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Inhibitors

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Empower Your Research: CD BioGlyco's Cutting-edge Inhibitors

The functions of cells are regulated by the kind of communication system known as a signal pathway, composed of a variety of proteins and other molecules, working together to perform basic functions such as growth, repair, or metabolism. Inhibitors are molecules that may interfere with the activity of a single or several components within an active signal pathway. They bind to the enzymes or proteins involved in these pathways and block, or change, signals released from them. Therefore, inhibitors provide invaluable tools for developing a flexible approach to understanding different types of disease.

Fig.1 The mechanisms of some inhibitors targeting the cancers. (Liu, et al., 2022)Fig.1 The mechanisms of some inhibitors targeting the cancers. (Liu, et al., 2022)

CD BioGlyco provides a wide range of inhibitors that are precisely tailored to meet the research needs of our clients. In-depth investigation of various research fields is facilitated by our variety of inhibitor products, including oncology, cardiovascular diseases, endocrinology, epigenetics, immunology, metabolic processes, neuroscience, and inflammatory responses. Our inhibitors are designed to attack specific pathways and mechanisms involved in the development of these diseases, addressing their limitations as compared to conventional approaches. These inhibitors are classified according to signaling pathways.

Fig.2 CD BioGlyco (https://unsplash.com/photos/a-close-up-of-a-double-strand-of-blue-plastic-7IieyeNYYFI)

Epigenetics

Inhibitors in the area of epigenetic research reveal not just fundamental gene regulation mechanisms, but also significant potential for developing novel therapeutic products.

  • HDAC
  • JAK
  • Aurora Kinase
  • Epigenetic Reader Domain
  • DNA Methyltransferase
  • Pim
  • Sirtuins
  • Histone Demethylase
  • Histone Acetyltransferase
  • Histone Methyltransferase
  • Protein Serine/Threonine Phosphatase
  • Protein Arginine Deiminase (PAD)
  • MicroRNA
  • PARP
  • Protein Arginine Methyltransferase
  • Protein Tyrosine Phosphatase
  • Methionine Adenosyltransferase (MAT)

Fig.3 CD BioGlyco (https://pixabay.com/illustrations/molecule-cell-biology-molecular-2082634/)

Apoptosis

Apoptosis, a type of programmed cell demise, is a natural occurrence in multicellular organisms. Apoptosis inhibitors are proteins that, in particular, inhibit the intrinsic pathway and interfere with programmed cell death.

  • Bcl-2 Family
  • Caspase
  • p53
  • TNF-α
  • IAP
  • MDM2
  • Apoptosis Inducers
  • Glutathione Peroxidase
  • DAPK
  • PERK
  • Survivin
  • RIP Kinase
  • ASK
  • c-Ret
  • Protein Kinase D (PKD)
  • Apoptosis Related
  • MIF
  • Oxidative Phosphorylation (OXPHOS)

Fig.4 CD BioGlyco (https://pixabay.com/vectors/cell-cell-nucleus-cytoblast-156402/)

PI3K/Akt/mTOR

The cellular quiescence, proliferation, cancer, and longevity are directly influenced by the PI3K/Akt/mTOR pathway, which is essential for regulating cell cycle regulation. PI3K/Akt/mTOR inhibitors target the PI3K/Akt/mTOR signaling axis, showing promise in attenuating chemotherapy resistance.

  • Akt
  • PI3K
  • mTOR
  • PDK1
  • DNA-PK
  • RSK
  • GSK-3
  • AMPK
  • MELK
  • ATM-ATR
  • PTEN
  • PI4K
  • PIN1

Fig.5 CD BioGlyco (https://commons.wikimedia.org/wiki/File:VEGF_receptors.png)

Protein Tyrosine Kinases

The protein tyrosine kinases, comprising a vast multigene family, are especially pertinent to numerous human diseases, notably cancer. They catalyze tyrosine phosphorylation by transferring phosphate from ATP to tyrosine residues on protein substrates. Tyrosine kinase inhibitors disrupt protein kinase signal transduction pathways through various modes of inhibition.

