GLPBio

Apoptosis

Read More about this category

As one of the cellular death mechanisms, apoptosis, also known as programmed cell death, can be defined as the process of a proper death of any cell under certain or necessary conditions. Apoptosis is controlled by the interactions between several molecules and responsible for the elimination of unwanted cells from the body.

Many biochemical events and a series of morphological changes occur at the early stage and increasingly continue till the end of apoptosis process. Morphological event cascade including cytoplasmic filament aggregation, nuclear condensation, cellular fragmentation, and plasma membrane blebbing finally results in the formation of apoptotic bodies. Several biochemical changes such as protein modifications/degradations, DNA and chromatin deteriorations, and synthesis of cell surface markers form morphological process during apoptosis.

Apoptosis can be stimulated by two different pathways: (1) intrinsic pathway (or mitochondria pathway) that mainly occurs via release of cytochrome c from the mitochondria and (2) extrinsic pathway when Fas death receptor is activated by a signal coming from the outside of the cell.

Different gene families such as caspases, inhibitor of apoptosis proteins, B cell lymphoma (Bcl)-2 family, tumor necrosis factor (TNF) receptor gene superfamily, or p53 gene are involved and/or collaborate in the process of apoptosis.

Caspase family comprises conserved cysteine aspartic-specific proteases, and members of caspase family are considerably crucial in the regulation of apoptosis. There are 14 different caspases in mammals, and they are basically classified as the initiators including caspase-2, -8, -9, and -10; and the effectors including caspase-3, -6, -7, and -14; and also the cytokine activators including caspase-1, -4, -5, -11, -12, and -13. In vertebrates, caspase-dependent apoptosis occurs through two main interconnected pathways which are intrinsic and extrinsic pathways. The intrinsic or mitochondrial apoptosis pathway can be activated through various cellular stresses that lead to cytochrome c release from the mitochondria and the formation of the apoptosome, comprised of APAF1, cytochrome c, ATP, and caspase-9, resulting in the activation of caspase-9. Active caspase-9 then initiates apoptosis by cleaving and thereby activating executioner caspases. The extrinsic apoptosis pathway is activated through the binding of a ligand to a death receptor, which in turn leads, with the help of the adapter proteins (FADD/TRADD), to recruitment, dimerization, and activation of caspase-8 (or 10). Active caspase-8 (or 10) then either initiates apoptosis directly by cleaving and thereby activating executioner caspase (-3, -6, -7), or activates the intrinsic apoptotic pathway through cleavage of BID to induce efficient cell death. In a heat shock-induced death, caspase-2 induces apoptosis via cleavage of Bid.

Bcl-2 family members are divided into three subfamilies including (i) pro-survival subfamily members (Bcl-2, Bcl-xl, Bcl-W, MCL1, and BFL1/A1), (ii) BH3-only subfamily members (Bad, Bim, Noxa, and Puma9), and (iii) pro-apoptotic mediator subfamily members (Bax and Bak). Following activation of the intrinsic pathway by cellular stress, pro‑apoptotic BCL‑2 homology 3 (BH3)‑only proteins inhibit the anti‑apoptotic proteins Bcl‑2, Bcl-xl, Bcl‑W and MCL1. The subsequent activation and oligomerization of the Bak and Bax result in mitochondrial outer membrane permeabilization (MOMP). This results in the release of cytochrome c and SMAC from the mitochondria. Cytochrome c forms a complex with caspase-9 and APAF1, which leads to the activation of caspase-9. Caspase-9 then activates caspase-3 and caspase-7, resulting in cell death. Inhibition of this process by anti‑apoptotic Bcl‑2 proteins occurs via sequestration of pro‑apoptotic proteins through binding to their BH3 motifs.

One of the most important ways of triggering apoptosis is mediated through death receptors (DRs), which are classified in TNF superfamily. There exist six DRs: DR1 (also called TNFR1); DR2 (also called Fas); DR3, to which VEGI binds; DR4 and DR5, to which TRAIL binds; and DR6, no ligand has yet been identified that binds to DR6. The induction of apoptosis by TNF ligands is initiated by binding to their specific DRs, such as TNFα/TNFR1, FasL /Fas (CD95, DR2), TRAIL (Apo2L)/DR4 (TRAIL-R1) or DR5 (TRAIL-R2). When TNF-α binds to TNFR1, it recruits a protein called TNFR-associated death domain (TRADD) through its death domain (DD). TRADD then recruits a protein called Fas-associated protein with death domain (FADD), which then sequentially activates caspase-8 and caspase-3, and thus apoptosis. Alternatively, TNF-α can activate mitochondria to sequentially release ROS, cytochrome c, and Bax, leading to activation of caspase-9 and caspase-3 and thus apoptosis. Some of the miRNAs can inhibit apoptosis by targeting the death-receptor pathway including miR-21, miR-24, and miR-200c.

p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.

