CYP2D6 Cancer Research Results

CYP2D6, Cytochrome P450 Family 2 Subfamily D Member 6: Click to Expand ⟱
Source:
Type: drug-metabolism / pharmacogenetic target

CYP2D6 - Cytochrome P450 Family 2 Subfamily D Member 6

Type: Cytochrome P450 monooxygenase / drug-metabolism enzyme / pharmacogenetic marker

Function: CYP2D6 is a highly polymorphic cytochrome P450 enzyme responsible for oxidative metabolism of numerous drugs and xenobiotics. Genetic variation produces poor, intermediate, normal, and ultrarapid metabolizer phenotypes and can substantially alter drug exposure, efficacy, and toxicity.

Cancer: ↕ Context-dependent. CYP2D6 can either activate or inactivate pharmacologically active compounds and therefore has treatment-specific effects rather than a uniform oncogenic or tumor-suppressive role. In estrogen-receptor-positive breast cancer, CYP2D6 contributes importantly to conversion of tamoxifen to the potent active metabolite endoxifen; reduced CYP2D6 activity can result in lower endoxifen concentrations and potentially reduced tamoxifen efficacy.
Scientific Papers found: Click to Expand⟱
7565- HYP,    Potential Implications of Hyperoside on Oxidative Stress-Induced Human Diseases: A Comprehensive Review
- Review, AD, NA
*Inflam↓, exhibits a multitude of biological functions including anti-inflammatory, antidepressant, antioxidative, vascular protective effects and neuroprotective effects,
*antiOx↑,
*neuroP↑,
*lipid-P↓, Anti-oxidant Saccharomyces Cerevisiae 5, 20 mg/L Decreased LPO and the level of ROS
*ROS↓,
*IL1β↓, HT22 cells 20 μM Alleviates the level of IL-1β, IL-6, IL-8, TNF-α, ROS, MDA, Bax, and caspase-3; increases the expression of CAT, SOD, GSH, Bcl-2, BDNF, TrkB, and NGF.
*IL6↓,
*IL8↓,
*TNF-α↓,
*MDA↓,
*BAX↓,
*Casp3↓,
*Catalase↑,
*SOD↑,
*GSH↑,
*BDNF↑,
*TrkB↑,
*NGF↑,
*BDNF↑, Male Albino Swiss mice 0.94 mg/kg, 3.75 mg/kg Mediated by monoaminergic system and the upregulation of BDNF level
*NF-kB↓, Inhibited the activation of NF-κB, lessened the expression of iNOS,
*AChE↓, ICR mice 2.5 mg/kg Inhibited AchE activity
*H2S↑, SD rats 1, 10, 100 μM Upregulation of H2S,
Casp3↑, Anti-lung cancer A549 cells, Balb/c-nude mice 15, 20, 25 μM in vitro 15, 20, 25 mg/kg in vivo Activation of caspase-3 to motivate apoptosis and inactivation of NF-κB to inhibit inflammatory
Apoptosis↑,
NF-kB↓,
AMPK↑, A549 cells 10, 50, 100 μM Upregulation of AMPK signal pathway and HO-1 expression to suppressed the survival and proliferation of A549 cells
HO-1↑,
MAPK↑, A549 cells, H466 cells, C57BL/6J mice – Upregulated the expression of p38 MAPK, caspase 3, caspase 9, cleaved caspase 3, cleaved caspase 9 and Bax, downregulated the expression of Cu/Zn SOD, CAT, Nrf2, NQO1, HO-1 and Bcl-2
cl‑Casp3↑,
cl‑Casp9↑,
BAX↑,
SOD?,
Catalase↓,
NRF2↓,
NQO1↓,
HO-1↓,
Bcl-2↓,
TumCCA↑, A549 cells 10, 20, 50, 100, 200, 400 μg/mL Inhibited the process of G1/S phase to inhibit proliferation
FOXO1↑, NCI-H1975 cells, PC-9 cells, Nude male mice 30, 60, 90, 120, 150 μM in vitro, 25 mg/kg in vivo Upregulation of FoxO1
TumAuto↑, A549 cells 0.5, 1, 2 mM Induced autophagy through inhibiting the Akt/mTOR/p70S6K signal pathway
Akt↓,
mTOR↓,
P70S6K↓,
BMP7/OP1↓, HepG2 cells 5, 10, 20, 40, 80 μM Inhibiting the BMP-7
*cardioP↑, Cardiovascular Protective Effect
*hepatoP↑, Hepatoprotective
*antiCG↑, The report indicates hyperoside possesses antithrombotic activities and offer bases for development of a novel anticoagulant
*AntiThr↑,
*Diar↓, Antidiarrheal Activity
*AntiFungal↑, Antifungal Activity
*CYP2D6↓, hyperoside is a potent selective CYP2D6 inhibitor in HLMs, and might cause herb-drug interactions when co-administrated with CYP2D substrates.
*PDGFR-BB↓, In diabetic rats’ model, hyperoside inhibited the platelet-derived growth factor-BB (PDGF-BB)/platelet-derived growth factor-B receptor (PDGFR-β) ligand binding
*PDGFRB↓,
*toxicity↓, In research conducted in Wistar rats, the researchers demonstrated that in a long-term oral administration lasted for 6 months, hyperoside has a good safety. And the possible target organ of toxicity is kidney and the damage is reversible
*Half-Life↑, hyperoside also showed a long half-life for 4 hours and the safety experiments also proves that it has good safety.