  • EGFR-HER2
  • FGFR
  • PDGFR
  • VEGFR
  • IGF-1R
  • FLT3
  • c-MET
  • ALK
  • Src
  • c-Kit
  • c-FMS
  • Tie-2
  • Tyrosine Kinase
  • Trk Receptor
  • CSF-1R
  • TAM Receptor
  • Ephrin Receptor
  • ITK
  • IRAK
  • DDR
  • Insulin Receptor

Fig.6 CD BioGlyco (https://unsplash.com/photos/pink-and-white-round-beads-kaOzojEliDE)

Angiogenesis

Angiogenesis, the physiological process of generation of new blood vessels from old ones, plays a role in development, muscle hypertrophy, menstrual cycles, pregnancy, and wounds but also contributes to disease. Angiogenesis inhibitors interfere with various steps in the development of blood vessels in several ways.

  • EGFR-HER2
  • FGFR
  • PDGFR
  • VEGFR
  • VDA
  • HIF
  • FLT3
  • ALK
  • BTK
  • FAK
  • Syk
  • Bcr-Abl
  • Antiangiogenics

Fig.7 CD BioGlyco (Novak, et al., 2023)

MAPK

In the transmission of signals within mammalian cells, MAPKs play an important role. The cellular functions such as proliferation, differentiation, growth, and survival are significantly influenced by this pathway. MAPK inhibitors with complex regulatory mechanisms have been extensively used in cancer research.

  • MEK
  • ERK
  • p38-MAPK
  • MNK
  • MAP4K
  • JNK-c-Jun
  • AP-1
  • KLF
  • MAPKAPK2 (MK2)
  • Raf
  • TOPK

Fig.8 CD BioGlyco (https://en.wikipedia.org/wiki/JAK-STAT_signaling_pathway#/media/File:Jakstat_pathway.svg)

JAK/Stat

Being pivotal in numerous essential cellular mechanisms, the JAK/STAT pathway serves as a swift membrane-to-nucleus signaling module, prompting the expression of pivotal mediators in cancer and inflammation. JAK/Stat inhibitors disrupt the phosphorylation of signal transducer and activator of Stat proteins.

  • JAK
  • Stat
  • Pim
  • EGFR-HER2

Fig.9 CD BioGlyco (Le Bourgeois, et al., 2018)

Metabolism

A metabolic pathway, a series of chemical reactions coordinated by specific enzymes, turns one chemical into another. Inhibitors direct the progression of pathways by preventing binding to enzyme substrate.

  • Cytochrome P450
  • PPAR
  • PDE
  • HSP
  • Hydroxylase
  • Factor Xa
  • MAO
  • DHFR
  • Dehydrogenases
  • Procollagen C-Proteinase
  • Carbonic Anhydrase
  • LXR
  • Decarboxylase
  • Hexokinase
  • Endogenous Metabolite
  • Adenosine Deaminase
  • Serine/Threonine Kinase
  • FAAH
  • 15-PGDH
  • CETP
  • Ferroptosis
  • HMG-CoA Reductase
  • FXR
  • Isocitrate Dehydrogenase (IDH)
  • IDO
  • Retinoid Receptor
  • Lipase
  • Phospholipase
  • Lipoxygenase
  • Stearoyl-CoA Desaturase (SCD)
  • PGC-1α
  • Mitochondrial Metabolism
  • SGK
  • AhR
  • NAMPT
  • GLUT
  • Antimetabolite
  • Lipid Metabolism
  • Neuronal Metabolism
  • SREBP
  • LDL
  • Foxo1
  • DGAT
  • Farnesyl Transferase
  • CRM1
  • Angiotensin Converting Enzyme (ACE)
  • Pyruvate Kinase
  • 11β-HSD
  • Thioredoxin
  • Vitamin
  • ACLY
  • Fatty Acid Synthase (FASN)
  • Glucokinase
  • Lactate Dehydrogenase A (LDHA)
  • Oxidative Phosphorylation
  • PFKFB3
  • Ribonucleotide Reductase
  • Acetyl-CoA Carboxylase
  • Glucosidase
  • PAI-1
  • Epoxide Hydrolase
  • Steroid Sulfatase (STS)
  • Xanthine Oxidase
  • Drug Metabolite

Fig.10 CD BioGlyco (Soni and Bacete, 2023).

