CD20 (membrane-spanning 4-domains, subfamily A, member 1) | CD molecules | IUPHAR/BPS Guide to PHARMACOLOGY

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CD20 (membrane-spanning 4-domains, subfamily A, member 1)

target has curated data in GtoImmuPdb

Target id: 2628

Nomenclature: CD20 (membrane-spanning 4-domains, subfamily A, member 1)

Family: CD molecules

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 297 11q12-q13.1 MS4A1 membrane spanning 4-domains A1
Mouse 4 291 19 B Ms4a1 membrane-spanning 4-domains, subfamily A, member 1
Rat - 297 1q43 Ms4a1 membrane spanning 4-domains A1
Previous and Unofficial Names
B-lymphocyte antigen CD20 | MS4A2 | membrane-spanning 4-domains, subfamily A, member 1 | membrane-spanning 4-domains
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein

Download all structure-activity data for this target as a CSV file

Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
ofatumumab Hs Binding 9.9 pKd 9
pKd 9.9 (Kd 1.21x10-10 M) [9]
Description: Binding affinity for clone 2F2 ((HuMax-CD20).
ocrelizumab Hs Binding 9.1 pKd 1
pKd 9.1 (Kd 8.4x10-10 M) [1]
rituximab Hs Binding 8.5 pKd 12
pKd 8.5 (Kd 3.1x10-9 M) [12]
veltuzumab Hs Binding 8.4 pKd 12
pKd 8.4 (Kd 3.6x10-9 M) [12]
BsAb (CD89-CD20) Hs Binding 8.0 pKd 8
pKd 8.0 (Kd 9.37x10-9 M) [8]
Description: FACS analysis of antibody binding to CD20-expressing Raji cells.
ibritumomab tiuxetan Hs Binding - -
tositumomab Hs Binding - -
obinutuzumab Hs Binding - - 2,11
ublituximab Hs Binding - - 6
Antibody Comments
Ofatumumab, rituximab, tositumomab and ibritumomab tiuxetan are monoclonal antibodies against the CD20 molecule (MS4A1). These references contain some details of their use and function:- [3,7,10,14,16].
Although the KD value for ofatumumab is derived from [9], the originating patent is US8529902 [13].
A trifunctional monoclonal (Triomab®) called FBTA05, that targets CD20/CD3e was progressed to Phase 1/2 evaluation (NCT01138579), but recruitment was delayed and the trial terminated when FBTA05 became unavailable. See the entry for catumaxomab for full details of Triomab® mechanism of action.
Immunopharmacology Comments
CD20 is a B cell antigen, involved in B cell development and maturation to antibody-producing plasma cells [4]. CD20 has no known ligand and is suggested to act as a calcium channel. CD20 is the target of monoclonal antibodies approved for the treatment of B cell lymphomas and leukemias (rituximab, obinutuzumab, Ibritumomab tiuxetan, ofatumumab and tositumomab). In obses mice, anti-CD20 antibodies prevent insulin insensitivity and development of diabetes mellitus or metabolic syndrome [15], suggesting a potentially druggable autoimmune link between obesity, diabetes mellitus and metabolic syndrome.
Cell Type Associations
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050853 B cell receptor signaling pathway IDA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 3 GO processes
GO:0030183 B cell differentiation IDA
GO:0042100 B cell proliferation NAS
GO:0042113 B cell activation IDA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0030183 B cell differentiation IDA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 4 GO processes
GO:0030183 B cell differentiation IDA
GO:0042100 B cell proliferation NAS
GO:0042113 B cell activation IDA
GO:0050853 B cell receptor signaling pathway IDA
Immuno Disease Associations
Disease Name:  Pemphigus
Disease Synonyms:  no synonynms
Comment:  CD20 is the molecular target of the antibody veltuzumab.
Disease X-refs:  Disease Ontology: DOID:9182
Disease Name:  Relapsing-remitting multiple sclerosis
Disease Synonyms:  no synonynms
Comment:  CD20 is the molecular target of the RRMS therapeutic ocrelizumab.
Disease X-refs:  Disease Ontology: DOID:2378
Disease Name:  non-Hodgkin lymphoma
Disease Synonyms:  no synonynms
Comment:  CD20 is the molecular target of the B cell NHL therapeutic ibritumomab tiuxetan.
Disease X-refs:  Disease Ontology: DOID:0060060
OMIM: 605027
Disease Name:  Chronic lymphocytic leukemia
Disease Synonyms:  no synonynms
Comment:  CD20 is the molecular target of the CLL therapeutics ofatumumab and obinutuzumab.
Disease X-refs:  Disease Ontology: DOID:1040
OMIM: 151400
Orphanet: ORPHA67038
Clinically-Relevant Mutations and Pathophysiology
Disease:  Common variable immunodeficiency
Description: CVID is a group of genetically heterogeneous primary immunodeficiencies. Whilst a small number of cases can be linked to deficiency in a single gene (see the OMIM links as examples), the cause is likely to be polygenic in the majority of cases. Symptoms vary between patients, but CVID is generally characterised by a failure to produce antibodies (hypogammaglobulinemia) and therefore susceptibility to recurrent infections and inflammation (including autoimmunity).
Disease Ontology: DOID:12177
OMIM: 613495, 607594, 606453, 240500, 613493
Orphanet: ORPHA1572
References:  5


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1. Adams CW, Chan AC, Crowley CW, Lowman HB, Nakamura GR, Presta LG. (2004) Immunoglobulin variants and uses thereof. Patent number: WO2004056312. Assignee: Genentech, Inc.. Priority date: 16/12/2002. Publication date: 08/07/2004.

