Target Information

Target General Infomation
Target ID
T98913
Former ID
TTDS00411
Target Name
Macrophage colony-stimulating factor receptor
Gene Name
CSF3R
Synonyms
CD115; CSF-1-R; CSF1R; FMS; Fms proto-oncogene; c-fms; GCSF receptor; CSF3R
Target Type
Successful
Disease Autoimmune diabetes [ICD10: E08-E13]
Alzheimer disease [ICD9: 331; ICD10: G30]
Bone cancer [ICD10: C41.0]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Cardiovascular disorder [ICD10: I00-I99]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Leukemia [ICD9: 208.9; ICD10: C90-C95]
Neutropenia [ICD9: 288; ICD10: D70]
Non-myeloid cancer [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25]
Severe neutropaenia in non-myeloid malignancies [ICD9: 140-239; ICD10: C00-C96]
Function
Receptor for granulocyte colony-stimulating factor (CSF3), essential for granulocytic maturation. Plays a crucial role in the proliferation, differientation and survival of cells along the neutrophilic lineage. In addition it may function in some adhesion or recognition events at the cell surface.
BioChemical Class
Type I cytokine receptor
Target Validation
T98913
UniProt ID
Q99062
Sequence
MARLGNCSLTWAALIILLLPGSLEECGHISVSAPIVHLGDPITASCIIKQNCSHLDPEPQ
ILWRLGAELQPGGRQQRLSDGTQESIITLPHLNHTQAFLSCCLNWGNSLQILDQVELRAG
YPPAIPHNLSCLMNLTTSSLICQWEPGPETHLPTSFTLKSFKSRGNCQTQGDSILDCVPK
DGQSHCCIPRKHLLLYQNMGIWVQAENALGTSMSPQLCLDPMDVVKLEPPMLRTMDPSPE
AAPPQAGCLQLCWEPWQPGLHINQKCELRHKPQRGEASWALVGPLPLEALQYELCGLLPA
TAYTLQIRCIRWPLPGHWSDWSPSLELRTTERAPTVRLDTWWRQRQLDPRTVQLFWKPVP
LEEDSGRIQGYVVSWRPSGQAGAILPLCNTTELSCTFHLPSEAQEVALVAYNSAGTSRPT
PVVFSESRGPALTRLHAMARDPHSLWVGWEPPNPWPQGYVIEWGLGPPSASNSNKTWRME
QNGRATGFLLKENIRPFQLYEIIVTPLYQDTMGPSQHVYAYSQEMAPSHAPELHLKHIGK
TWAQLEWVPEPPELGKSPLTHYTIFWTNAQNQSFSAILNASSRGFVLHGLEPASLYHIHL
MAASQAGATNSTVLTLMTLTPEGSELHIILGLFGLLLLLTCLCGTAWLCCSPNRKNPLWP
SVPDPAHSSLGSWVPTIMEEDAFQLPGLGTPPITKLTVLEEDEKKPVPWESHNSSETCGL
PTLVQTYVLQGDPRAVSTQPQSQSGTSDQVLYGQLLGSPTSPGPGHYLRCDSTQPLLAGL
TPSPKSYENLWFQASPLGTLVTPAPSQEDDCVFGPLLNFPLLQGIRVHGMEALGSF
Structure
1AZ7; 2D9Q
Drugs and Mode of Action
Drug(s) Filgrastim Drug Info Approved Neutropenia [536361], [542000]
Filgrastim-SNDZ Drug Info Approved Neutropenia [551873]
Pegfilgrastim Drug Info Approved Non-myeloid cancer [536361], [542001]
Tbo-Filgrastim Drug Info Approved Severe neutropaenia in non-myeloid malignancies [532210]
Peg-G-CSF Drug Info Phase 3 Cancer [524038]
PLX-3397 Drug Info Phase 3 Alzheimer disease [525099]
AX-200 Drug Info Phase 2 Cardiovascular disorder [521663]
MAXY-G34 Drug Info Phase 2 Neutropenia [522065]
SBC-014 Drug Info Phase 2 Neutropenia [522057]
MK-6302 Drug Info Phase 1 Neutropenia [551956]
PLX-5622 Drug Info Phase 1 Autoimmune diabetes [523330]
PLX7486 Drug Info Phase 1 Pancreatic cancer [549504]
ZD-6003 Drug Info Terminated Cancer [545575]
Inhibitor AC-710 Drug Info [543466]
AZD-7507 Drug Info [543466]
BLZ-945 Drug Info [543466]
N-(2-morpholinophenyl)-5-nitrofuran-2-carboxamide Drug Info [529071]
PLX-3397 Drug Info [550447]
PLX-5622 Drug Info [544233]
PLX7486 Drug Info [550497]
Modulator AX-200 Drug Info [532461]
Filgrastim-SNDZ Drug Info [551871]
MK-6302 Drug Info [525376]
SBC-014 Drug Info [544066]
Tbo-Filgrastim Drug Info [532210]
ZD-6003 Drug Info [543466]
Binder Filgrastim Drug Info [535943], [537204]
Pegfilgrastim Drug Info [535943]
Stimulator G-CSF Drug Info [543466]
Peg-G-CSF Drug Info [543466]
ZP-G-CSF Drug Info [543466]
Agonist MAXY-G34 Drug Info [532564]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cytokine-cytokine receptor interaction
PI3K-Akt signaling pathway
Jak-STAT signaling pathway
Hematopoietic cell lineage
Pathways in cancer
NetPath Pathway Leptin Signaling Pathway
RANKL Signaling Pathway
References
Ref 521663ClinicalTrials.gov (NCT00132470) Treatment With AX200 for Acute Ischemic Stroke. U.S. National Institutes of Health.
