Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03579
[1], [2]
Histone modification H3K27ac EP300 LINC01605 Indirect Enhancement m6A modification VEGFA VEGFA METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Vascular endothelial growth factor A (VEGFA)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone acetyltransferase p300 (P300) WRITER View Details
Regulated Target Histone H3 lysine 27 acetylation (H3K27ac) View Details
Downstream Gene LINC01605 View Details
Crosstalk Relationship Histone modification  →  m6A Enhancement
Crosstalk Mechanism histone modification indirectly regulates m6A modification through downstream signaling pathways
Crosstalk Summary LINC01605 was regulated by SMYD2-p300-mediated modifications of histone H3K4me3 as well as Histone H3 lysine 27 acetylation (H3K27ac). LINC01605 was found to bind to METTL3 and promote the m6A modification of SPTBN2 mRNA, thereby facilitating the translation of SPTBN2. EphA2 and Vascular endothelial growth factor A (VEGFA) targeted by METTL3 via different IGF2BP-dependent mechanisms were found to promote vasculogenic mimicry (VM) formation via PI3K/AKT/mTOR and ERK1/2 signaling in CRC.
Responsed Disease Colorectal cancer ICD-11: 2B91
Pathway Response PI3K-Akt signaling pathway hsa04151
Cell Process Cell proliferation and metastasis
Cell apoptosis
In-vitro Model
HCT 116 Colon carcinoma Homo sapiens CVCL_0291
NCM460 Normal Homo sapiens CVCL_0460
HT29 Colon cancer Mus musculus CVCL_A8EZ
LoVo Colon adenocarcinoma Homo sapiens CVCL_0399
DLD-1 Colon adenocarcinoma Homo sapiens CVCL_0248
SW480 Colon adenocarcinoma Homo sapiens CVCL_0546
SW620 Colon adenocarcinoma Homo sapiens CVCL_0547
In-vivo Model A total of 8 × 106 wild-type (WT) or METTL3-knockdown cells were injected into the dorsal flanks of 6-week-old nude mice. Seven mice were randomly selected to calculate the volume according to the following formula: V = (width2 × length)/2. Mice were euthanized three weeks after injection and tumors removed, weighed, fixed, and embedded for immunohistochemical analysis.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone acetyltransferase p300 (P300) 2 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name CCS1477 Phase 1/2 [3]
Synonyms
CCS-1477; CBP-IN-1; 2222941-37-7; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one; SCHEMBL20094038; SCHEMBL21515367; SCHEMBL22134021; EX-A3687; NSC818619; NSC-818619; HY-111784; CS-0091862; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-(trans-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name FT-7051 Phase 1 [4]
MOA Inhibitor
External Link
Vascular endothelial growth factor A (VEGFA) 85 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Ranibizumab Approved [5]
Synonyms
Ranibizumab (nasal spray, hereditary hemorrhagic telangiectasia)
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [6]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Brolucizumab Approved [7]
MOA Inhibitor
External Link
 Compound Name Faricimab Approved [8]
Synonyms
RO6867461; RG7716
    Click to Show/Hide
External Link
 Compound Name Aflibercept Approved [9]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Bevacizumab + Rituximab Phase 3 [10]
MOA Inhibitor
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [10]
MOA Inhibitor
External Link
 Compound Name Bevacizumab + Trastuzumab Phase 3 [10]
Synonyms
Lithocholic acid; 434-13-9; Lithocolic acid; Lithocholate; 3alpha-Hydroxy-5beta-cholanic acid; 3alpha-Hydroxy-5beta-cholan-24-oic acid; 3-Hydroxycholan-24-oic acid; 3alpha-Hydroxycholanic acid; 3-alpha-Hydroxycholanic acid; 5beta-Cholanic acid-3alpha-ol; NCI-C03861; 3alpha-Hydroxy-5beta-cholanoic acid; (3alpha,5beta)-3-hydroxycholan-24-oic acid; 3-alpha-Hydroxy-5-beta-cholanic acid; CCRIS 363; UNII-5QU0I8393U; 3alpha-Hydroxy-5beta-cholanate; 5-beta-Cholanic acid, 3-alpha-hydroxy-; Cholan-24-oic acid, 3-hydroxy-,
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Avastin+/-Tarceva Phase 3 [11]
Synonyms
Juglone; 481-39-0; 5-Hydroxy-1,4-naphthoquinone; 5-Hydroxy-1,4-naphthalenedione; Regianin; Juglon; Nucin; 5-Hydroxynaphthalene-1,4-dione; Walnut extract; 5-Hydroxynaphthoquinone; Akhnot; Yuglon; 8-Hydroxy-1,4-naphthoquinone; CI Natural Brown 7; 1,4-NAPHTHALENEDIONE, 5-HYDROXY-; 5-Hydroxy-p-naphthoquinone; 1,4-Naphthoquinone, 5-hydroxy-; CI 75500; Juglane; Jugnlon; Iuglon; Caswell No 515AA; 1,4-Naphthoquinone, 8-hydroxy-; 5-Hydroxy-1,4-naphthosemiquinone; 5-Hydroxy-1,4-naftochinon; UNII-W6Q80SK9L6; NSC 622948; NSC 153189; CCRIS