7769- IBC,    Potential Determinants for Metabolic Fates and Inhibitory Effects of Isobavachalcone Involving in Human Cytochrome P450, UDP-Glucuronosyltransferase Enzymes, and Efflux Transporters
- in-vivo, NA, NA
*AntiCan↑, Isobavachalcone, a naturally occurring chalcone in Psoralea corylifolia, posses many biological properties including anticancer, antiplatelet, and antifungal.
*AntiAg↑,
*AntiFungal↑,
CYP2C9↓, isobavachalcone demonstrated broad-spectrum inhibitory effects against CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, UGT1A1, UGT1A9, UGT2B7 with IC50 values of 1.08-9.78 μM.
UGT1A↓,
CYP2D6↓,
CYP2E1↓,


Showing Research Papers: 1 to 2 of 2

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 2

Pathway results for Effect on Cancer / Diseased Cells:


NA, unassigned(tgid=0) ⓘ

BMP7/OP1↓, 1,   CYP2D6↓, 1,   UGT1A↓, 1,  

Redox & Oxidative Stress(tgid=1) ⓘ

Catalase↓, 1,   CYP2E1↓, 1,   HO-1↓, 1,   HO-1↑, 1,   NQO1↓, 1,   NRF2↓, 1,   SOD?, 1,  

Core Metabolism/Glycolysis(tgid=4) ⓘ

AMPK↑, 1,  

Cell Death(tgid=5) ⓘ

Akt↓, 1,   Apoptosis↑, 1,   BAX↑, 1,   Bcl-2↓, 1,   Casp3↑, 1,   cl‑Casp3↑, 1,   cl‑Casp9↑, 1,   MAPK↑, 1,  

Autophagy & Lysosomes(tgid=9) ⓘ

TumAuto↑, 1,  

Cell Cycle & Senescence(tgid=11) ⓘ

TumCCA↑, 1,  

Proliferation, Differentiation & Cell State(tgid=12) ⓘ

FOXO1↑, 1,   mTOR↓, 1,   P70S6K↓, 1,  

Immune & Inflammatory Signaling(tgid=16) ⓘ

NF-kB↓, 1,  

Drug Metabolism & Resistance(tgid=21) ⓘ

CYP2C9↓, 1,  
Total Targets: 26

Pathway results for Effect on Normal Cells:


NA, unassigned(tgid=0) ⓘ

antiCG↑, 1,   CYP2D6↓, 1,  

Redox & Oxidative Stress(tgid=1) ⓘ

antiOx↑, 1,   Catalase↑, 1,   GSH↑, 1,   lipid-P↓, 1,   MDA↓, 1,   ROS↓, 1,   SOD↑, 1,  

Core Metabolism/Glycolysis(tgid=4) ⓘ

H2S↑, 1,  

Cell Death(tgid=5) ⓘ

BAX↓, 1,   Casp3↓, 1,  

Transcription & Epigenetics(tgid=7) ⓘ

AntiThr↑, 1,  

Proliferation, Differentiation & Cell State(tgid=12) ⓘ

PDGFRB↓, 1,  

Migration(tgid=13) ⓘ

AntiAg↑, 1,  

Angiogenesis & Vasculature(tgid=14) ⓘ

PDGFR-BB↓, 1,  

Immune & Inflammatory Signaling(tgid=16) ⓘ

IL1β↓, 1,   IL6↓, 1,   IL8↓, 1,   Inflam↓, 1,   NF-kB↓, 1,   TNF-α↓, 1,  

Synaptic & Neurotransmission(tgid=18) ⓘ

AChE↓, 1,   BDNF↑, 2,   NGF↑, 1,   TrkB↑, 1,  

Drug Metabolism & Resistance(tgid=21) ⓘ

Half-Life↑, 1,  

Clinical Biomarkers(tgid=22) ⓘ

IL6↓, 1,  

Functional Outcomes(tgid=23) ⓘ

AntiCan↑, 1,   cardioP↑, 1,   hepatoP↑, 1,   neuroP↑, 1,   toxicity↓, 1,  

Infection & Microbiome(tgid=24) ⓘ

AntiFungal↑, 2,   Diar↓, 1,  
Total Targets: 35

Scientific Paper Hit Count for: CYP2D6, Cytochrome P450 Family 2 Subfamily D Member 6
Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells

Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:%  Target#:1661  State#:%  Dir#:1
  wNotes=on  sortOrder:rid,rpid

 

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