General Information of the Protein
Protein ID
PT04856
Protein Name
B-cell lymphoma 6 protein
Secondarily
Protein Name
B-cell lymphoma 5 protein
Protein LAZ-3
Zinc finger and BTB domain-containing protein 27
Zinc finger protein 51
Gene Name
BCL6
Secondarily
Gene Name
BCL5
LAZ3
ZBTB27
ZNF51
Sequence
MASPADSCIQFTRHASDVLLNLNRLRSRDILTDVVIVVSREQFRAHKTVLMACSGLFYSIFTDQLKCNLSVINLDPEINPEGFCILLDFMYTSRLNLREGNIMAVMATAMYLQMEHVVDTCRKFIKASEAEMVSAIKPPREEFLNSRMLMPQDIMAYRGREVVENNLPLRSAPGCESRAFAPSLYSGLSTPPASYSMYSHLPVSSLLFSDEEFRDVRMPVANPFPKERALPCDSARPVPGEYSRPTLEVSPNVCHSNIYSPKETIPEEARSDMHYSVAEGLKPAAPSARNAPYFPCDKASKEEERPSSEDEIALHFEPPNAPLNRKGLVSPQSPQKSDCQPNSPTESCSSKNACILQASGSPPAKSPTDPKACNWKKYKFIVLNSLNQNAKPEGPEQAELGRLSPRAYTAPPACQPPMEPENLDLQSPTKLSASGEDSTIPQASRLNNIVNRSMTGSPRSSSESHSPLYMHPPKCTSCGSQSPQHAEMCLHTAGPTFPEEMGETQSEYSDSSCENGAFFCNECDCRFSEEASLKRHTLQTHSDKPYKCDRCQASFRYKGNLASHKTVHTGEKPYRCNICGAQFNRPANLKTHTRIHSGEKPYKCETCGARFVQVAHLRAHVLIHTGEKPYPCEICGTRFRHLQTLKSHLRIHTGEKPYHCEKCNLHFRHKSQLRLHLRQKHGAITNTKVQYRVSATDLPPELPKAC
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Transcriptional repressor mainly required for germinal center (GC) formation and antibody affinity maturation which has different mechanisms of action specific to the lineage and biological functions. Forms complexes with different corepressors and histone deacetylases to repress the transcriptional expression of different subsets of target genes. Represses its target genes by binding directly to the DNA sequence 5'-TTCCTAGAA-3' (BCL6-binding site) or indirectly by repressing the transcriptional activity of transcription factors. In GC B-cells, represses genes that function in differentiation, inflammation, apoptosis and cell cycle control, also autoregulates its transcriptional expression and up-regulates, indirectly, the expression of some genes important for GC reactions, such as AICDA, through the repression of microRNAs expression, like miR155. An important function is to allow GC B-cells to proliferate very rapidly in response to T-cell dependent antigens and tolerate the physiological DNA breaks required for immunglobulin class switch recombination and somatic hypermutation without inducing a p53/TP53-dependent apoptotic response. In follicular helper CD4(+) T-cells (T(FH) cells), promotes the expression of T(FH)-related genes but inhibits the differentiation of T(H)1, T(H)2 and T(H)17 cells. Also required for the establishment and maintenance of immunological memory for both T- and B-cells. Suppresses macrophage proliferation through competition with STAT5 for STAT-binding motifs binding on certain target genes, such as CCL2 and CCND2. In response to genotoxic stress, controls cell cycle arrest in GC B-cells in both p53/TP53-dependedent and -independent manners. Besides, also controls neurogenesis through the alteration of the composition of NOTCH-dependent transcriptional complexes at selective NOTCH targets, such as HES5, including the recruitment of the deacetylase SIRT1 and resulting in an epigenetic silencing leading to neuronal differentiation.
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Uniprot ID
Primary ID:
P41182

Secondarily ID:
A7E241
B8PSA7
D3DNV5
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Ensembl ID
ENSG00000113916
HGNC ID
HGNC:1001
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000314 , HEK293T/17
Compound ID Compound Name Compound Formula
CP0412952
(12S,14S,17E)-7-chloro-12-(hydroxymethyl)-23-[(3-methoxyphenyl)methyl]-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one
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C32H33ClN6O5
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0543050
(12S,14S,17E)-12-(hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile
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C25H25N7O4
 1
1
IC50 = 1995.26 nM
   TI
   LI
   LO
   TS
CP0544260
(12S,14S)-7-chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaen-24-one
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C24H27ClN6O4
 1
1
IC50 = 3981.07 nM
   TI
   LI
   LO
   TS
CP0519940
(12S,14S)-12-(hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaene-7-carbonitrile
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C25H27N7O4
 1
1
IC50 = 6309.57 nM
   TI
   LI
   LO
   TS
CP0469977
(12S,14S)-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaen-24-one
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C24H28N6O4
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0472404
(14S)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaene-7-carbonitrile
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C24H25N7O3
 1
1
IC50 = 15848.93 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0543050
(12S,14S,17E)-12-(hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile
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C25H25N7O4
 1
1 IC50 = 2.9 nM
CP0364740
5-[[5-chloro-2-(pyridin-3-ylmethylamino)pyrimidin-4-yl]amino]-1,3-dihydroindol-2-one
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C18H15ClN6O
 3
1 IC50 = 480 nM
2 IC50 = 8600 nM
3 Kd = 78 nM
CP0260408
5-[[5-chloro-2-[(3R,5S)-4,4-difluoro-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-3-(3-hydroxy-3-methylbutyl)-1-methylbenzimidazol-2-one
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C24H31ClF2N6O2
 1
1 IC50 = 520 nM
CP0564296
US11161839, Example 10a
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C26H24ClN7O
 1
1 Kd = 234.42 nM
Clinical Information about the Protein
Target 1 ( B-cell lymphoma 6 protein (BCL-6) )
Target Type Literature-reported Target