2. Alduaij W, Ivanov A, Honeychurch J, Cheadle EJ, Potluri S, Lim SH, Shimada K, Chan CH, Tutt A, Beers SA et al.. (2011) Novel type II anti-CD20 monoclonal antibody (GA101) evokes homotypic adhesion and actin-dependent, lysosome-mediated cell death in B-cell malignancies. Blood, 117 (17): 4519-29. [PMID:21378274]

3. Anderson DR, Grillo-López A, Varns C, Chambers KS, Hanna N. (1997) Targeted anti-cancer therapy using rituximab, a chimaeric anti-CD20 antibody (IDEC-C2B8) in the treatment of non-Hodgkin's B-cell lymphoma. Biochem. Soc. Trans., 25 (2): 705-8. [PMID:9191187]

4. Cragg MS, Walshe CA, Ivanov AO, Glennie MJ. (2005) The biology of CD20 and its potential as a target for mAb therapy. Curr. Dir. Autoimmun., 8: 140-74. [PMID:15564720]

5. Kuijpers TW, Bende RJ, Baars PA, Grummels A, Derks IA, Dolman KM, Beaumont T, Tedder TF, van Noesel CJ, Eldering E et al.. (2010) CD20 deficiency in humans results in impaired T cell-independent antibody responses. J. Clin. Invest., 120 (1): 214-22. [PMID:20038800]

6. Le Garff-Tavernier M, Decocq J, de Romeuf C, Parizot C, Dutertre CA, Chapiro E, Davi F, Debré P, Prost JF, Teillaud JL et al.. (2011) Analysis of CD16+CD56dim NK cells from CLL patients: evidence supporting a therapeutic strategy with optimized anti-CD20 monoclonal antibodies. Leukemia, 25 (1): 101-9. [PMID:20975664]

7. Leandro MJ. (2013) B-cell subpopulations in humans and their differential susceptibility to depletion with anti-CD20 monoclonal antibodies. Arthritis Res. Ther., 15 Suppl 1: S3. [PMID:23566754]

8. Li B, Xu L, Pi C, Yin Y, Xie K, Tao F, Li R, Gu H, Fang J. (2017) CD89-mediated recruitment of macrophages via a bispecific antibody enhances anti-tumor efficacy. Oncoimmunology, 7 (1): e1380142. [PMID:29296544]

9. Liu Q. (2013) Fully human antibodies against human cd20. Patent number: WO2013007052. Assignee: Qingfa Liu. Priority date: 13/07/2011. Publication date: 17/01/2013.

10. Mayes S, Brown N, Illidge TM. (2011) New antibody drug treatments for lymphoma. Expert Opin Biol Ther, 11 (5): 623-40. [PMID:21395497]

11. Reslan L, Dalle S, Herveau S, Perrial E, Dumontet C. (2014) Apoptotic induction by anti-CD20 antibodies in chronic lymphocytic leukemia: comparison of rituximab and obinutuzumab. Leuk. Lymphoma, 55 (1): 188-90. [PMID:23537278]

12. Stein R, Qu Z, Chen S, Rosario A, Shi V, Hayes M, Horak ID, Hansen HJ, Goldenberg DM. (2004) Characterization of a new humanized anti-CD20 monoclonal antibody, IMMU-106, and Its use in combination with the humanized anti-CD22 antibody, epratuzumab, for the therapy of non-Hodgkin's lymphoma. Clin. Cancer Res., 10 (8): 2868-78. [PMID:15102696]

13. Teeling J, Ruuls S, Glennie M, van de Winkel JGJ, Parren P, Petersen J, Baadsgaard O, Huang H. (2013) for promoting proliferation and/or differentiation of B cells involved in cancers and autoimmune disorders; animal models; genetic engineering. Patent number: US8529902. Assignee: Genmab A/S. Priority date: 17/10/2002. Publication date: 10/09/2013.

14. White CA, Berlfein JR, Grillo-López AJ. (2000) Antibody-targeted immunotherapy for treatment of non-Hodgkin's lymphoma. Curr Pharm Biotechnol, 1 (4): 303-12. [PMID:11467328]

15. Winer DA, Winer S, Shen L, Wadia PP, Yantha J, Paltser G, Tsui H, Wu P, Davidson MG, Alonso MN et al.. (2011) B cells promote insulin resistance through modulation of T cells and production of pathogenic IgG antibodies. Nat. Med., 17 (5): 610-7. [PMID:21499269]

16. Witzig TE, White CA, Wiseman GA, Gordon LI, Emmanouilides C, Raubitschek A, Janakiraman N, Gutheil J, Schilder RJ, Spies S et al.. (1999) Phase I/II trial of IDEC-Y2B8 radioimmunotherapy for treatment of relapsed or refractory CD20(+) B-cell non-Hodgkin's lymphoma. J. Clin. Oncol., 17 (12): 3793-803. [PMID:10577851]

How to cite this page

CD molecules: CD20 (membrane-spanning 4-domains, subfamily A, member 1). Last modified on 23/10/2019. Accessed on 19/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,