Cell Cycle

Cell cycle inhibitors, by inhibiting the progression of the cell cycle through various mechanisms that induce an arrest at different stages and reduce both division rates and a number of active cells, interfere with cellular cycles.

  • Chk
  • CDK
  • Aurora Kinase
  • RAD51
  • PLK
  • ROCK
  • c-Myc
  • LIM Kinase (LIMK)
  • BMI-1
  • APC
  • Wee1
  • ATF6
  • Ras
  • DYRK
  • G-quadruplex
  • Nur77

Fig.11 CD BioGlyco (https://unsplash.com/photos/a-close-up-of-a-blue-and-purple-structure-8o_LkMpo8ug).

DNA Damage

DNA damage plays a pivotal role in the mechanisms underlying aging and disease, spanning from birth defects and cancer to premature aging syndromes and specific neurological disorders. DNA damage inhibitors halt the growth and division of cancers with DNA repair defects.

  • HDAC
  • PARP
  • DNA-PK
  • Topoisomerase
  • Telomerase
  • ATM/ATR
  • DNA/RNA Synthesis
  • RNA/DNA Polymerase
  • PARG
  • Antifolate
  • DNA Alkylator
  • Synthases/Synthetase
  • MTH1
  • Sirtuins
  • IRE1
  • DNA Stain
  • DNA
  • Nucleoside Antimetabolite/Analog
  • Eukaryotic Initiation Factor (eIF)

Fig.12 CD BioGlyco (https://bioicons.com/icons/cc-by-3.0/Cell_membrane/Servier/emptycell-quarteroval-membrane-red.svg)

Cytoskeletal Signaling

Mechanical support needed for cellular functions such as division and movement is also provided by the cytoskeleton, which plays an essential role in keeping cells shaped and organization. Abnormalities in the cytoskeleton, crucial for cellular processes, often lead to disease. Cytoskeletal inhibitors are small compounds that interact with either actin or tubulin.

  • Microtubule/Tubulin
  • PAK
  • Dynamin
  • Integrin
  • Kinesin
  • Mps1
  • Gap Junction Protein
  • MLCK
  • Myosin

Fig.13 CD BioGlyco (https://bioicons.com/icons/cc-by-3.0/Cell_membrane/Servier/endocytosis.svg)

Autophagy Signaling

Autophagy, an intracellular degradation system transporting cytoplasmic components to lysosomes, encompasses diverse physiological and pathophysiological roles, occasionally intricate. Autophagy inhibitors inhibit activity of autophagy and offer a way to regulate and study the function of autophagy in both cells and organisms.

  • Autophagy
  • LRRK2
  • CXCR
  • Mitophagy
  • Atg4

Fig.14 CD BioGlyco (https://bioicons.com/icons/cc-by-3.0/Blood_Immunology/Servier/acidophil-erythroblast.svg)

Immunology & Inflammation

The inflammatory response is pivotal in immunity, triggering tissue damage and mobilizing the immune system. Immunology & inflammation inhibitors are used to dampen the immune system's reaction to damage, thereby lessening inflammation.

  • IL Receptor
  • COX
  • CCR
  • Toll-like Receptor
  • CXCR
  • ROS
  • NOS
  • Keap1-Nrf2
  • STING
  • NFAT
  • Complement System
  • Immunosuppressants
  • Thrombopoietin Receptor (TPO)
  • MALT
  • PD-1-PD-L1
  • NADPH Oxidase
  • PGE Synthase
  • Arginase
  • Salt-inducible Kinase (SIK)
  • Immunology & Inflammation Related
  • IFNAR
  • NOD-like Receptor (NLR)
  • FKBP
  • CD Markers
  • Galectin
  • cGAS
  • LTR

Fig.15 CD BioGlyco (https://en.wikipedia.org/wiki/G_protein-coupled_receptor#/media/File:PDB_1hzx_7TM_Sketch_Membrane.png)

GPCR/G Protein

GPCRs are the largest group of membrane receptors in eukaryotes with a wide variety of functions, such as cell gates for various signals. These signals provide vital information about the presence or absence of basic resources and cellular communications in a cell's environment. GPCR/G inhibitors intervene in the function of G protein-coupled receptors in various ways, such as blocking the binding of receptors to ligands.

