Target Information
| Target General Information | Top | |||||
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| Target ID |
T73097
(Former ID: TTDS00442)
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| Target Name |
GMCSFR-alpha (CSF2RA)
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| Synonyms |
GMR; GM-CSFR; GM-CSF-R-alpha; CSF2RA; CDw116; CD116 antigen
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| Gene Name |
CSF2RA
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Transplanted organ/tissue [ICD-11: QB63] | |||||
| Function |
Low affinity receptor for granulocyte-macrophage colony- stimulating factor. Transduces a signal that results in the proliferation, differentiation, and functional activation of hematopoietic cells.
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| BioChemical Class |
Type I cytokine receptor family
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| UniProt ID | ||||||
| Sequence |
MLLLVTSLLLCELPHPAFLLIPEKSDLRTVAPASSLNVRFDSRTMNLSWDCQENTTFSKC
FLTDKKNRVVEPRLSNNECSCTFREICLHEGVTFEVHVNTSQRGFQQKLLYPNSGREGTA AQNFSCFIYNADLMNCTWARGPTAPRDVQYFLYIRNSKRRREIRCPYYIQDSGTHVGCHL DNLSGLTSRNYFLVNGTSREIGIQFFDSLLDTKKIERFNPPSNVTVRCNTTHCLVRWKQP RTYQKLSYLDFQYQLDVHRKNTQPGTENLLINVSGDLENRYNFPSSEPRAKHSVKIRAAD VRILNWSSWSEAIEFGSDDGNLGSVYIYVLLIVGTLVCGIVLGFLFKRFLRIQRLFPPVP QIKDKLNDNHEVEDEIIWEEFTPEEGKGYREEVLTVKEIT Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Sargramostim | Drug Info | Approved | Bone marrow transplantation | [2], [3] | |
| Clinical Trial Drug(s) | [+] 10 Clinical Trial Drugs | + | ||||
| 1 | B-cell lymphoma vaccine | Drug Info | Preregistration | Follicular lymphoma | [4] | |
| 2 | Molgramostim | Drug Info | Phase 3 | Autoimmune pulmonary alveolar proteinosis | [5] | |
| 3 | Pixykine | Drug Info | Phase 3 | Human immunodeficiency virus infection | [6] | |
| 4 | AFTVac | Drug Info | Phase 2 | Glioblastoma multiforme | [7] | |
| 5 | GM-CSF cancer vaccine | Drug Info | Phase 2 | Solid tumour/cancer | [8] | |
| 6 | Leukemia cancer vaccine | Drug Info | Phase 2 | Acute myeloid leukaemia | [9] | |
| 7 | Mavrilimumab | Drug Info | Phase 2 | Rheumatoid arthritis | [10], [11] | |
| 8 | Myeloma cancer vaccine | Drug Info | Phase 2 | Multiple myeloma | [9] | |
| 9 | MOR-103 | Drug Info | Phase 1/2 | Multiple sclerosis | [12] | |
| 10 | KH-901 | Drug Info | Phase 1 | Solid tumour/cancer | [13] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | SDZ-62-826 | Drug Info | Terminated | Solid tumour/cancer | [14] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | Sargramostim | Drug Info | [1], [15] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | Molgramostim | Drug Info | [17] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Pixykine | Drug Info | [18] | |||
| 2 | SDZ-62-826 | Drug Info | [19] | |||
| Stimulator | [+] 1 Stimulator drugs | + | ||||
| 1 | BBT-007 | Drug Info | [19] | |||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Cytokine-cytokine receptor interaction | |||||
| 2 | Jak-STAT signaling pathway | |||||
| 3 | Hematopoietic cell lineage | |||||
| 4 | Pathways in cancer | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | IL3 Signaling Pathway | |||||
| 2 | RANKL Signaling Pathway | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | GMCSF-mediated signaling events | |||||
| 2 | Alpha9 beta1 integrin signaling events | |||||
| Reactome | [+] 6 Reactome Pathways | + | ||||
| 1 | GPVI-mediated activation cascade | |||||
| 2 | G beta:gamma signalling through PI3Kgamma | |||||
| 3 | Interleukin-3, 5 and GM-CSF signaling | |||||
| 4 | RAF/MAP kinase cascade | |||||
| 5 | Surfactant metabolism | |||||
