Target Information
| Target General Information | Top | |||||
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| Target ID |
T49493
(Former ID: TTDS00498)
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| Target Name |
Hemoglobin (HB)
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| Synonyms |
Hemoglobin subunit alpha; Hemoglobin alpha chain; HBA1; Alpha-globin
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| Gene Name |
HBA2
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Iron deficiency anaemia [ICD-11: 3A00] | |||||
| 2 | Sickle-cell disorder [ICD-11: 3A51] | |||||
| Function |
Involved in oxygen transport from the lung to the various peripheral tissues.
Click to Show/Hide
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| BioChemical Class |
Pore-forming globin
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| UniProt ID | ||||||
| Sequence |
MVLSPADKTNVKAAWGKVGAHAGEYGAEALERMFLSFPTTKTYFPHFDLSHGSAQVKGHG
KKVADALTNAVAHVDDMPNALSALSDLHAHKLRVDPVNFKLLSHCLLVTLAAHLPAEFTP AVHASLDKFLASVSTVLTSKYR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A06271 | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
| 1 | Iron | Drug Info | Approved | Iron-deficiency anemia | [2] | |
| 2 | Iron Dextran | Drug Info | Approved | Iron-deficiency anemia | [3], [4] | |
| 3 | Voxelotor | Drug Info | Approved | Sickle-cell disorder | [5] | |
| Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
| 1 | Efaproxyn | Drug Info | Phase 3 | Lung cancer | [6] | |
| 2 | PolyHeme | Drug Info | Phase 3 | Blood forming organ disorder | [7] | |
| 3 | Hemoglobin raffimer | Drug Info | Phase 2/3 | Anemia | [8] | |
| 4 | 5-hydroxymethyl-2-furfural | Drug Info | Phase 2 | Anemia | [9] | |
| 5 | FBS-0701 | Drug Info | Phase 2 | Iron overload disease | [10] | |
| 6 | HQK-1001 | Drug Info | Phase 2 | Beta thalassemia | [11] | |
| 7 | CTX110 | Drug Info | Phase 1/2 | Non-hodgkin lymphoma | [12] | |
| 8 | OXY-111A | Drug Info | Phase 1/2 | Cardiovascular disease | [13] | |
| Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
| 1 | Hemoximer | Drug Info | Discontinued in Phase 3 | Hypotension | [14] | |
| 2 | VX-366 | Drug Info | Discontinued in Phase 2 | Constitutional neutropenia | [15] | |
| 3 | HRC-302 | Drug Info | Discontinued in Phase 1 | Chronic myelogenous leukaemia | [16] | |
| 4 | AN-10 | Drug Info | Terminated | Alopecia | [17] | |
| 5 | Diaspirin crosslinked hemoglobin | Drug Info | Terminated | Cerebrovascular ischaemia | [18] | |
| 6 | HRC-101 | Drug Info | Terminated | Blood transfusion | [19] | |
| 7 | HRC-102 | Drug Info | Terminated | Reperfusion injury | [20] | |
| 8 | HRC-201 | Drug Info | Terminated | Liver cancer | [21] | |
| 9 | RHb1.1 | Drug Info | Terminated | Anemia | [22] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Activator | [+] 2 Activator drugs | + | ||||
| 1 | Iron | Drug Info | [1] | |||
| 2 | Iron Dextran | Drug Info | [1] | |||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | Voxelotor | Drug Info | [5] | |||
| 2 | PolyHeme | Drug Info | [24] | |||
| 3 | Hemoglobin raffimer | Drug Info | [25] | |||
| 4 | 5-hydroxymethyl-2-furfural | Drug Info | [26] | |||
| 5 | FBS-0701 | Drug Info | [27] | |||
| 6 | HRC-302 | Drug Info | [33] | |||
| 7 | AN-10 | Drug Info | [34] | |||
| 8 | Diaspirin crosslinked hemoglobin | Drug Info | [35] | |||
| 9 | HRC-101 | Drug Info | [36] | |||
| 10 | HRC-102 | Drug Info | [37] | |||
| 11 | RHb1.1 | Drug Info | [38] | |||
| Inhibitor | [+] 9 Inhibitor drugs | + | ||||
| 1 | Efaproxyn | Drug Info | [23] | |||
| 2 | VX-366 | Drug Info | [32] | |||
| 3 | 1,3,5-BENZENETRICARBOXYLIC ACID | Drug Info | [39] | |||
| 4 | 2,6-DICARBOXYNAPHTHALENE | Drug Info | [39] | |||
| 5 | 2-[(2-methoxy-5-methylphenoxy)methyl]pyridine | Drug Info | [39] | |||
| 6 | 4-Carboxycinnamic Acid | Drug Info | [39] | |||
| 7 | 4-[(5-methoxy-2-methylphenoxy)methyl]pyridine | Drug Info | [39] | |||
| 8 | Heme | Drug Info | [39] | |||
| 9 | SEBACIC ACID | Drug Info | [39] | |||
| Inducer | [+] 1 Inducer drugs | + | ||||
| 1 | HQK-1001 | Drug Info | [28] | |||
| Enhancer | [+] 2 Enhancer drugs | + | ||||
| 1 | OXY-111A | Drug Info | [30] | |||
| 2 | HRC-201 | Drug Info | [37] | |||
| Antagonist | [+] 1 Antagonist drugs | + | ||||
| 1 | Hemoximer | Drug Info | [31] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | African trypanosomiasis | |||||
| 2 | Malaria | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Erythrocytes take up carbon dioxide and release oxygen | |||||
| 2 | Erythrocytes take up oxygen and release carbon dioxide | |||||
| 3 | Scavenging of heme from plasma | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | Binding and Uptake of Ligands by Scavenger Receptors | |||||
| 2 | Uptake of Carbon Dioxide and Release of Oxygen by Erythrocytes | |||||
| 3 | Uptake of Oxygen and Release of Carbon Dioxide by Erythrocytes | |||||
| 4 | Factors involved in megakaryocyte development and platelet production | |||||
| 5 | Folate Metabolism | |||||
| 6 | Vitamin B12 Metabolism | |||||