  • 5-HT Receptor
  • Dopamine Receptor
  • Opioid Receptor
  • mGluR
  • Melatonin Receptor
  • Smoothened Receptor
  • CXCR
  • MCHR1 (GPR24)
  • Formyl Peptide Receptor (FPR)
  • Melanocortin Receptor
  • GRK
  • G Protein
  • Platelet-Activating Factor (PAF) Receptor
  • Endothelin Receptor
  • LPA Receptor
  • Prostanoid Receptor
  • Vasopressin Receptor
  • Peptide Receptor
  • Adrenergic Receptor
  • Adenosine Receptor
  • Cannabinoid Receptor
  • Neurotensin Receptor
  • Orexin Receptor
  • Somatostatin Receptor
  • Adenylyl Cyclase
  • Thyrotropin receptor (TSHR)
  • Neurokinin Receptor
  • Protease-activated Receptor (PAR)
  • S1P Receptor
  • CGRP Receptor
  • Sigma Receptor
  • Oxytocin Receptor
  • Guanylate Cyclase
  • cAMP
  • Urotensin Receptor
  • Bradykinin Receptor
  • Histamine Receptor
  • Rev-Erb Receptors
  • NPY Receptor
  • RGS Protein
  • GHSR
  • Bombesin Receptor
  • Imidazoline Receptor
  • CCK
  • GLP-1 Receptor
  • Calcium-sensing Receptor
  • GPCR19
  • CRFR
  • Angiotensin Receptor
  • Bradykinin Receptor
  • MRGPR
  • FFAR
  • Leukotriene Receptor
  • Glucagon Receptor

Fig 16 CD BioGlyco (https://en.wikipedia.org/wiki/NF-%CE%BAB#/media/File:NFKB_mechanism_of_action.png)

NF-kB/IkB

In response to a variety of stimuli, such as stress, infection, and toxins, NF-kB/IkB ligand complexes regulate DNA transcription, cytokine production, and cellular survival. Dysregulation of NF-kB/IkB is associated with cancer, inflammatory diseases, viral infections, and immune disorders, and it also influences synaptic plasticity and memory processes. We have numerous NF-kB/IkB pathway inhibitors that can be researched for many types of disorders.

  • NF-κB
  • IKK/IκB
  • HDAC

Fig 17 CD BioGlyco (https://en.wikipedia.org/wiki/Transforming_growth_factor_beta)

TGF-β/Smad

The TGF-β superfamily signaling pathway regulates cell growth, differentiation, and development through ligand-induced receptor kinase oligomerization and subsequent phosphorylation of Smad proteins. TGF-β/Smad inhibitors intervene in the TGF-β signaling pathway in several ways, including inhibiting the production of TGF-β, its activity, the interaction between TGF-β ligands and their receptors, or the kinase activity of the TGF-β receptor.

  • TGF-β-Smad Inhibitor
  • Protein Kinase C (PKC)
  • Protein Kinase A (PKA)
  • ROCK

Fig.18 CD BioGlyco (https://pixabay.com/illustrations/brain-network-digital-web-neurons-5814971/)

Neuronal Signaling

In addition to its structure, function, and genetic and physiological functions, neuronal signal regulates the functioning of the central nervous system to understand neurological disorders. In the central nervous system (CNS), neurons and glia play an important role in information processing because of their different capacities for intracellular and intracellular signaling. Inhibitors that target neuronal signaling, can be studied for various CNS disorders.

  • β-Amyloid
  • γ-Secretase
  • Beta-secretase (BACE)
  • COX
  • GABA Receptor
  • NMDA Receptor
  • CaMK
  • AAK1
  • AChE
  • mAChR
  • nAChR
  • P2X Receptor
  • Purinergic (P2Y) Receptor
  • GlyT
  • Catechol-O-methyltransferase (COMT)
  • Glucosylceramide Synthase

Fig.19 CD BioGlyco (Kumar, et al., 2016)

Proteases

Proteases, also known as peptidases, hydrolyze peptide bonds in proteins and regulate other proteases directly through cleavage. Protease inhibitors are preventing polyproteins from breaking down into functional proteins.

