochondrial membrane potential, altered the S1PR1-STAT3 loop, and inhibited epithelial to mesenchymal (EMT) transition. Fingolimod Hydrochloride 0-6 sphingosine-1-phosphate receptor 1 Homo sapiens 98-103 33603656-1 2021 Background: The sphingosine-1-phosphate receptor (S1PR) modulator fingolimod (FTY720), which is commonly used as an immunomodulator in multiple sclerosis treatment, has recently been found to reduce pathological changes in the brain tissue of Alzheimer"s disease (AD) animal models, but this has yet to be verified in human brain tissue. Fingolimod Hydrochloride 66-76 sphingosine-1-phosphate receptor 1 Homo sapiens 50-54 33603656-1 2021 Background: The sphingosine-1-phosphate receptor (S1PR) modulator fingolimod (FTY720), which is commonly used as an immunomodulator in multiple sclerosis treatment, has recently been found to reduce pathological changes in the brain tissue of Alzheimer"s disease (AD) animal models, but this has yet to be verified in human brain tissue. Fingolimod Hydrochloride 78-84 sphingosine-1-phosphate receptor 1 Homo sapiens 50-54 31526917-1 2019 Fingolimod inhibits the egress of lymphocytes from lymphatic tissues and also directly affects their functions by modulation of the sphingosine-1-phosphate receptor 1 (S1P1). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 132-166 31526917-1 2019 Fingolimod inhibits the egress of lymphocytes from lymphatic tissues and also directly affects their functions by modulation of the sphingosine-1-phosphate receptor 1 (S1P1). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 168-172 30785748-2 2019 In comparison to fingolimod (1), a full agonist of S1P1 currently marketed for the treatment of relapse remitting multiple sclerosis (RRMS), 2 offers several potential advantages having demonstrated improved safety multiples in preclinical evaluations against undesired pulmonary and cardiovascular effects. Fingolimod Hydrochloride 17-27 sphingosine-1-phosphate receptor 1 Homo sapiens 51-55 30828332-7 2019 Comparison of peripheral blood ILC numbers between fingolimod-receiving and treatment-free MS patients revealed that, in vivo, ILCs respond to fingolimod, an S1PR1 agonist, resulting in ILC-penia in circulation. Fingolimod Hydrochloride 51-61 sphingosine-1-phosphate receptor 1 Homo sapiens 158-163 30828332-7 2019 Comparison of peripheral blood ILC numbers between fingolimod-receiving and treatment-free MS patients revealed that, in vivo, ILCs respond to fingolimod, an S1PR1 agonist, resulting in ILC-penia in circulation. Fingolimod Hydrochloride 143-153 sphingosine-1-phosphate receptor 1 Homo sapiens 158-163 30828332-9 2019 Importantly, ex vivo exposure of ILC3 and ILC1 to fingolimod or SEW2871, another S1PR1 antagonist, reduced production of ILC3- and ILC1- associated cytokines GM-CSF, IL-22, IL-17, and IFN-gamma, respectively. Fingolimod Hydrochloride 50-60 sphingosine-1-phosphate receptor 1 Homo sapiens 81-86 33797705-1 2021 Fingolimod (Gilenya) received regulatory approval from the US FDA in 2010 as the first-in-class sphingosine 1-phosphate (S1P) receptor (S1PR) modulator and was the first oral disease-modifying therapy (DMT) used for the treatment of the relapsing forms of multiple sclerosis (MS). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 136-140 33797705-7 2021 Improved understanding of fingolimod"s mechanism of action has provided strategies for the development of the more selective second-generation S1PR modulators. Fingolimod Hydrochloride 26-36 sphingosine-1-phosphate receptor 1 Homo sapiens 143-147 33797705-16 2021 This review covers the available data about the mechanisms of action, pharmacodynamics and kinetics, efficacy, safety, and tolerability of the various S1PR modulators for patients with relapsing-remitting, secondary progressive, and, for fingolimod, primary progressive MS. Fingolimod Hydrochloride 238-248 sphingosine-1-phosphate receptor 1 Homo sapiens 151-155 