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PI3K/Akt/mTOR
- PI3K
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Epigenetics
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Methylation
- DNA Methyltransferase
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- WDR5
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Immunology & Inflammation
- CD markers
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Protein Tyrosine Kinase
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Angiogenesis
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Apoptosis
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- TNF-alpha
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- Survivin
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- OXPHOS
- Heme Oxygenase
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Autophagy
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ER stress & UPR
- JNK
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JAK/STAT
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MAPK
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Cytoskeletal Signaling
- Akt
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- Dynamin
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- Integrin
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- TACC3
- MLCK
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- Actin
Cell Cycle
- CDK
- DNA/RNA Synthesis
- PD-1/PD-L1
- Ras
- Aurora Kinase
- HSP (HSP90)
- Kinesin
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- DHFR
- PLK
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- Wee1
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- Myc
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- BMI-1
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TGF-beta/Smad
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DNA Damage/DNA Repair
- HDAC
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- RNR
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- SMN
- Nucleoside Analog/Antimetabolite
- LIM kinase
- RAD51
- CRISPR/Cas9
- BMI-1
- Pax
- FENs
- OGG1
- Thymidylate Synthase
- G-quadruplex
Stem Cells & Wnt
- GSK-3
- JAK
- STAT
- TGF-beta/Smad
- Wnt/beta-catenin
- ROCK
- Hedgehog/Smoothened
- PKA
- ERK
- Stemness kinase
- KLF
- OCT
- Casein Kinase
- SFRP
- Fascin
- PORCN
- Notch
- Secretase
Hippo
- LATS
- TEAD
- MAP4K
- MST
- YAP
Ubiquitin
- Proteasome
- DUB
- p97
- E1 Activating
- SUMO
- E2 conjugating
- E3 Ligase
Neuronal Signaling
- Calcium Channel
- Beta Amyloid
- 5-HT Receptor
- COX
- GluR
- Adrenergic Receptor
- AChR
- Histamine Receptor
- Dopamine Receptor
- Opioid Receptor
- GABA Receptor
- P-gp
- P2 Receptor
- Cannabinoid Receptor
- OX Receptor
- CGRP Receptor
- MT Receptor
- MAO
- FAAH
- BACE
- Trk receptor
- GlyT
- NMDAR
- CaMK
- Neurokinin Receptor
- Notch
- Imidazoline Receptor
- Sigma Receptor
- NPY receptor
- Serotonin Transporter
- CCK receptor
- COMT
- Neurotensin Receptor
- Melanocortin Receptor
- Adenosine Deaminase
- TRP Channel
- Adenosine Kinase
- BChE
- EAAT
NF-κB
- HDAC
- NF-κB
- IκB/IKK
- MALT
- Nrf2
- ROS
- NOD
- AP-1
- Antioxidant
GPCR & G Protein
- Ras
- 5-HT Receptor
- CCR
- GluR
- Adrenergic Receptor
- AChR
- Histamine Receptor
- Dopamine Receptor
- Opioid Receptor
- GPR
- P2 Receptor
- Cannabinoid Receptor
- Endothelin Receptor
- S1P Receptor
- Hedgehog/Smoothened
- SGLT
- LPA Receptor
- OX Receptor
- CGRP Receptor
- MT Receptor
- PAFR
- PKA
- Adenosine Receptor
- Vasopressin Receptor
- cAMP
- CXCR
- CaSR
- TAAR
- Glucagon Receptor
- LTR
- PAR
- Taste Receptor
- NPY receptor
- Parathyroid Hormone Receptor
- DOCK
- AdipoR
- GPCR19
- Guanylate Cyclase
- GHSR
- CCK receptor
- GRK
- Leukotriene
- FPR
- Prostaglandin Receptor
- PKD
- TSH Receptor
- Neurokinin Receptor
- GNRH Receptor
- PKG
- CRFR
- Angiotensin Receptor
- Bradykinin Receptor
- Imidazoline Receptor
- Bombesin Receptor
- RGS
- Neurotensin Receptor
- Sigma Receptor
- Melanocortin Receptor
Endocrinology & Hormones
- Adrenergic Receptor
- 5-alpha Reductase
- Estrogen/progestogen Receptor
- Androgen Receptor
- RAAS
- Opioid Receptor
- Aromatase
