Target Information

Target General Information

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Target ID

T03634 (Former ID: TTDNC00387)

Target Name

CREB-binding protein (CREBBP)

Synonyms

CREBbinding protein; CBP

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Gene Name

CREBBP

Target Type

Clinical trial target

[1]

Disease

[+] 4 Target-related Diseases

Acute myeloid leukaemia [ICD-11: 2A60]

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Systemic sclerosis [ICD-11: 4A42]

Prostate cancer [ICD-11: 2C82]

Function

Acetylates non-histone proteins, like NCOA3 and FOXO1. Binds specifically to phosphorylated CREB and enhances its transcriptional activity toward cAMP-responsive genes. Acts as a coactivator of ALX1. Acts as a circadian transcriptional coactivator which enhances the activity of the circadian transcriptional activators: NPAS2-ARNTL/BMAL1 and CLOCK-ARNTL/BMAL1 heterodimers. Acetylates PCNA; acetylation promotes removal of chromatin-bound PCNA and its degradation during nucleotide excision repair (NER). Functions as a transcriptional coactivator for SMAD4 in the TGF-beta signaling pathway. Acetylates histones, giving a specific tag for transcriptional activation.

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BioChemical Class

Acyltransferase

UniProt ID

CBP_HUMAN

EC Number

EC 2.3.1.48

Sequence

MAENLLDGPPNPKRAKLSSPGFSANDSTDFGSLFDLENDLPDELIPNGGELGLLNSGNLV
PDAASKHKQLSELLRGGSGSSINPGIGNVSASSPVQQGLGGQAQGQPNSANMASLSAMGK
SPLSQGDSSAPSLPKQAASTSGPTPAASQALNPQAQKQVGLATSSPATSQTGPGICMNAN
FNQTHPGLLNSNSGHSLINQASQGQAQVMNGSLGAAGRGRGAGMPYPTPAMQGASSSVLA
ETLTQVSPQMTGHAGLNTAQAGGMAKMGITGNTSPFGQPFSQAGGQPMGATGVNPQLASK
QSMVNSLPTFPTDIKNTSVTNVPNMSQMQTSVGIVPTQAIATGPTADPEKRKLIQQQLVL
LLHAHKCQRREQANGEVRACSLPHCRTMKNVLNHMTHCQAGKACQVAHCASSRQIISHWK
NCTRHDCPVCLPLKNASDKRNQQTILGSPASGIQNTIGSVGTGQQNATSLSNPNPIDPSS
MQRAYAALGLPYMNQPQTQLQPQVPGQQPAQPQTHQQMRTLNPLGNNPMNIPAGGITTDQ
QPPNLISESALPTSLGATNPLMNDGSNSGNIGTLSTIPTAAPPSSTGVRKGWHEHVTQDL
RSHLVHKLVQAIFPTPDPAALKDRRMENLVAYAKKVEGDMYESANSRDEYYHLLAEKIYK
IQKELEEKRRSRLHKQGILGNQPALPAPGAQPPVIPQAQPVRPPNGPLSLPVNRMQVSQG
MNSFNPMSLGNVQLPQAPMGPRAASPMNHSVQMNSMGSVPGMAISPSRMPQPPNMMGAHT
NNMMAQAPAQSQFLPQNQFPSSSGAMSVGMGQPPAQTGVSQGQVPGAALPNPLNMLGPQA
SQLPCPPVTQSPLHPTPPPASTAAGMPSLQHTTPPGMTPPQPAAPTQPSTPVSSSGQTPT
PTPGSVPSATQTQSTPTVQAAAQAQVTPQPQTPVQPPSVATPQSSQQQPTPVHAQPPGTP
LSQAAASIDNRVPTPSSVASAETNSQQPGPDVPVLEMKTETQAEDTEPDPGESKGEPRSE
MMEEDLQGASQVKEETDIAEQKSEPMEVDEKKPEVKVEVKEEEESSSNGTASQSTSPSQP
RKKIFKPEELRQALMPTLEALYRQDPESLPFRQPVDPQLLGIPDYFDIVKNPMDLSTIKR
KLDTGQYQEPWQYVDDVWLMFNNAWLYNRKTSRVYKFCSKLAEVFEQEIDPVMQSLGYCC
GRKYEFSPQTLCCYGKQLCTIPRDAAYYSYQNRYHFCEKCFTEIQGENVTLGDDPSQPQT
TISKDQFEKKKNDTLDPEPFVDCKECGRKMHQICVLHYDIIWPSGFVCDNCLKKTGRPRK
ENKFSAKRLQTTRLGNHLEDRVNKFLRRQNHPEAGEVFVRVVASSDKTVEVKPGMKSRFV
DSGEMSESFPYRTKALFAFEEIDGVDVCFFGMHVQEYGSDCPPPNTRRVYISYLDSIHFF
RPRCLRTAVYHEILIGYLEYVKKLGYVTGHIWACPPSEGDDYIFHCHPPDQKIPKPKRLQ
EWYKKMLDKAFAERIIHDYKDIFKQATEDRLTSAKELPYFEGDFWPNVLEESIKELEQEE
EERKKEESTAASETTEGSQGDSKNAKKKNNKKTNKNKSSISRANKKKPSMPNVSNDLSQK
LYATMEKHKEVFFVIHLHAGPVINTLPPIVDPDPLLSCDLMDGRDAFLTLARDKHWEFSS
LRRSKWSTLCMLVELHTQGQDRFVYTCNECKHHVETRWHCTVCEDYDLCINCYNTKSHAH
KMVKWGLGLDDEGSSQGEPQSKSPQESRRLSIQRCIQSLVHACQCRNANCSLPSCQKMKR
VVQHTKGCKRKTNGGCPVCKQLIALCCYHAKHCQENKCPVPFCLNIKHKLRQQQIQHRLQ
QAQLMRRRMATMNTRNVPQQSLPSPTSAPPGTPTQQPSTPQTPQPPAQPQPSPVSMSPAG
FPSVARTQPPTTVSTGKPTSQVPAPPPPAQPPPAAVEAARQIEREAQQQQHLYRVNINNS
MPPGRTGMGTPGSQMAPVSLNVPRPNQVSGPVMPSMPPGQWQQAPLPQQQPMPGLPRPVI
SMQAQAAVAGPRMPSVQPPRSISPSALQDLLRTLKSPSSPQQQQQVLNILKSNPQLMAAF
IKQRTAKYVANQPGMQPQPGLQSQPGMQPQPGMHQQPSLQNLNAMQAGVPRPGVPPQQQA
MGGLNPQGQALNIMNPGHNPNMASMNPQYREMLRRQLLQQQQQQQQQQQQQQQQQQGSAG
MAGGMAGHGQFQQPQGPGGYPPAMQQQQRMQQHLPLQGSSMGQMAAQMGQLGQMGQPGLG
ADSTPNIQQALQQRILQQQQMKQQIGSPGQPNPMSPQQHMLSGQPQASHLPGQQIATSLS
NQVRSPAPVQSPRPQSQPPHSSPSPRIQPQPSPHHVSPQTGSPHPGLAVTMASSIDQGHL
GNPEQSAMLPQLNTPSRSALSSELSLVGDTTGDTLEKFVEGL

