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)

  • GC64127 structure
    GC64127Xylopine
    CAS: 517-71-5
    Purity: >98.00%

    La xylopine est un alcaloÏde aporphine ayant une activité cytotoxique sur les cellules cancéreuses. La xylopine induit un stress oxydatif, provoque l'arrêt du cycle cellulaire G2/M et l'apoptose des cellules cancéreuses.

  • GC64139 structure
    GC64139Dibromoacetic acid
    CAS: 631-64-1
    Purity: >98.00%
  • GC64223 structure
    GC64223Sophocarpine monohydrate
    CAS: 145572-44-7
    Purity: >98.00%

    La sophocarpine (monohydrate) est l'un des alcaloÏdes importants extraits de la plante médicinale traditionnelle Sophora flavescens qui possède de nombreuses propriétés pharmacologiques telles qu'anti-virus, anti-tumorale, anti-inflammatoire.

  • GC64303 structure
    GC64303S2116
    CAS: 2262489-89-2
    Purity: >98.00%

    Le S2116, un dérivé N-alkylé de la tranylcypromine (TCP), est un puissant inhibiteur de la déméthylase 1 spécifique de la lysine (LSD1). S2116 augmente la méthylation de H3K9 et la désacétylation réciproque de H3K27 dans les régions super-enhancer. S2116 induit l'apoptose dans les cellules de leucémie lymphoblastique aiguë À cellules T résistantes au TCP (T-ALL) en réprimant la transcription des gènes NOTCH3 et TAL1. S2116 retarde significativement la croissance des cellules T-ALL chez les souris xénogreffées.

  • GC64325 structure
    GC64325Ligustilide
    CAS: 4431-01-0
    Purity: >98.00%

    Ligustilide est un dérivé de phtalide bioactif isolé d'Angelica sinensis et de Chuanxiong.

  • GC64331 structure
    GC64331Ritonavir-13C,d3
    CAS: 155213-67-5
    Purity: >98.00%
  • GC64352 structure
    GC64352L-Glutamic acid-15N
    CAS: 21160-87-2
    Purity: >98.00%
  • GC64354 structure
    GC64354Bendamustine
    CAS: 16506-27-7
    Purity: >98.00%

    La bendamustine (base libre SDX-105), un analogue purique, est un agent de réticulation de l'ADN. La bendamustine active la réponse au stress et l'apoptose des dommages À l'ADN. La bendamustine possède de puissantes propriétés alkylantes, anticancéreuses et antimétabolites.

  • GC64370 structure
    GC64370Kongensin A
    CAS: 885315-96-8
    Purity: >98.00%

    Kongensin A est un produit naturel isolé de Croton kongensis.

  • GC64373 structure
    GC64373Tezacitabine
    CAS: 130306-02-4
    Purity: >99.00%

    La tézacitabine est un antimétabolite cytostatique et cytotoxique et un analogue nucléosidique. La tézacitabine inhibe de manière irréversible la ribonucléotide réductase et interfère avec la réplication et la réparation de l'ADN. La tézacitabine induit efficacement l'apoptose des cellules. La tézacitabine a le potentiel de traiter les leucémies et les tumeurs solides (carcinomes).

  • GC64375 structure
    GC64375Difopein TFA
    Purity: >94.00%

    Difopéine (TFA), un inhibiteur spécifique et compétitif de la protéine 14-3-3 (une molécule régulatrice eucaryote hautement conservée), bloquant la capacité du 14-3-3 À se lier aux protéines cibles et inhibe les interactions 14-3-3/Ligand . La difopéine (TFA) conduit À l'induction de l'apoptose et améliore la capacité du cisplatine À tuer les cellules.

  • GC64467 structure
    GC64467Lisaftoclax
    CAS: 2180923-05-9
    Purity: >98.00%

    Le lisaftoclax (composé 6) est un double inhibiteur Bcl-2 et Bcl-xl À activité anti-tumorale, extrait du brevet WO2018027097A1. Lisaftoclax présente des valeurs IC50 de 2 nM et 5,9 nM pour Bcl-2 et Bcl-xl, respectivement.