- GPR
- Glucocorticoid Receptor
- PGES
- TSH Receptor
- GNRH Receptor
- PGDS
- Mineralocorticoid Receptor
- THR
- ACE
- SSTR
- GHSR
- CCK receptor
Transmembrane Transporters
- CD markers
- Calcium Channel
- Sodium Channel
- ATPase
- Chloride Channel
- Potassium Channel
- GluR
- AChR
- GABA Receptor
- P-gp
- Proton Pump
- CFTR
- P2 Receptor
- SGLT
- NMDAR
- OCT
- CRM1
- GLUT
- GlyT
- Aquaporin
- EAAT
- VDAC
- MTP
- VMAT
- GlyR
- MCT
- Amino acid transporter
- Mechanosensitive Channel
- OAT
- NKCC
- BCRP
- NCX
- OATP
- TRP Channel
- VRAC
Metabolism
- PPAR
- P450 (e.g. CYP17)
- HSP (HSP90)
- PDE
- Hydroxylase
- Factor Xa
- DHFR
- Aminopeptidase
- Dehydrogenase
- Procollagen C Proteinase
- Phospholipase (e.g. PLA)
- DPP
- Carbonic Anhydrase
- Phosphorylase
- Liver X Receptor
- FAAH
- Acyltransferase
- phosphatase
- GLUT
- HMG-CoA Reductase
- Vitamin
- PKM
- Lipoxygenase
- FOX
- Lipase
- Fatty Acid Synthase
- LDL
- NAMPT
- Casein Kinase
- Decarboxylase
- Retinoid Receptor
- Thioredoxin
- FXR
- Transferase
- Serine/threonin kinase
- CETP
- IDO/TDO
- SCD
- CPT
- AP-1
- LDH
- Carbohydrate Metabolism
- CAR
- PAI-1
- γGCS
- SSTR
- ATP-citrate lyase
- FAO
- FTase
- SOD
- 3-MST
- GTPCH
- SGK
- GOT
- Serine hydrolase
- Epoxide Hydrolase
- glucocerebrosidase
- FABP
- Catalase
- THR
- ACSS2
- ROR
- Glucosylceramide Synthase
- ACE
- Thioredoxin Reductase
- PDHK
- PARG
- Xanthine Oxidase
- Mannosidase
- PGC-1α
- Adenosine Deaminase
- Aldose Reductase
- CPSase
- Leukotriene
- Adenosine Kinase
- OXPHOS
- Glutathione
- Acetyl-CoA carboxylase
- Mitochondrial Metabolism
- Peroxidases
- SHIP
- PCSK9
- PGDS
- Mitochondrial pyruvate carrier
- PREP
- PP2A
- Neprilysin
- RUNX
- FTO
- AdipoR
- PAD
- SREBP
Proteases
- HDAC
- Proteasome
- Caspase
- Aminopeptidase
- HCV Protease
- DPP
- HIV Protease
- MMP
- Thrombin
- Acyltransferase
- Cysteine Protease
- MALT
- Glutaminase
- Tyrosinase
- Serine Protease
- Cathepsin B
- PGDS
- Neprilysin
- SGK
- PREP
- GOT
- 3C-Like Protease
- PAD
- PCSK9
- Secretase
Microbiology
- HCV Protease
- Integrase
- Reverse Transcriptase
- HIV Protease
- Anti-infection
- HIV
- Fungal
- CMV
- Neuraminidase
- Parasite
- Thioredoxin Reductase
- Antiviral
- β-lactamase
- Bacterial
- 3C-Like Protease
- Antibiotics
- Enterovirus
- COVID-19
- Influenza Virus
- Ribosomal Peptidyl Transferase
- SARS-CoV
- RSV
- HPV
- HSV
- HCV
- HBV
Others
- ADC Cytotoxin
- ADC Linker
- Drug-Linker Conjugates for ADC
- Antineoplastic and Immunosuppressive Antibiotics
- Selection Antibiotics for Transfected Cell
- Antibiotics for Mammalian Cell Culture
- Antibiotics for Plant Cell Culture
- Hydrotropic Agents
- Dyes
- PROTAC
- PROTAC Linker
- E3 ligase Ligand
- Target Protein Ligand
- Others
- Antibody-Drug Conjugate

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NVP-BKM120 inhibits colon cancer growth via FoxO3a-dependent PUMA induction

by Selleckchem | Oct 12 2019

NVP-BKM120, a potent and highly selective PI3K inhibitor, is currently being investigated in phase I/II clinical trials. The mechanisms of action of NVP-BKM120 in colon cancer cells are unclear. In the present study, we investigated how NVP-BKM120 suppresses colon cancer cells growth and potentiates effects of other chemotherapeutic drugs. We found that NVP-BKM120 treatment enhance PUMA induction irrespective of p53 status through the FoxO3a pathway following AKT inhibition. Furthermore, PUMA is required for NVP-BKM120-induced apoptosis in colon cancer cells. In addition, NVP-BKM120 also synergized with 5-Fluorouracil or regorafenib to induce marked apoptosis via PUMA induction. Deficiency of PUMA suppressed apoptosis and antitumor effect of NVP-BKM120 in xenograft model. These results demonstrate a key role of PUMA in mediating the anticancer effects of NVP-BKM120 and suggest that PUMA could be used as an indicator of NVP-BKM120 sensitivity, and also have important implications for it clinical applications.

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S2247	Buparlisib (BKM120)	Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.

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