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3D Structure

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AlphaFold

HIT2.0 ID

T15M1G

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 4 Clinical Trial Drugs

C 82

Drug Info

Phase 1/2

Scleroderma

[2]

CCS1477

Drug Info

Phase 1/2

Solid tumour/cancer

[3]

PRI-724

Drug Info

Phase 1/2

Acute myeloid leukaemia

[4]

FT-7051

Drug Info

Phase 1

Prostate cancer

[5]

Mode of Action

[+] 2 Modes of Action

Inhibitor

[+] 7 Inhibitor drugs

C 82

Drug Info

[2]

CCS1477

Drug Info

[6]

FT-7051

Drug Info

[7]

Pyrrolo-pyrrolone derivative 6

Drug Info

[8]

I-CBP112

Drug Info

[9]

ischemin

Drug Info

[10]

SGC-CBP30

Drug Info

[11]

Modulator

[+] 1 Modulator drugs

PRI-724

Drug Info

[1]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

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Ligand Name: Acetaminophen

Ligand Info

Structure Description

BROMODOMAIN OF HUMAN CREBBP WITH N-(4-hydroxyphenyl)acetamide

PDB:4A9K

Method

X-ray diffraction

Resolution

1.81 Å

Mutation

[12]

PDB Sequence

KIFKPEELRQ

¹⁰⁹²

ALMPTLEALY

¹¹⁰²

RQDPESLPFR

¹¹¹²

QPVDPQLLGI

¹¹²²

PDYFDIVKNP

¹¹³²

MDLSTIKRKL

¹¹⁴²

DTGQYQEPWQ

¹¹⁵²

YVDDVWLMFN

¹¹⁶²

NAWLYNRKTS

¹¹⁷²

RVYKFCSKLA

¹¹⁸²

EVFEQEIDPV

¹¹⁹²

MQSLG

Residue

Distance (Å)

PRO1110

3.868

PHE1111

3.698

VAL1115

3.456

LEU1120

3.720

ILE1122

3.676

Residue

Distance (Å)