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Abicipar pegol Phase 2 [12]
MOA Inhibitor
External Link
 Compound Name PTC299 Phase 2 [13]
Synonyms
6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo(2,1-b)thiazole; skf-86002; 72873-74-6; Skf 86002; F 86002; F 86002-A(2); UNII-9R6QDF1UO7; 9R6QDF1UO7; CHEMBL313417; 5-(4-Pyridyl)-6-(4-fluorophenyl)-2,3-dihydroimidazo(2,1-b)-thiazole; 4-[6-(4-fluorophenyl)-2H,3H-imidazo[2,1-b][1,3]thiazol-5-yl]pyridine; 6-(4-fluorophenyl)-5-(4-pyridyl)-2,3-dihydroimidazo[2,1-b]thiazole; 6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridyl)imidazo[2,1-b]thiazole; Imidazo(2,1-b)thiazole,; SK&F 86002
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name RG7221 Phase 2 [14]
MOA Modulator
External Link
 Compound Name RO5520985 Phase 2 [15]
MOA Modulator
External Link
 Compound Name SNN-0029 Phase 1/2 [16]
Synonyms
VEGF (intracerebroventricular, amyotrophic lateral sclerosis), NeuroNova/VIB/Genentech
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name MP0250 Phase 1/2 [17]
MOA Inhibitor
External Link
 Compound Name AT001/r84 Phase 1 [18]
External Link
 Compound Name MP-0112 Phase 1 [19]
Synonyms
DARPin (age related macular degeneration), Molecular Partners/Allergan; VEGF-A specific DARPin, Molecular Partners/Allergan
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Navicixizumab Phase 1 [20]
External Link
 Compound Name SFLT-01 Phase 1 [21]
Synonyms
AAV2-sFLT-01; VEGF/PIGF suppression gene therapy (cancer), Genzyme; SFLT-01 gene therapy (wet AMD), AGTC/Genzyme; VEGF suppression gene therapy (wet age-related macular degeneration), Applied Genetic Technologies/ Genzyme
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name ABI-011 Phase 1 [17]
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 17 Patented [22]
Synonyms
PMID28621580-Compound-WO2012089137c13
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 16 Patented [22]
Synonyms
PMID28621580-Compound-WO2012028106c12
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 18 Patented [22]
Synonyms
PMID28621580-Compound-WO2014086102c29
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Antibodie derivative 11 Patented [22]
Synonyms
PMID28621580-Compound-WO2016059057
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External Link
 Compound Name Pyridine derivative 2 Patented [22]
Synonyms
PMID28621580-Compound-US20130096136c42
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
 Compound Name Indoline derivative 16 Patented [22]
Synonyms
PMID28621580-Compound-WO2013037293c26
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 31 nM
External Link
 Compound Name Carbamide derivative 22 Patented [22]
Synonyms
PMID28621580-Compound-WO2014040243c18
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 15 to 1000 nM
External Link
 Compound Name Oxetane 3,3-dicarboxamide compound 1 Patented [22]
Synonyms
PMID28621580-Compound-WO2013032797c63
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 Patented [22]
Synonyms
PMID28621580-Compound-WO2012084683c62
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1,6-naphyridine-4-ketone fused heterocyclic derivative 1 Patented [22]
Synonyms
PMID28621580-Compound-WO2013097753c65
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyrimidine derivative 5 Patented [22]
Synonyms
PMID28621580-Compound-US20160096832c60
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MOA Inhibitor
External Link
 Compound Name PMID28621580-Compound-WO2013112959C68 Patented [22]
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 23 Patented [22]
Synonyms
PMID28621580-Compound-WO2014201127c20
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 7 Patented [22]
Synonyms
PMID28621580-Compound-WO2013112950c37
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID28621580-Compound-WO2015089220C70 Patented [22]
MOA Inhibitor
External Link
 Compound Name Pyrimidine derivative 9 Patented [22]
Synonyms
PMID28621580-Compound-WO2010066684c55
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 4 Patented [22]
Synonyms
PMID28621580-Compound-WO2012127012c31
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MOA Inhibitor
External Link
 Compound Name Pyridine derivative 5 Patented [22]
Synonyms
PMID28621580-Compound-WO2013015657c41
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 15 Patented [22]
Synonyms
PMID28621580-Compound-US20160096828c21
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