| 7 | Selenium Micronutrient Network | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Efficacy and safety of total dose infusion of low molecular weight iron dextran in the treatment of iron deficiency anemia during pregnancy. J Coll Physicians Surg Pak. 2008 Jul;18(7):424-7. | |||||
| REF 2 | Drug information of Iron, 2008. eduDrugs. | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010787. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
| REF 6 | ClinicalTrials.gov (NCT00083304) Whole Brain Radiation Therapy With Oxygen, With or Without RSR13, in Women With Brain Metastases From Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT00076648) Safety and Efficacy of PolyHeme(R) in Hemorrhagic Shock Following Traumatic Injuries Beginning in the Pre-Hospital Setting. U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT00038454) Phase II Study To Evaluate The Safety and Efficacy of Hemoglobin Raffimer in Patients Undergoing First Time CABG Surgery. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT01987908) Evaluation of Different Dose Regimens of Aes-103 Given for 28 Days to Subjects With Stable Sickle Cell Disease. U.S. National Institutes of Health. | |||||
| REF 10 | ClinicalTrials.gov (NCT01186419) Safety and Pharmacodynamic Study of an Oral Iron Chelator Given for 6 Months to Patients With Iron Overload. U.S. National Institutes of Health. | |||||
| REF 11 | A phase 2 trial of HQK-1001 in HbE-beta thalassemia demonstrates HbF induction and reduced anemia. Blood. 2014 Mar 20;123(12):1956-7. | |||||
| REF 12 | ClinicalTrials.gov (NCT04035434) A Safety and Efficacy Study Evaluating CTX110 in Subjects With Relapsed or Refractory B-Cell Malignancies (CARBON). U.S. National Institutes of Health. | |||||
| REF 13 | ClinicalTrials.gov (NCT02528526) Effects of OXY111A in Primary and Secondary Hepato-Pancreato-Biliary Neoplasm. | |||||
| 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 800008774) | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006007) | |||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014790) | |||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008114) | |||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005412) | |||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016356) | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016740) | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020214) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008362) | |||||
| REF 23 | Increased oxygenation of intracranial tumors by efaproxyn (efaproxiral), an allosteric hemoglobin modifier: In vivo EPR oximetry study. Int J Radiat Oncol Biol Phys. 2005 Apr 1;61(5):1503-9. | |||||
| REF 24 | Blood substitutes- the polyheme trials. Mcgill J Med. 2008 January; 11(1): 59-65. | |||||
| REF 25 | Use of hemoglobin raffimer for postoperative life-threatening anemia in a Jehovah's Witness. Can J Anaesth. 2005 Apr;52(4):369-73. | |||||
| REF 26 | 5-hydroxymethyl-2-furfural modifies intracellular sickle haemoglobin and inhibits sickling of red blood cells. Br J Haematol. 2005 Feb;128(4):552-61. | |||||
| REF 27 | A high-affinity fully human anti-IL-6 mAb, 1339, for the treatment of multiple myeloma. Clin Cancer Res. 2009 Dec 1;15(23):7144-52. | |||||
| REF 28 | A phase 2 study of HQK-1001, an oral fetal haemoglobin inducer, in beta-thalassaemia intermedia. Br J Haematol. 2014 Feb;164(3):456-8. | |||||
| REF 29 | Clinical pipeline report, company report or official report of CRISPR Therapeutics. | |||||
| REF 30 | Modulating the oxygen affinity of human fetal haemoglobin with synthetic allosteric modulators. Br J Haematol. 1998 Sep;102(5):1165-71. | |||||
| REF 31 | Effect of NaBH4 Concentration and Reaction Time on Physical Properties of Glutaraldehyde-Polymerized Hemoglobin. Biotechnology Progress. 05/2004; 20(3):946-52. | |||||
| REF 32 | A combination of hydroxyurea and isobutyramide to induce fetal hemoglobin in transgenic mice is more hematotoxic than the individual agents. Blood Cells Mol Dis. 1999 Jun-Aug;25(3-4):255-69. | |||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014790) | |||||
| REF 34 | Genes for Development, Cell Growth and Infectious Diseases, Gabriel Gachelin, 1995. Page(215). | |||||
| REF 35 | Diaspirin cross-linked hemoglobin infusion did not influence base deficit and lactic acid levels in two clinical trials of traumatic hemorrhagic shock patient resuscitation. J Trauma. 2010 May;68(5):1158-71. | |||||
| REF 36 | The novel hemoglobin-based oxygen carrier HRC 101 improves survival in murine sickle cell disease. Anesthesiology. 2007 Aug;107(2):281-7. | |||||
| REF 37 | WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting. | |||||
| REF 38 | Effects of recombinant-hemoglobin solutions rHb2.0 and rHb1.1 on blood pressure, intestinal blood flow, and gut oxygenation in a rat model of hemorrhagic shock. J Lab Clin Med. 2005 Jan;145(1):21-32. | |||||
| REF 39 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
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