Some inhibitors of apoptosis proteins (IAPs) can inhibit apoptosis indirectly (such as cIAP1/BIRC2, cIAP2/BIRC3) or inhibit caspase directly, such as XIAP/BIRC4 (inhibits caspase-3, -7, -9), and Bruce/BIRC6 (inhibits caspase-3, -6, -7, -8, -9). 

Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases and malignancies especially cancer.

 

References:

1.Yağmur Kiraz, Aysun Adan, Melis Kartal Yandim, et al. Major apoptotic mechanisms and genes involved in apoptosis[J]. Tumor Biology, 2016, 37(7):8471.

2.Aggarwal B B, Gupta S C, Kim J H. Historical perspectives on tumor necrosis factor and its superfamily: 25 years later, a golden journey.[J]. Blood, 2012, 119(3):651.

3.Ashkenazi A, Fairbrother W J, Leverson J D, et al. From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors[J]. Nature Reviews Drug Discovery, 2017.

4.McIlwain D R, Berger T, Mak T W. Caspase functions in cell death and disease[J]. Cold Spring Harbor perspectives in biology, 2013, 5(4): a008656.

5.Ola M S, Nawaz M, Ahsan H. Role of Bcl-2 family proteins and caspases in the regulation of apoptosis[J]. Molecular and cellular biochemistry, 2011, 351(1-2): 41-58.

Research Areas

Products Related to Apoptosis(3394)

  • GC73491 structure
    GC73491RapaBlock
    CAS: 2474076-02-1
    Purity: >98.00%

    RapaBlock ist ein potenter, nicht immunsuppressiver und hirndurchlässiger FKBP12-Ligand.

  • GC73501 structure
    GC73501Wu-5
    CAS: 2630378-05-9
    Purity: >98.00%

    Wu-5 ist ein USP10-Inhibitor, der FLT3- und AMPK-Signalwege hemmen, FLT3-ITD-Abbau induzieren und Apoptose induzieren kann.

  • GC73541 structure
    GC73541PRMT5-IN-31
    Purity: >99.00%

    PRMT5-IN-31 (Verbindung 3m) ist ein selektiver PRMT5-Hemmer (IC50: 0,31 μM).

  • GC73543 structure
    GC73543FC-116
    CAS: 2417298-29-2
    Purity: >98.00%

    FC-116 ist ein Tubulin-Inhibitor, der das Tumorwachstum bei Mäusen wirksam hemmt.

  • GC73546 structure
    GC73546PD-L1-IN-3
    CAS: 2953044-29-4
    Purity: >99.00%

    PD-L1-IN-3 (Verbindung 4a) ist eine Verbindung, die auf PD-1/PD-L1 abzielt, der IC50-Wert und der EC50-Wert beträgt 4.97nM und 2.70 μM für die Inhibition von PD-L1- und Jurkat-T-Zellen.

  • GC73549 structure
    GC73549LSD1-IN-27
    CAS: 2904571-94-2
    Purity: >98.00%

    LSD1-IN-27 (Verbindung 5Ac) ist ein LSD1-Hemmer (IC50: 13 nM).

  • GC73555 structure
    GC73555PI3Kδ-IN-16
    CAS: 2766437-35-6
    Purity: >99.00%

    PI3Kδ-IN-16 ist ein starker und selektiver Inhibitor von PI3Kδ.

  • GC73561 structure
    GC73561YS-363
    CAS: 2470908-90-6
    Purity: >99.00%

    YS-363 ist ein potenter, selektiver und oral aktiver EGFR-Inhibitor mit IC50s von 0,96 nM und 0,67 nM für Wildtyp- bzw. L858R-Mutantenformen von EGFR.