| 6 | Interleukin receptor SHC signaling | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | Interleukin-2 signaling | |||||
| 2 | Interleukin-3, 5 and GM-CSF signaling | |||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Stem cell transplantation and hematopoietic growth factors. Curr Hematol Rep. 2002 Nov;1(2):103-9. | |||||
| REF 2 | URL: 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: 7905). | |||||
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006688) | |||||
| REF 5 | ClinicalTrials.gov (NCT04544293) Clinical Trial of Inhaled Molgramostim Nebulizer Solution in Autoimmune Pulmonary Alveolar Proteinosis (aPAP) (IMPALA-2). U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT00001338) A Prospective, Randomized, Phase III Trial of FLAC (5-Fluorouracil, Leucovorin, Adriamycin, Cytoxan) Chemotherapy With GM-CSF (Granulocyte-Macrophage Colony-Stimulating Factor) Versus PIXY 321 in Advanced Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 7 | Phase II randomized trial of autologous formalin-fixed tumor vaccine for postsurgical recurrence of hepatocellular carcinoma. Clin Cancer Res. 2004 Mar 1;10(5):1574-9. | |||||
| REF 8 | A safety and efficacy trial of lethally irradiated allogeneic pancreatic tumor cells transfected with the GM-CSF gene in combination with adjuvant chemoradiotherapy for the treatment of adenocarcinoma of the pancreas. Journal of Clinical Oncology, Vol 25, No 18S (June 20 Supplement), 2007: 3010. | |||||
| REF 9 | ClinicalTrials.gov (NCT02243371) GVAX Pancreas Vaccine (With CY) and CRS-207 With or Without Nivolumab. U.S. National Institutes of Health. | |||||
| REF 10 | URL: 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: 7785). | |||||
| REF 11 | Clinical pipeline report, company report or official report of MedImmune (2011). | |||||
| REF 12 | ClinicalTrials.gov (NCT01023256) Safety and Preliminary Efficacy of MOR103 in Patients With Active Rheumatoid Arthritis. U.S. National Institutes of Health. | |||||
| REF 13 | A Phase I study of KH901, a conditionally replicating granulocyte-macrophage colony-stimulating factor: armed oncolytic adenovirus for the treatmen... Cancer Biol Ther. 2009 Apr;8(8):676-82. | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004355) | |||||
| REF 15 | Economic evaluation of filgrastim, sargramostim, and sequential sargramostim and filgrastim after myelosuppressive chemotherapy. Bone Marrow Transplant. 2002 Jan;29(2):159-64. | |||||
| REF 16 | Idiotypevaccinetherapy (BiovaxID) infollicularlymphomain first complete remission: Phase III clinical trial results, Journal of Clinical Oncology, Vol 27, No 18S (June 20 Supplement), 2009: 2. | |||||
| REF 17 | Clinical pipeline report, company report or official report of gensci-china. | |||||
| REF 18 | Phase I/II trial of PIXY321 (granulocyte-macrophage colony stimulating factor/interleukin-3 fusion protein) for treatment of inherited and acquired... Br J Haematol. 1998 Nov;103(2):304-7. | |||||
| REF 19 | URL: 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: 1707). | |||||
| REF 20 | MOR103, a human monoclonal antibody to granulocyte-macrophage colony-stimulating factor, in the treatment of patients with moderate rheumatoid arthritis: results of a phase Ib/IIa randomised, double-blind, placebo-controlled, dose-escalation trial. Ann Rheum Dis. 2015 Jun;74(6):1058-64. | |||||
| REF 21 | Effects of KH901, a tumor-specific oncolytic recombinant adenovirus, on antitumor and expressing GM-CSF in xenograft tumor models. Sichuan Da Xue Xue Bao Yi Xue Ban. 2007 Jun;38(3):386-90. | |||||
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