CYP1A2

What is CYP1A2 Protein?

CYP1A2 is a protein that works quietly but importantly in our bodies. Part of the cytochrome P450 family, it helps process a range of chemicals. You’ll mostly find CYP1A2 in the liver, where it breaks down things like drugs, caffeine, and some hormones. It acts like a natural filter, making sure we detoxify or convert what we consume into something useful or ready to be expelled. Because it plays a big part in drug metabolism, scientists are very interested in how CYP1A2 functions. When new medicines are being developed, understanding this protein is key because how active it is can change how well a drug works or what side effects might appear.

What is the Function of CYP1A2 Protein?

CYP1A2 is a busy protein found in our liver and a part of the cytochrome P450 group. Its main job is to help break down all kinds of substances we consume. This includes processing medications, so they work effectively in our bodies. It also deals with caffeine and some hormones, ensuring they're handled the right way. You can think of CYP1A2 as a natural filter, detoxifying chemicals and turning them into forms we can either use or safely eliminate. How well CYP1A2 works can change how drugs behave in our system, affecting their success and any side effects. Because of this, scientists pay a lot of attention to CYP1A2, especially when creating new drugs, since variations in its activity can influence how well medicines work and interact.

CYP1A2 Related Signaling Pathway

CYP1A2 is part of an important signaling pathway in our body that involves breaking down various chemicals. Located mainly in the liver, this protein is key for processing drugs and compounds we encounter daily. It works by helping to modify these substances into something our bodies can use or get rid of. This pathway influences how effectively drugs work and their potential side effects. Changes in this signaling pathway can affect everything from how quickly a drug leaves our system to how active certain compounds become. Because of this, understanding the CYP1A2 pathway helps researchers and doctors predict drug interactions and personalize treatments for safer and more effective therapies.

CYP1A2 Related Diseases

CYP1A2 plays a big role in processing what we put into our bodies, and when it’s off, health issues can arise. It's especially important for how we break down drugs and caffeine. If CYP1A2 is out of whack, medicines might not perform right, or you might experience side effects since they're not broken down properly. Plus, research suggests that how active CYP1A2 is could affect the risk of some cancers, especially those linked to hormones, like breast cancer. Since CYP1A2 also helps detoxify substances, changes in its activity could impact liver-related conditions. Doctors keep a close eye on CYP1A2 to tailor treatments and potentially lower the risk of these issues by tracking how active this protein is.

Bioapplications of CYP1A2

CYP1A2 is a super important enzyme in our bodies, especially when it comes to handling different substances like medications and dietary elements. It's the one that helps process caffeine, for instance, and plays a part in how other drugs are broken down, such as some asthma medications. Beyond that, it also tackles some environmental toxins, helping to neutralize them. Factors like what you eat—take broccoli, for example—can actually ramp up its activity. Plus, researchers are digging into its potential connections to cancer, looking at how it might activate or deactivate certain carcinogens. This enzyme is really a testament to how our bodies manage so many intricate and crucial processes.

Case Study 1: Zietek BM. et al. SLAS Discov. 2018

By testing how drugs interact with cytochrome P450 enzymes like CYP1A2 early on, researchers can reduce failures in drug development. The nanofractionation platform helps with this. Here's how: a metabolic mix is split via liquid chromatography (LC), analyzed in tiny fractions on a plate using mass spectrometry (MS), and tested for CYP1A2 inhibition. This method creates a bioactivity map, identifying inhibitors by matching bioassay peaks with MS data. It successfully identified five CYP1A2 inhibitors and effectively tested mixtures with potent inhibitors and ellipticine metabolites, achieving clear separation and accurate bioactivity correlation.

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  Fig1. Detection of potent inhibitors of CYP1A2 present in a mixture.
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  Fig2. Detection of CYP1A2 inhibitors present in a Phase I metabolic mixture of ellipticine.

Case Study 2: Hou C. et al. BMC Cancer. 2024

Circular RNA, or circRNAs, are important in colorectal cancer (CRC) development. However, the role of circ_0008345, transcribed by PTK2, isn't fully understood. In this study, researchers explored what circ_0008345 does in CRC. They confirmed circ_0008345's circular structure and found it mainly in the cytoplasm. It binds to miR-182-5p, which targets the CRC oncogene CYP1A2. Drop in circ_0008345 lowered colony formation, cell movement, and tumor growth in mice. However, these effects were reversed when miR-182-5p was also knocked down. They discovered that METTL3 modifies circ_0008345 with m6A, and lowering METTL3 drops circ_0008345 levels.

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  Fig3. The CYP1A2 expression in FHC, DLD1, and SW480 cells using immunoblotting.
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  Fig4. The mRNA expression of CYP1A2 in response to different infections by RT-qPCR.

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  Fig1. Main pathways and enzymes involved in caffeine degradation. (Jingjing Yu, 2024)
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  Fig2. Two-step metabolic activation of clopidogrel within the liver. (Frank A Plakogiannis, 2024)

CYP1A2 has several biochemical functions, for example, aromatase activity,caffeine oxidase activity,demethylase activity. Some of the functions are cooperated with other proteins, some of the functions could acted by CYP1A2 itself. We selected most functions CYP1A2 had, and list some proteins which have the same functions with CYP1A2. You can find most of the proteins on our site.

Function	Related Protein
demethylase activity	KDM1A,CYP3A41A,ALKBH4,CYP1A1,CYP3A41B
heme binding	CYP2AD2,PTGES2,HBAA,CYB5D2,HBG1,CYP1D1,CYP4V7,CYP2K18,CYP17A2,CBS
oxidoreductase activity	SUMF1,MOXD1L,DHRS13B,ALDH9A1B,CYP2AA12,DHRS13A.1,CYP2E1,CYP3A41B,CYP4F14,RDH13
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	CYP2AD6,CYP2K18,CYP2K19,CYP2X8,CYP2D9,CYP2F2,CYP1B1,CYP2F1,CYP2AA8,CYP2B19
caffeine oxidase activity	CYP2C39,CYP2C9,FAM84B,CYP2C38,CYP3A4
enzyme binding	TSPAN10,CCDC99,ZFP36,HIST1H2AG,HMOX1,APOA5,ABCD1,RPS2,HSPA5,USP22
monooxygenase activity	CYP2C37,MICAL2,CYP2D10,COQ6,TPH1B,CYP39A1,CYP2C55,MICAL2B,YWHAE1,CYP46A1.4
iron ion binding	PDF,HBG2,P4HA3,ACO2,CYP2B6,CYGB,CYP4A12A,CYP7A1A,HBA2,ISCU
aromatase activity	CYP2H1,CYP4B1,CYP2D6,CYP2U1,CYP2S1,CYP4A12A,CYP2C37,CYP3A5,CYP2J5,CYP3A25

CYP1A2 has direct interactions with proteins and molecules. Those interactions were detected by several methods such as yeast two hybrid, co-IP, pull-down and so on. We selected proteins and molecules interacted with CYP1A2 here. Most of them are supplied by our site. Hope this information will be useful for your research of CYP1A2.