  • GC73567 structure
    GC73567Os30
    CAS: 2998928-68-8
    Purity: >98.00%

    Os30, ein potenter EGFR-Hemmer der vierten Generation, ist ein potenter EGFRC797S-TK-Hemmer mit IC50-Werten von 18 nM und 113 nM für EGFRDel19/T790M/C797S TK bzw. EGFRL858R/T790M/C797S TK.

  • GC73569 structure
    GC73569MY-1076
    CAS: 3008262-76-5
    Purity: >99.00%

    MY-1076 ist ein YAP-Hemmer.

  • GC73571 structure
    GC73571Tubulin polymerization-IN-56
    CAS: 2966790-98-5
    Purity: >99.00%

    Tubulin polymerization-IN-56, ein Indazol-Derivat, ist ein starker Tubulin-Polymerisationshemmer durch Wechselwirkung mit der Colchicinstelle, was zu Zellzyklusarrest und Zellapoptose führt.

  • GC73572 structure
    GC73572PP5-IN-1
    CAS: 1022417-69-1
    Purity: >99.00%

    PP5-IN-1 (Verbindung P053) ist ein kompetitiver Inhibitor von Serin/Threonin Protein Phosphatase-5 (PP5), der an seine katalytische Domäne bindet und Apoptose bei Nierenkrebs verursacht.

  • GC73579 structure
    GC73579DDO-2728
    CAS: 3029515-97-4
    Purity: >98.50%

    DDO-2728 (Verbindung 19) ist ein selektiver AlkB homologer 5 (ALKBH5)-Inhibitor mit einem IC50 von 2,97 μM.

  • GC73585 structure
    GC73585(Rac)-M826
    CAS: 2649883-37-2

    (Rac)-M826 ist der Racemate von M826.

  • GC73594 structure
    GC73594KH16
    Purity: >98.00%

    KH16 ist ein potenter und niedrig nanomolarer HDAC-Inhibitor.

  • GC73599 structure
    GC73599TH9619
    CAS: 2379556-22-4
    Purity: >99.00%

    TH9619 ist ein starker Inhibitor der Dedrogenase- und Cyclodrolase-Aktivitäten sowohl in MTHFD1 als auch in MTHFD2 mit einem IC50-Wert von 47 nM und tötet gezielt Krebszellen ab.

  • GC73601 structure
    GC73601UCM-1336
    CAS: 1621535-90-7
    Purity: >99.00%

    UCM-1336 ist ein starker ICMT-Inhibitor mit einem IC50 von 2 μM.

  • GC73604 structure
    GC73604MeOIstPyrd
    CAS: 2308548-54-9
    Purity: >99.00%

    MeOIstPyrd ist ein Anti-Hautkrebsmittel.

  • GC73619 structure
    GC73619M190S
    CAS: 2578300-07-7
    Purity: >99.00%

    M190S ist ein neuartiges kleines Molekül, das Zellen sowohl in vitro als auch in vivo vor mitochondrienabhängiger Apoptose schützt.

  • GC73627 structure
    GC73627HDAC/JAK/BRD4-IN-1
    CAS: 2755325-84-7
    Purity: >95.00%

    HDAC/JAK/BRD4-IN-1(Verbindung 25ap) ist ein starker HDAC/JAK/BRD4 Triple Inhibitor.

  • GC73629 structure
    GC73629FB49
    CAS: 3074495-82-9
    Purity: >98.50%

    FB49 ist ein hochselektiver Inhibitor von Bcl-2-assoziiertem Athanogen 3 (BAG3), mit dem Ki von 45 μM.

  • GC73630 structure
    GC73630ZZM-1220
    Purity: >98.00%

    ZZM-1220 ist ein kovalenter Histon-Lysin-Metltransferase-G9a/GLP-Inhibitor mit IC50s von 458 nM bzw. 924 nM.

  • GC73631 structure
    GC73631FPR1 antagonist 1
    Purity: >95.00%

    FPR1 antagonist 1 (Verbindung 24a) ist ein Formylpeptid-Rezeptor-1 (FPR1)-Antagonist mit einem IC50 von 25 nM.

  • GC73632 structure
    GC73632NSC 48160
    CAS: 6640-90-0
    Purity: >99.00%

    NSC 48160 hemmt das Wachstum der Bauchspeicheldrüsenkrebszellen mit IC50s von 84,3 μM für CPFAC-1 und 94,5 μM für BxPC-3.