 Compound Name Antibodie derivative 3 Patented [22]
Synonyms
PMID28621580-Compound-WO2012125123
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External Link
 Compound Name Pyrimidine derivative 7 Patented [22]
Synonyms
PMID28621580-Compound-US20169233968c59
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MOA Inhibitor
External Link
 Compound Name Carbamide derivative 18 Patented [22]
Synonyms
PMID28621580-Compound-WO2012094451c15
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MOA Inhibitor
External Link
 Compound Name Indoline derivative 21 Patented [22]
Synonyms
PMID28621580-Compound-WO2015117551c25
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 65 nM
External Link
 Compound Name Pyrimidine derivative 10 Patented [22]
Synonyms
PMID28621580-Compound-WO2014000686c53
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 7 Patented [22]
Synonyms
PMID28621580-Compound-WO2013044362c44
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MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 6 Patented [22]
Synonyms
PMID28621580-Compound-WO2013040515c36
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Antibodie derivative 7 Patented [22]
Synonyms
PMID28621580-Compound-WO2014055998
    Click to Show/Hide
MOA Binder
External Link
 Compound Name Antibodie derivative 2 Patented [22]
Synonyms
PMID28621580-Compound-WO2012088563
    Click to Show/Hide
MOA Binder
External Link
 Compound Name Pyridine derivative 3 Patented [22]
Synonyms
PMID28621580-Compound-US20140336108c48
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 8 Patented [22]
Synonyms
PMID28621580-Compound-WO2014029250c45
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 19 Patented [22]
Synonyms
PMID28621580-Compound-WO2012139499c14
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 13 Patented [22]
Synonyms
PMID28621580-Compound-WO2012088506c23
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyrimidine derivative 11 Patented [22]
Synonyms
PMID28621580-Compound-WO2014139458c54
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyrimidine derivative 8 Patented [22]
Synonyms
PMID28621580-Compound-US20169296747c52
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 10 Patented [22]
Synonyms
PMID28621580-Compound-WO2014127335c34
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 8 Patented [22]
Synonyms
PMID28621580-Compound-WO2014113859c33
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 10 Patented [22]
Synonyms
PMID28621580-Compound-WO2014040242c47
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 14 Patented [22]
Synonyms
PMID28621580-Compound-WO2012139019c24
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID28621580-Compound-WO2014079545C69 Patented [22]
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 14 Patented [22]
Synonyms
PMID28621580-Compound-US20140256819c19
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 460 nM
External Link
 Compound Name Pyridine derivative 11 Patented [22]
Synonyms
PMID28621580-Compound-WO2015075483c49
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 9 Patented [22]
Synonyms
PMID28621580-Compound-WO2014029251c46
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 5 Patented [22]
Synonyms
PMID28621580-Compound-WO2012171487c32
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 4 Patented [22]
Synonyms
PMID28621580-Compound-WO2012169934c40
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 32 nM
External Link
 Compound Name Quinoline and quinazoline derivative 3 Patented [22]
Synonyms
PMID28621580-Compound-US20150158854c39
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 2 Patented [22]
Synonyms
PMID28621580-Compound-US20130165458c38
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 17 Patented [22]
Synonyms
PMID28621580-Compound-WO2014086102c28
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 19 Patented [22]
Synonyms
PMID28621580-Compound-WO2014102377c27
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyridine derivative 6 Patented [22]
Synonyms
PMID28621580-Compound-WO2013044361c43
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Quinoline and quinazoline derivative 9 Patented [22]
Synonyms
PMID28621580-Compound-WO2014127214c35
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivative 1 Patented [22]
Synonyms
PMID28621580-Compound-WO2013101954c67
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID28621580-Compound-WO2013036866C66 Patented [22]
MOA Inhibitor
External Link