TYR1125

4.187

ALA1164

4.346

TYR1167

3.640

ASN1168

3.136

VAL1174

3.557

Ligand Name: CCS1477

Ligand Info

Structure Description

Crystal structure of CBP bromodomain liganded with CCS1477

PDB:7XH6

Method

X-ray diffraction

Resolution

1.75 Å

Mutation

[13]

PDB Sequence

FKPEELRQAL

¹⁰⁹⁴

MPTLEALYRQ

¹¹⁰⁴

DPESLPFRQP

¹¹¹⁴

VDPQLLGIPD

¹¹²⁴

YFDIVKNPMD

¹¹³⁴

LSTIKRKLDT

¹¹⁴⁴

GQYQEPWQYV

¹¹⁵⁴

DDVWLMFNNA

¹¹⁶⁴

WLYNRKTSRV

¹¹⁷⁴

YKFCSKLAEV

¹¹⁸⁴

FEQEIDPVMQ

¹¹⁹⁴

Residue

Distance (Å)

PRO1106

3.510

LEU1109

4.019

PRO1110

3.439

PHE1111

3.819

VAL1115

3.768

LEU1120

3.921

ILE1122

3.492

Residue

Distance (Å)

TYR1125

3.575

ALA1164

4.176

TYR1167

3.689

ASN1168

3.043

ARG1173

2.852

VAL1174

3.398

PHE1177

3.347

Click to View More Binding Site Information of This Target with Different Ligands

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues. The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Tissue Distribution Human Pathway Affiliation Biological Network Descriptors

Different Human System Profiles of Target

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Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.

The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Tissue Distribution

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Microtubule-actin cross-linking factor 1, isoforms 6/7 (MACF1)	PF13499 ; PF02187 ; PF00435 More >>	31.633 (62/196)	3.00E-03


Note: If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.

KEGG Pathway	Pathway ID	Affiliated Target
Viral life cycle - HIV-1	hsa03250	Affiliated Target
Class: Genetic Information Processing => Information processing in viruses	Pathway Hierarchy
cAMP signaling pathway	hsa04024	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
HIF-1 signaling pathway	hsa04066	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
FoxO signaling pathway	hsa04068	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Cell cycle	hsa04110	Affiliated Target
Class: Cellular Processes => Cell growth and death	Pathway Hierarchy
Wnt signaling pathway	hsa04310	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Notch signaling pathway	hsa04330	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
TGF-beta signaling pathway	hsa04350	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Adherens junction	hsa04520	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
JAK-STAT signaling pathway	hsa04630	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Long-term potentiation	hsa04720	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy
Melanogenesis	hsa04916	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Thyroid hormone signaling pathway	hsa04919	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Glucagon signaling pathway	hsa04922	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Growth hormone synthesis, secretion and action	hsa04935	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Click to Show/Hide the Information of Affiliated Human Pathways

Degree	97	Degree centrality	1.04E-02	Betweenness centrality	1.08E-02
Closeness centrality	2.80E-01	Radiality	1.47E+01	Clustering coefficient	1.20E-01
Neighborhood connectivity	4.71E+01	Topological coefficient	2.75E-02	Eccentricity	10
Download	Click to Download the Full PPI Network of This Target

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"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