  • Caspase
  • γ-Secretase
  • Proteasome
  • HCV Protease
  • Microsomal Triglyceride Transfer Protein (MTP)
  • Thrombin
  • MMP
  • Urokinase
  • HIV Protease
  • DPP-4
  • Cysteine Protease
  • Serine Protease
  • Tyrosinase
  • Carboxypeptidase
  • Glutaminase
  • Elastases
  • ADAMs
  • Aminopeptidase
  • Aldose Reductase
  • NEDD8-activating Enzyme (NAE)
  • Neprilysin
  • FABP
  • Phosphatase
  • Nek2
  • Ketohexokinase (KHK)
  • Acetolactate Synthase (ALS)

Fig 20 CD BioGlyco (https://unsplash.com/photos/a-pile-of-small-purple-objects-gP9d3iWlELo)

Microbiology

Microbiology inhibitors are substances or compounds that target specific processes or components involved in the growth, replication, or spread of microorganisms or viruses.

  • Reverse Transcriptase
  • HIV Integrase
  • HCV Protease
  • HIV Protease
  • CCR
  • Antifection
  • HBV
  • HSV
  • RSV
  • SARS-CoV
  • Parasite
  • Enterovirus
  • Influenza Virus
  • β-Lactamase

Fig 21 CD BioGlyco (https://en.wikipedia.org/wiki/Embryonic_stem_cell)

Stem Cells/Wnt

Wnt signaling is implicated in regulating various stem cell types and potentially serves as a niche factor to sustain stem cells in a state of self-renewal. Stem cell/Wnt inhibitors target and suppress stem cell activity, particularly in cancer, potentially hindering tumor growth and recurrence.

  • Hedgehog
  • Wnt
  • β-Catenin
  • Casein Kinase
  • Smoothened
  • GSK-3
  • Hippo
  • γ-Secretase
  • Notch
  • YAP
  • PKG

Fig.22 CD BioGlyco (https://en.wikipedia.org/wiki/Membrane_transport_protein#/media/File:Scheme_sodium-potassium_pump-en.svg)

Membrane Transporters-Ion Channels

In order to transport nutrients into organisms and cells, remove toxic compounds and waste from the body as well as regulate excitability in the nervous system, membrane transporters, and ion channels are vital. Membrane transporters-ion channel inhibitors disrupt the function of membrane proteins involved in the movement of ions and molecules across biological membranes.

  • ATPase
  • CFTR
  • Calcium Channel
  • Sodium Channel
  • Potassium Channel
  • Chloride Channels
  • SGLT
  • Monocarboxylate Transporters (MCT)
  • AMPA Receptor
  • P-gp
  • CRM1
  • Piezo Channel
  • VDAC
  • ASBT
  • OAT
  • TRP Channel
  • TRPV
  • Glutamate (EAAT) Transporter
  • Serotonin Transporter
  • Proton Pump
  • OCT
  • NCX
  • BCRP
  • MRP
  • Na+-H+ Exchanger
  • Monoamine Transporter
  • HCN Channel
  • Aquaporin
  • Amino Acid Transporter

Fig.23 CD BioGlyco (https://en.wikipedia.org/wiki/Growth_hormone#/media/File:Somatotropine.GIF)

Endocrinology-Hormones

The endocrine system comprises a complex network of glands tasked with the intricate process of producing and secreting hormones, pivotal for orchestrating a myriad of functions across the body's systems and organs. Endocrinology-hormone inhibitors interfere with hormone function or secretion within the endocrine system, potentially impacting a range of physiological processes governed by hormonal activity.

  • Estrogen Receptor
  • Progesterone Receptor
  • Androgen Receptor
  • GPR
  • Glucocorticoid Receptor
  • Vitamin D Receptor
  • GnRH Receptor
  • 5-Alpha-reductase
  • Pregnane X Receptor
  • Renin-angiotensin-aldosterone System (RAAS)
  • Aromatase
  • ROR
  • Apelin Receptor
  • Mineralocorticoid Receptor

Fig.24 CD BioGlyco (https://en.wikipedia.org/wiki/Transferase#/media/File:Alpha-Amanitin%E2%80%93RNA_polymerase_II_complex_1K83.png)

Transferases

Transferase inhibitors inhibit the activity of transferase enzymes, which are responsible for transferring functional groups from one molecule to another.