 Compound Name Antibodie derivative 8 Patented [22]
Synonyms
PMID28621580-Compound-WO2014081202
    Click to Show/Hide
MOA Disrupter
External Link
 Compound Name Pyrimidine derivative 6 Patented [22]
Synonyms
PMID28621580-Compound-US20160096837c61
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MOA Inhibitor
External Link
 Compound Name Carbamide derivative 20 Patented [22]
Synonyms
PMID28621580-Compound-WO2013037292c17
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indoline derivative 15 Patented [22]
Synonyms
PMID28621580-Compound-WO2012139019c25
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 65 nM
External Link
 Compound Name Antibodie derivative 9 Patented [22]
Synonyms
PMID28621580-Compound-WO2016044219
    Click to Show/Hide
MOA Stablizer
External Link
 Compound Name Antibodie derivative 1 Patented [22]
Synonyms
PMID28621580-Compound-WO2012004631
    Click to Show/Hide
MOA Blocker
External Link
 Compound Name Indoline derivative 20 Patented [22]
Synonyms
PMID28621580-Compound-WO2015117551c24
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Carbamide derivative 21 Patented [22]
Synonyms
PMID28621580-Compound-WO2013107225c16
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MOA Inhibitor
External Link
 Compound Name Antibodie derivative 4 Patented [22]
Synonyms
PMID28621580-Compound-WO2012161372
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MOA Inhibitor
External Link
 Compound Name Indoline derivative 12 Patented [22]
Synonyms
PMID28621580-Compound-WO2012088506c22
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MOA Inhibitor
External Link
 Compound Name Oxetane 3,3-dicarboxamide compound 2 Patented [22]
Synonyms
PMID28621580-Compound-WO2013032797c64
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MOA Inhibitor
External Link
 Compound Name Bevasiranib Discontinued in Phase 3 [23]
MOA Modulator
External Link
 Compound Name ALN-VEG01 Terminated [24]
Synonyms
RNAi therapeutics (ocular disease), Alnylam; VEGF-silencing siRNAs, Alnylam; Vascular endothelial growth factor gene-silencing siRNAs, Alnylam; RNAi therapeutics (ocular disease), Alnylam/Merck; VEGF-silencing siRNAs, Alnylam/Merck; Vascular endothelial growth factor-silencing siRNAs, Alnylam/Merck
    Click to Show/Hide
External Link
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [25]
Synonyms
INCMGA0012; Retifanlimab
    Click to Show/Hide
External Link
 Compound Name Aflibercept Approved [9]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
External Link
 Compound Name Regorafenib Approved [26]
Synonyms
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [17]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
    Click to Show/Hide
External Link
 Compound Name SYM-004 Phase 3 [17]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
    Click to Show/Hide
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [27]
External Link
 Compound Name CPI-613 Phase 3 [17]
Synonyms
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [9]
External Link
 Compound Name AlloStim Phase 2/3 [28]
Synonyms
AlloStim (TN)
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External Link
 Compound Name Sibrotuzumab Phase 2 [29]
External Link
 Compound Name CV301 Phase 2 [30]
External Link
 Compound Name Efatutazone Phase 2 [31]
Synonyms
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
    Click to Show/Hide
External Link
 Compound Name LOR-2040 Phase 2 [32]
External Link
 Compound Name RG7221 Phase 2 [20]
External Link
 Compound Name PEG-SN38 Phase 2 [33]
Synonyms
EZN-2208
    Click to Show/Hide
External Link
 Compound Name MEGF0444A Phase 2 [34]
External Link
 Compound Name Encapsulated cell therapy Phase 1/2 [35]
External Link
 Compound Name AB928 Phase 1/2 [36]
External Link
 Compound Name MGD007 Phase 1 [20]
External Link
 Compound Name BNC-101 Phase 1 [37]
External Link
 Compound Name Navicixizumab Phase 1 [17]
External Link
 Compound Name RG7160 Discontinued in Phase 2 [38]
External Link
 Compound Name Nimesulide Terminated [39]
Synonyms
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
    Click to Show/Hide
External Link
 Compound Name Saracatinib Phase 2 [40]
External Link
 Compound Name G3139 + Irinotecan Investigative [41]
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References
Ref 1 LINC01605, regulated by the EP300-SMYD2 complex, potentiates the binding between METTL3 and SPTBN2 in colorectal cancer. Cancer Cell Int. 2021 Sep 20;21(1):504. doi: 10.1186/s12935-021-02180-8.