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 81-87 sphingosine-1-phosphate receptor 1 Homo sapiens 36-51 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 81-87 sphingosine-1-phosphate receptor 1 Homo sapiens 53-58 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 88-98 sphingosine-1-phosphate receptor 1 Homo sapiens 36-51 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 88-98 sphingosine-1-phosphate receptor 1 Homo sapiens 53-58 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 212-222 sphingosine-1-phosphate receptor 1 Homo sapiens 36-51 33010954-5 2020 Functional sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) antagonists, such as FTY720/fingolimod, used clinically for non-pain conditions, are emerging as non-narcotic analgesics, supporting the repurposing of fingolimod for chronic pain treatment and energizing drug discovery focused on S1P signaling. Fingolimod Hydrochloride 212-222 sphingosine-1-phosphate receptor 1 Homo sapiens 53-58 28716816-6 2017 We show in vitro and in human NB xenograft models that treatment with FTY720, an FDA-approved drug and antagonist of S1PR1, dramatically sensitizes drug-resistant cells to etoposide. Fingolimod Hydrochloride 70-76 sphingosine-1-phosphate receptor 1 Homo sapiens 117-122 26130058-1 2015 Fingolimod affords protection from MS by sequestering lymphocytes in secondary lymphoid organs via down regulation of their sphingosine 1 phosphate receptor (S1P1). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 158-162 27055778-6 2016 Phosphorylated-fingolimod was shown in vitro to reduce S1PR1 RNA and protein, to slightly increase viability and to activate anti-apoptotic Bcl2 in transformed B cells of patients with MS. Fingolimod Hydrochloride 15-25 sphingosine-1-phosphate receptor 1 Homo sapiens 55-60 28356890-2 2017 Sphingosine-1-phosphate receptor (S1PR1) modulators have been approved for the management of MS. Phosphorylated fingolimod mimics endogenous sphingosine-1-phosphate (S1P), a bioactive lipid that regulates remyelination and cell injury. Fingolimod Hydrochloride 112-122 sphingosine-1-phosphate receptor 1 Homo sapiens 34-39 28356890-4 2017 This study utilized the fingolimod and amiselimod scaffolds, together with their critical binding interactions for the S1PR1 Ligand Binding Pocket, as templates for the in silico de novo design of high efficiency binding Lipinski rule-compliant molecules. Fingolimod Hydrochloride 24-34 sphingosine-1-phosphate receptor 1 Homo sapiens 119-124 27663260-3 2016 The therapeutic potential of targeting this system took center stage when it was demonstrated that the immune modulator, fingolimod (FTY720/Gilenya), exerts it lymphopenic effect by acting on S1P receptors, primarily on S1P receptor 1 (S1P1). Fingolimod Hydrochloride 121-131 sphingosine-1-phosphate receptor 1 Homo sapiens 220-234 27663260-3 2016 The therapeutic potential of targeting this system took center stage when it was demonstrated that the immune modulator, fingolimod (FTY720/Gilenya), exerts it lymphopenic effect by acting on S1P receptors, primarily on S1P receptor 1 (S1P1). Fingolimod Hydrochloride 121-131 sphingosine-1-phosphate receptor 1 Homo sapiens 236-240 26130058-7 2015 Also, consistent with the ability of S1P1 to counteract polarization and function of T regulatory lymphocytes their number and suppression of effector T cells is reduced by fingolimod suspension. Fingolimod Hydrochloride 173-183 sphingosine-1-phosphate receptor 1 Homo sapiens 37-41 25582213-2 2015 Interfering with the activation and recruitment of immune cells reduces disease activity in MS. We review the mechanism of action and treatment effects of natalizumab and fingolimod, which interfere with the recruitment of pathogenic immune cells in MS. Fingolimod blocks the egress of activated lymphocytes from lymph nodes by binding to the sphingosine-1-phosphate (S1P) receptor 1, but may also have effects on S1P receptor-expressing