  • GC64485 structure
    GC64485HXR9 hydrochloride
    Purity: >99.00%

    Le chlorhydrate de HXR9 est un peptide perméable aux cellules et un antagoniste compétitif de l'interaction HOX/PBX. Le chlorhydrate de HXR9 antagonise l'interaction entre HOX et un second facteur de transcription (PBX), qui se lie aux protéines HOX dans les groupes paralogues 1 À 8. Le chlorhydrate de HXR9 diminue sélectivement la prolifération cellulaire et favorise l'apoptose dans les cellules avec un niveau élevé d'expression du HOXA/ Gènes PBX3, tels que les cellules leucémiques réarrangées MLL.

  • GC64561 structure
    GC64561Toripalimab
    CAS: 1924598-82-2
    Purity: >97.00%

    Toripalimab est un anticorps monoclonal humanisé recombinant anti-PD-1.

  • GC64619 structure
    GC64619β-Ionone
    CAS: 14901-07-6
    Purity: >99.00%

    β-Ionone est efficace dans l'induction de l'apoptose dans les cellules d'adénocarcinome gastrique SGC7901. Activité anticancéreuse.

  • GC64645 structure
    GC64645Sappanchalcone
    CAS: 94344-54-4
    Purity: >99.00%

    La sappanchalcone, un flavonoÏde isolé de Caesalpinia sappan L., induit une apoptose dépendante de la caspase et dépendante de l'AIF dans les cellules cancéreuses du cÔlon humain.

  • GC64649 structure
    GC64649Cjoc42
    CAS: 2171519-89-2
    Purity: >98.00%

    Cjoc42 est un composé capable de se lier À la gankyrine. Cjoc42 inhibe l'activité de la gankyrine de manière dose-dépendante. Cjoc42 empêche la diminution des niveaux de protéine p53 normalement associée À des quantités élevées de gankyrine. Cjoc42 restaure la transcription dépendante de p53 et la sensibilité aux dommages À l'ADN.

  • GC64662 structure
    GC64662Helichrysetin
    CAS: 62014-87-3
    Purity: >99.00%

    L'hélichrysétine, isolée des fleurs d'Helichrysum odoratissimum, est un inhibiteur ID2 (inhibiteur de la liaison À l'ADN 2) et supprime la formation de CCIS (carcinome canalaire in situ). L'hélichrysétine possède de puissants effets inhibiteurs sur la croissance cellulaire et est capable d'induire l'apoptose des cellules A549.

  • GC64674 structure
    GC64674ABBV-167
    CAS: 1351456-78-4
    Purity: >98.00%

    ABBV-167 est un promédicament phosphate du vénétoclax inhibiteur de BCL-2.

  • GC64726 structure
    GC6472610-Formyl-5,8-dideazafolic acid
    CAS: 61038-31-1
    Purity: >96.00%

    L'acide 10-formyl-5,8-didéazafolique est un inhibiteur de la thymidylate synthase.

  • GC64762 structure
    GC647623,6-Dihydroxyflavone
    CAS: 108238-41-1
    Purity: >98.00%

    La 3,6-dihydroxyflavone est un agent anticancéreux. La 3,6-dihydroxyflavone diminue en fonction de la dose et du temps la viabilité cellulaire et induit l'apoptose en activant la cascade de caspases, en clivant la poly (ADP-ribose) polymérase (PARP). La 3,6-dihydroxyflavone augmente le stress oxydatif intracellulaire et la peroxydation lipidique.

  • GC64767 structure
    GC64767ISIS 104838
    CAS: 250755-32-9
    Purity: >98.00%

    ISIS104838est un médicament oligonucléotidique antisens qui réduit la production de facteur de nécrose tumorale (TNF-alpha),une substance qui contribue À la douleur et À l'enflure des articulations dans la polyarthrite rhumatoÏde.

  • GC64768 structure
    GC64768PK9327
    CAS: 2413987-20-7
    Purity: >98.00%

    Le PK9327 est un stabilisateur À petite molécule ciblant les mutations cancéreuses p53 créant des cavités.

  • GC64786 structure
    GC64786Hellebrigenin
    CAS: 465-90-7
    Purity: >98.00%

    L'hellebrigénine, l'un des bufadienolides appartenant aux stéroÏdes cardioactifs, est isolée de la médecine traditionnelle chinoise Venenum Bufonis. L'hellebrigénine induit des dommages À l'ADN et un arrêt du cycle cellulaire G2/M. L'hellebrigénine déclenche l'apoptose médiée par les mitochondries.