Ref 522057ClinicalTrials.gov (NCT00497809) Safety and Efficacy Study of GCSF Therapy to Treat Patients at High Risk for Chemotherapy Induced Severe Neutropenia. U.S. National Institutes of Health.
Ref 522065ClinicalTrials.gov (NCT00501332) Evaluation of Maxy-G34 in Breast Cancer Patients Treated With TAC (Docetaxel, Adriamycin, Cyclophosphamide) Chemotherapy. U.S. National Institutes of Health.
Ref 523330ClinicalTrials.gov (NCT01282684) Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of PLX5622 in Healthy Adult Volunteers. U.S. National Institutes of Health.
Ref 524038ClinicalTrials.gov (NCT01674855) Phase III Study of DA-3031(PEG-G-CSF) in Chemotherapy-induced Neutropenia. U.S. National Institutes of Health.
Ref 525099ClinicalTrials.gov (NCT02371369) PLX3397 Phase 3 Study for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS). U.S. National Institutes of Health.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 542000(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6968).
Ref 542001(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6969).
Ref 545575Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003738)
Ref 549504Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038879)
Ref 551873Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551956Clinical pipeline report, company report or official report of Merck.
Ref 525376Merck ditches biogeneric. Nat Biotechnol. 2010 Jul;28(7):636. doi: 10.1038/nbt0710-636a.
Ref 529071Bioorg Med Chem Lett. 2007 Nov 15;17(22):6070-4. Epub 2007 Sep 19.Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 532461Granulocyte colony-stimulating factor in patients with acute ischemic stroke: results of the AX200 for Ischemic Stroke trial. Stroke. 2013 Oct;44(10):2681-7.
Ref 532564Survival efficacy of the PEGylated G-CSFs Maxy-G34 and neulasta in a mouse model of lethal H-ARS, and residual bone marrow damage in treated survivors. Health Phys. 2014 Jan;106(1):21-38.
Ref 535943Evidence that the granulocyte colony-stimulating factor (G-CSF) receptor plays a role in the pharmacokinetics of G-CSF and PegG-CSF using a G-CSF-R KO model. Pharmacol Res. 2004 Jul;50(1):55-8.
Ref 537204XM02, the first granulocyte colony-stimulating factor biosimilar, is safe and effective in reducing the duration of severe neutropenia and incidence of febrile neutropenia in patients with non-Hodgkin lymphoma receiving chemotherapy. Leuk Lymphoma. 2009 Mar;50(3):374-9.
Ref 543466(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1719).
Ref 544066A glycosylated recombinant human granulocyte colony stimulating factor produced in a novel protein production system (AVI-014) in healthy subjects: a first-in human, single dose, controlled study. BMC Clin Pharmacol. 2009; 9: 2.
Ref 544233Microglial Stimulation of Glioblastoma Invasion Involves Epidermal Growth Factor Receptor (EGFR) and Colony Stimulating Factor 1 Receptor (CSF-1R) Signaling. Mol Med. 2012; 18(1): 519-527.
Ref 550447National Cancer Institute Drug Dictionary (drug id 659167).
Ref 550497National Cancer Institute Drug Dictionary (drug id 747694).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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