Ref 2 m6A methylated EphA2 and VEGFA through IGF2BP2/3 regulation promotes vasculogenic mimicry in colorectal cancer via PI3K/AKT and ERK1/2 signaling. Cell Death Dis. 2022 May 21;13(5):483. doi: 10.1038/s41419-022-04950-2.
Ref 3 Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov. 2021 May;11(5):1118-1137. doi: 10.1158/2159-8290.CD-20-0751. Epub 2021 Jan 11.
Ref 4 Clinical pipeline report, company report or official report of FORMA Therapeutics.
Ref 5 Development of ranibizumab, an anti-vascular endothelial growth factor antigen binding fragment, as therapy for neovascular age-related macular degeneration. Retina. 2006 Oct;26(8):859-70. doi: 10.1097/01.iae.0000242842.14624.e7.
Ref 6 FDA Approved Drug Products from FDA Official Website. 2004. Application Number: (ANDA) 125085.
Ref 7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
Ref 8 Faricimab: an investigational agent targeting the Tie-2/angiopoietin pathway and VEGF-A for the treatment of retinal diseases. Expert Opin Investig Drugs. 2021 Mar;30(3):193-200.
Ref 9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 10 Clinical pipeline report, company report or official report of Roche (2009).
Ref 11 Clinical pipeline report, company report or official report of Genentech (2009).
Ref 12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 13 Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015 Jan;121(1):217-24. doi: 10.1007/s11060-014-1665-1. Epub 2014 Nov 19.
Ref 14 Bispecific antibodies and their applications
Ref 15 Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
Ref 16 Clinical pipeline report, company report or official report of Neuronova.
Ref 17 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 18 Clinical pipeline report, company report or official report of Affitech (2011).
Ref 19 Treatment of exudative age-related macular degeneration with a designed ankyrin repeat protein that binds vascular endothelial growth factor: a phase I/II study. Am J Ophthalmol. 2014 Oct;158(4):724-732.e2.
Ref 20 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 21 sFLT01: a novel fusion protein with antiangiogenic activity. Mol Cancer Ther. 2011 Mar;10(3):404-15. doi: 10.1158/1535-7163.MCT-10-0813. Epub 2011 Jan 20.
Ref 22 VEGFR-2 inhibitors and the therapeutic applications thereof: a patent review (2012-2016). Expert Opin Ther Pat. 2017 Sep;27(9):987-1004. doi: 10.1080/13543776.2017.1344215. Epub 2017 Jun 23.
Ref 23 Bevasiranib for the Treatment of Wet, Age-Related Macular Degeneration
Ref 24 TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751.
Ref 25 Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway.J Med Chem. 2019 Feb 28;62(4):1715-1730.
Ref 26 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: 5891).
Ref 27 ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer
Ref 28 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 29 ClinicalTrials.gov (NCT02198274) Intravenous BIBH 1 in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
Ref 30 ClinicalTrials.gov (NCT03547999) A Trial of Perioperative CV301 Vaccination in Combination With Nivolumab and Systemic Chemotherapy for Metastatic CRC. U.S. National Institutes of Health.
Ref 31 ClinicalTrials.gov (NCT02152137) Efatutazone With Paclitaxel Versus Paclitaxel Alone in Treating Patients With Advanced Anaplastic Thyroid Cancer. U.S. National Institutes of Health.
Ref 32 ClinicalTrials.gov (NCT00087165) GTI-2040, Docetaxel, and Prednisone in Treating Patients With Prostate Cancer. U.S. National Institutes of Health.
Ref 33 ClinicalTrials.gov (NCT01036113) A Phase 2 Study of EZN-2208 in Patients With Metastatic Breast Cancer. U.S. National Institutes of Health.
Ref 34 ClinicalTrials.gov (NCT00909740) A Study of the Safety and Pharmacokinetics of MEGF0444A Administered to Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 35 VC-01's Path to the Clinic. Viacyte. 2015.
Ref 36 ClinicalTrials.gov (NCT04660812) An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.
Ref 37 ClinicalTrials.gov (NCT02726334) A Phase I, Dose Escalation Study of BNC101 in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.
Ref 38 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029052)
Ref 39 Clinical pipeline report, company report or official report of Genentech (2011).
Ref 40 Phase II Study of Saracatinib (AZD0530) in Patients With Previously Treated Metastatic Colorectal Cancer. Invest New Drugs. 2015 Aug;33(4):977-84.
Ref 41 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.