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

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Target-regulating microRNAs

Target-regulating microRNAs Info

Target-interacting Proteins

Target-interacting Proteins Info

Target Affiliated Biological Pathways		Top
KEGG Pathway	[+] 25 KEGG Pathways	+
1	cAMP signaling pathway
2	HIF-1 signaling pathway
3	FoxO signaling pathway
4	Cell cycle
5	Wnt signaling pathway
6	Notch signaling pathway
7	TGF-beta signaling pathway
8	Adherens junction
9	Jak-STAT signaling pathway
10	Long-term potentiation
11	Melanogenesis
12	Thyroid hormone signaling pathway
13	Glucagon signaling pathway
14	Huntington's disease
15	Tuberculosis
16	Hepatitis B
17	Influenza A
18	HTLV-I infection
19	Herpes simplex infection
20	Epstein-Barr virus infection
21	Pathways in cancer
22	Viral carcinogenesis
23	MicroRNAs in cancer
24	Renal cell carcinoma
25	Prostate cancer
NetPath Pathway	[+] 1 NetPath Pathways	+
1	TCR Signaling Pathway
Panther Pathway	[+] 8 Panther Pathways	+
1	Hedgehog signaling pathway
2	Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
3	Huntington disease
4	Hypoxia response via HIF activation
5	TGF-beta signaling pathway
6	Transcription regulation by bZIP transcription factor
7	Wnt signaling pathway
8	p53 pathway
PID Pathway	[+] 26 PID Pathways	+
1	Regulation of nuclear SMAD2/3 signaling
2	Signaling events mediated by HDAC Class III
3	E2F transcription factor network
4	HIF-2-alpha transcription factor network
5	Validated targets of C-MYC transcriptional activation
6	Presenilin action in Notch and Wnt signaling
7	Signaling events mediated by TCPTP
8	Signaling events mediated by HDAC Class I
9	Role of Calcineurin-dependent NFAT signaling in lymphocytes
10	Glucocorticoid receptor regulatory network
11	FoxO family signaling
12	Posttranslational regulation of adherens junction stability and dissassembly
13	Direct p53 effectors
14	Regulation of Androgen receptor activity
15	IFN-gamma pathway
16	FOXM1 transcription factor network
17	C-MYB transcription factor network
18	Retinoic acid receptors-mediated signaling
19	Hedgehog signaling events mediated by Gli proteins
20	Signaling events mediated by Stem cell factor receptor (c-Kit)
21	HIF-1-alpha transcription factor network
22	p53 pathway
23	Regulation of retinoblastoma protein
24	FOXA1 transcription factor network
25	Notch-mediated HES/HEY network
26	IL12 signaling mediated by STAT4
Reactome	[+] 23 Reactome Pathways	+
1	Regulation of gene expression by Hypoxia-inducible Factor
2	RORA activates gene expression
3	BMAL1:CLOCK,NPAS2 activates circadian gene expression
4	Pre-NOTCH Transcription and Translation
5	PPARA activates gene expression
6	Formation of the beta-catenin:TCF transactivating complex
7	YAP1- and WWTR1 (TAZ)-stimulated gene expression
8	NOTCH1 Intracellular Domain Regulates Transcription
9	Transcriptional activation of mitochondrial biogenesis
10	Activation of gene expression by SREBF (SREBP)
11	Constitutive Signaling by NOTCH1 PEST Domain Mutants
12	Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
13	LRR FLII-interacting protein 1 (LRRFIP1) activates type I IFN production
14	HATs acetylate histones
15	Attenuation phase
16	Notch-HLH transcription pathway
17	Transcriptional regulation of white adipocyte differentiation
18	Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
19	Circadian Clock
20	CD209 (DC-SIGN) signaling
21	TRAF3-dependent IRF activation pathway
22	TRAF6 mediated IRF7 activation
23	Factors involved in megakaryocyte development and platelet production
WikiPathways	[+] 22 WikiPathways	+
1	SIDS Susceptibility Pathways
2	TGF Beta Signaling Pathway
3	Wnt Signaling Pathway and Pluripotency
4	TGF beta Signaling Pathway
5	IL-6 signaling pathway
6	Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
7	Cytosolic sensors of pathogen-associated DNA
8	Pre-NOTCH Expression and Processing
9	Transcriptional Regulation of White Adipocyte Differentiation
10	YAP1- and WWTR1 (TAZ)-stimulated gene expression
11	Regulation of Hypoxia-inducible Factor (HIF) by Oxygen
12	Signaling by NOTCH1
13	Activation of Gene Expression by SREBP (SREBF)
14	Notch Signaling Pathway
15	Integrated Pancreatic Cancer Pathway
16	TNF alpha Signaling Pathway
17	RIG-I/MDA5 mediated induction of IFN-alpha/beta pathways
18	Generic Transcription Pathway
19	Factors involved in megakaryocyte development and platelet production
20	Circadian Clock
21	Angiogenesis
22	Androgen receptor signaling pathway

References

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REF 1

Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14309-14.

REF 2

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 3

ClinicalTrials.gov (NCT03568656) Study to Evaluate CCS1477 in Advanced Tumours. U.S. National Institutes of Health.

REF 4

ClinicalTrials.gov (NCT01606579) Safety and Efficacy Study of PRI-724 in Subjects With Advanced Myeloid Malignancies. U.S. National Institutes of Health.

REF 5

ClinicalTrials.gov (NCT04575766) A Study of FT-7051 in Men With MCRPC. U.S. National Institutes of Health.

REF 6

Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov. 2021 May;11(5):1118-1137.

REF 7

Clinical pipeline report, company report or official report of FORMA Therapeutics.

REF 8

BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.

REF 9

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: 2734).

REF 10

A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem Biol. 2011 Apr 22;18(4):531-41.

REF 11

Bromodomains and their pharmacological inhibitors. ChemMedChem. 2014 Mar;9(3):438-64.

REF 12

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery. J Med Chem. 2012 Jan 26;55(2):576-86.

REF 13

Structural insights revealed by the cocrystal structure of CCS1477 in complex with CBP bromodomain. doi:10.1016/j.bbrc.2022.07.021.

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