  • Acyltransferase
  • Phosphorylase
  • Protein Prenyltransferase
  • SphK
  • Gutathione S-Transferase

Fig.25 CD BioGlyco (Dougherty, et al., 2020)

Ubiquitin

The ubiquitin system is crucial for maintaining protein balance and regulating proteins involved in various pathways like DNA repair, cell cycle, and signal transduction. When this system malfunctions, it can lead to diseases. Ubiquitin inhibitors block the process of ubiquitination, potentially preventing the attachment of ubiquitin to target proteins and interfering with various cellular processes regulated by ubiquitin-mediated signaling pathways.

  • E1 Activating
  • E2 Conjugating
  • E3 Ligase
  • DUB
  • p97

Fig.26 CD BioGlyco (https://en.wikipedia.org/wiki/Proteolysis_targeting_chimera)

PROTAC

PROTAC, a heterobi functional compound that consists of two active domains connected, is able to eliminate certain undesired proteins. PROTAC inhibitors function by inducing targeted intracellular proteolysis, unlike traditional inhibitors of enzymes.

  • E3 Ligase Ligand-linker Conjugate
  • E3 Ligase Ligand
  • PROTAC Degrader
  • PROTAC Linker
  • Ligand for Target Protein for PROTAC
  • Molecular Glues
  • SNIPERs

Advantages

  • We continuously strive to innovate, by using our expertise and dedication to innovation.
  • We continuously learn to ensure that we are staying at the forefront of inhibitor research and development.
  • We are committed to providing cutting-edge solutions to propel the development of inhibitors.

With a focus on inhibitors, a cornerstone of modern targeted therapeutic research, CD BioGlyco also provides Glycosylation Inhibitor Development. If you are interested in our inhibitor products, please contact us.

References

  1. Liu, G.H.; et al. Small molecule inhibitors targeting the cancers. MedComm. 2022, 3(4): e181.
  2. https://commons.wikimedia.org/wiki/File:VEGF_receptors.png
  3. Novak, L.; et al. Mutation in the common docking domain affects MAP kinase ERK2 catalysis and stability. Cancers. 2023, 15: 2938.
  4. https://en.wikipedia.org/wiki/JAK-STAT_signaling_pathway#/media/File:Jakstat_pathway.svg
  5. Le Bourgeois, T.; et al. Targeting T cell metabolism for improvement of cancer immunotherapy. Frontiers in oncology. 2018, 8: 237.
  6. Soni, N.; Bacete, L. The interplay between cell wall integrity and cell cycle progression in plants. Plant Molecular Biology. 2023, 113(6): 367-382.
  7. https://en.wikipedia.org/wiki/G_protein-coupled_receptor#/media/File:PDB_1hzx_7TM_Sketch_Membrane.png
  8. https://en.wikipedia.org/wiki/NF-%CE%BAB#/media/File:NFKB_mechanism_of_action.png
  9. https://en.wikipedia.org/wiki/Transforming_growth_factor_beta
  10. Kumar, P.; et al. Substrate complexes of human dipeptidyl peptidase III reveal the mechanism of enzyme inhibition. Scientific reports. 2016, 6(1): 23787.
  11. https://en.wikipedia.org/wiki/Embryonic_stem_cell
  12. https://en.wikipedia.org/wiki/Membrane_transport_protein#/media/File:Scheme_sodium-potassium_pump-en.svg
  13. https://en.wikipedia.org/wiki/Growth_hormone#/media/File:Somatotropine.GIF
  14. https://en.wikipedia.org/wiki/Transferase#/media/File:Alpha-Amanitin%E2%80%93RNA_polymerase_II_complex_1K83.png
  15. Dougherty, S.E.; et al. Expanding role of ubiquitin in translational control. International journal of molecular sciences. 2020, 21(3): 1151.
  16. https://en.wikipedia.org/wiki/Proteolysis_targeting_chimera

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