cells within the central nervous system (CNS). Fingolimod Hydrochloride 171-181 sphingosine-1-phosphate receptor 1 Homo sapiens 343-383 25582213-2 2015 Interfering with the activation and recruitment of immune cells reduces disease activity in MS. We review the mechanism of action and treatment effects of natalizumab and fingolimod, which interfere with the recruitment of pathogenic immune cells in MS. Fingolimod blocks the egress of activated lymphocytes from lymph nodes by binding to the sphingosine-1-phosphate (S1P) receptor 1, but may also have effects on S1P receptor-expressing cells within the central nervous system (CNS). Fingolimod Hydrochloride 254-264 sphingosine-1-phosphate receptor 1 Homo sapiens 343-383 22493799-4 2012 Fingolimod (FTY720), the novel S1PR1 agonist, has been approved for the treatment of multiple sclerosis in clinical trials. Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 31-36 26648781-2 2015 Mode of action of fingolimod is based on intense S1P1 receptor stimulation and "arresting" lymphocytes in lymphatic organs. Fingolimod Hydrochloride 18-28 sphingosine-1-phosphate receptor 1 Homo sapiens 49-53 25239520-0 2014 Prominence of central sphingosine-1-phosphate receptor-1 in attenuating abeta-induced injury by fingolimod. Fingolimod Hydrochloride 96-106 sphingosine-1-phosphate receptor 1 Homo sapiens 22-56 25239520-2 2014 The present work aims to answer whether central S1P receptor 1 (S1P1) plays significant role in the impact of fingolimod in AD. Fingolimod Hydrochloride 110-120 sphingosine-1-phosphate receptor 1 Homo sapiens 48-62 25239520-2 2014 The present work aims to answer whether central S1P receptor 1 (S1P1) plays significant role in the impact of fingolimod in AD. Fingolimod Hydrochloride 110-120 sphingosine-1-phosphate receptor 1 Homo sapiens 64-68 25518386-3 2014 In lymph node, fingolimod acts as functional antagonist, leading to internalization of sphingosine-1-phosphate 1(S1P1) receptors of lymphocytes. Fingolimod Hydrochloride 15-25 sphingosine-1-phosphate receptor 1 Homo sapiens 113-117 24069553-5 2013 FTY720, an antagonist of S1PR1, abolished persistent NFkappaB/IL-6/STAT3 signaling and reduced the development and progression of colitis-associated cancer. Fingolimod Hydrochloride 0-6 sphingosine-1-phosphate receptor 1 Homo sapiens 25-30 22999882-2 2012 Fingolimod (FTY720, Gilenya) is a S1P(1) receptor agonist that has recently been approved for the treatment of multiple sclerosis (MS). Fingolimod Hydrochloride 0-10 sphingosine-1-phosphate receptor 1 Homo sapiens 34-40 22999882-2 2012 Fingolimod (FTY720, Gilenya) is a S1P(1) receptor agonist that has recently been approved for the treatment of multiple sclerosis (MS). Fingolimod Hydrochloride 12-18 sphingosine-1-phosphate receptor 1 Homo sapiens 34-40 24239768-3 2014 In September 2010, fingolimod/FTY720 (Gilenya, Novartis) was approved as the first oral treatment for relapsing forms of MS. Fingolimod causes down-modulation of S1P1 receptors on lymphocytes which prevents the invasion of autoaggressive T cells into the CNS. Fingolimod Hydrochloride 125-135 sphingosine-1-phosphate receptor 1 Homo sapiens 162-166 23518370-4 2013 However, emerging evidence indicates that fingolimod has direct effects in the CNS in MS. For example, in the MS animal model of experimental autoimmune encephalomyelitis (EAE), fingolimod is highly efficacious in both a prophylactic and therapeutic setting, yet becomes ineffective in animals selectively deficient for S1P1 on astrocytes, despite maintained normal immunologic receptor expression and functions, and S1P-mediated immune activities. Fingolimod Hydrochloride 42-52 sphingosine-1-phosphate receptor 1 Homo sapiens 320-324 22493799-4 2012 Fingolimod (FTY720), the novel S1PR1 agonist, has been approved for the treatment of multiple sclerosis in clinical trials. Fingolimod Hydrochloride 12-18 sphingosine-1-phosphate receptor 1 Homo sapiens 31-36