Apoptosis
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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
- Caspase(114)
- Pyroptosis(37)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(154)
- Bcl-xL(8)
- c-RET(8)
- IAP(31)
- KEAP1-Nrf2(81)
- MDM2(12)
- p53(145)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(12)
- Thymidylate Synthase(10)
- TNF-α(189)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(106)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(23)
- Cuproptosis(4)
Products Related to Apoptosis(3030)
- GC91427Glutaminase C Inhibitor 11Purity: >95.00%
Le inhibiteur de la glutaminase C 11 est un inhibiteur de la glutaminase C (GAC).
- GC91782DPP-9 Inhibitor 42Purity: >95.00%
DPP-9 inhibitor 42 is an inhibitor of dipeptidyl peptidase 9 (DDP-9; IC50 = 0.0034 µM).
- GC91967LMTK3 Inhibitor C28CAS: 2764850-23-7Purity: >98.00%
LMTK3 Inhibitor C28 est un inhibiteur de la multi-kinase.
- GC91977TrkB Agonist Prodrug R13CAS: 1609067-49-3Purity: >95.00%
TrkB Agonist Prodrug R13 (R13) est une forme propharmaceutique de l'activateur de la kinase B associée à la protomyosine (TrkB), la 7,8 - dihydroxyflavone.
- GC92037JQKD82 (hydrochloride)CAS: 2863676-87-1Purity: >98.00%
JQKD82 (hydrochloride) est une forme promédicament de KDM5-C49, un inhibiteur du domaine interactif 1A riche en Jumonji at (JARID1A), également connu sous le nom de déméthylase 5A spécifique de la lysine (KDM5A).
- GC920741,2,3-Trioleoyl Glycerol-d5CAS: 60892-83-3Purity: >99.00%
1,2,3-Trioleoyl Glycerol-d5 est destiné à être utilisé comme étalon interne pour la quantification du 1,2,3-trioléoyl glycérol par GC- ou LC-MS.
- GC92099MSG606 (trifluoroacetate salt)Purity: >95.00%
MSG606 (trifluoroacetate salt) est un antagoniste peptidique du récepteur 1 de la mélanocortine (MC1R; IC50 = 17 nm pour les récepteurs humains) et un dérivé de l'hormone stimulante des gamma - mélanocytes (gamma - MSH).
- GF04703Phosphocreatine di-tris saltCAS: 108321-17-1Purity: >97.00%
Phosphocreatine di-tris salt est une molécule de créatine phosphorylée qui sert de réserve de phosphate à forte énergie dans muscles des vertébrés et de certains invertébrés, fournissant du phosphate pour la conversion de ADP en ATP.
- GF15486Cathepsin B from bovine spleenCAS: 9047-22-7
Cathepsin B from bovine spleen (Cathepsine B) est un membre de la famille des protéases cystéïnes de papaine - type. Cathepsin B est synthétisé sous forme d'une préproenzyme composée de 335 acides aminés, avec un poids moléculaire calculé approximativement 36,7kDa. Cathepsin B est localisé dans la compartiment endosomal/lysosomal, où Cathepsin B fonctionne à la fois comme une endoprotéase et une exoprotéase. Cathepsin B participe principalement au renouvellement régulier les protéines intracellulaires et extracellulaires, ainsi donc, maintient l'activité métabolique homéostatique en cellule.
- GF175318-EpixanthatinCAS: 30890-35-8Purity: >98.00%
8-Epixanthatin est un inhibiteur de croissance induit par la lumière, qui régule la courbure phototropique des hypocotyles de tournesol.
- GN10040DehydrocorydalineCAS: 30045-16-0Purity: >98.00%
Dehydrocorydaline est l'un des alcaloïdes quarternaires de Corydalis Rhizoma.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC91427 | Glutaminase C Inhibitor 11 | - | >95.00% | |
Le inhibiteur de la glutaminase C 11 est un inhibiteur de la glutaminase C (GAC). | ||||
| GC91595 | PDIC-NC | 2633013-75-7 | >95.00% | |
PDIC-NC is an activator of stimulator of interferon genes (STING) and an anticancer agent. | ||||
| GC91688 | PDIC-NN | 932740-48-2 | >95.00% | |
PDIC-NN is an intermediate in the synthesis of PDIC-NS , an activator of stimulator of interferon genes (STING) with anticancer activity. | ||||
| GC91782 | DPP-9 Inhibitor 42 | - | >95.00% | |
DPP-9 inhibitor 42 is an inhibitor of dipeptidyl peptidase 9 (DDP-9; IC50 = 0.0034 µM). | ||||
| GC91820 | PDIC-NS | - | >95.00% | |
PDIC-NS is an activator of stimulator of interferon genes (STING). | ||||
| GC91967 | LMTK3 Inhibitor C28 | 2764850-23-7 | >98.00% | |
LMTK3 Inhibitor C28 est un inhibiteur de la multi-kinase. | ||||
| GC91977 | TrkB Agonist Prodrug R13 | 1609067-49-3 | >95.00% | |
TrkB Agonist Prodrug R13 (R13) est une forme propharmaceutique de l'activateur de la kinase B associée à la protomyosine (TrkB), la 7,8 - dihydroxyflavone. | ||||
| GC92023 | PTX80 | 2376297-69-5 | >95.00% | |
PTX80 est un antagoniste de p62 (ci50 = 31,18 nM pour le récepteur humain). | ||||
| GC92037 | JQKD82 (hydrochloride) | 2863676-87-1 | >98.00% | |
JQKD82 (hydrochloride) est une forme promédicament de KDM5-C49, un inhibiteur du domaine interactif 1A riche en Jumonji at (JARID1A), également connu sous le nom de déméthylase 5A spécifique de la lysine (KDM5A). | ||||
| GC92066 | RMC-6236 | 2765081-21-6 | >99.00% | |
RMC-6236 est un inhibiteur réversibe de RAS multisélectif qui connecte GTP. | ||||
| GC92074 | 1,2,3-Trioleoyl Glycerol-d5 | 60892-83-3 | >99.00% | |
1,2,3-Trioleoyl Glycerol-d5 est destiné à être utilisé comme étalon interne pour la quantification du 1,2,3-trioléoyl glycérol par GC- ou LC-MS. | ||||
| GC92099 | MSG606 (trifluoroacetate salt) | - | >95.00% | |
MSG606 (trifluoroacetate salt) est un antagoniste peptidique du récepteur 1 de la mélanocortine (MC1R; IC50 = 17 nm pour les récepteurs humains) et un dérivé de l'hormone stimulante des gamma - mélanocytes (gamma - MSH). | ||||
| GF04703 | Phosphocreatine di-tris salt | 108321-17-1 | >97.00% | |
Phosphocreatine di-tris salt est une molécule de créatine phosphorylée qui sert de réserve de phosphate à forte énergie dans muscles des vertébrés et de certains invertébrés, fournissant du phosphate pour la conversion de ADP en ATP. | ||||
| GF11023 | Hecubine | 62874-52-6 | >98.00% | |
Hecubine is a natural aspidosperma-type alkaloid found in E. officinalis , with anti-neuroinflammation properties. | ||||
| GF15486 | Cathepsin B from bovine spleen | 9047-22-7 | - | |
Cathepsin B from bovine spleen (Cathepsine B) est un membre de la famille des protéases cystéïnes de papaine - type. Cathepsin B est synthétisé sous forme d'une préproenzyme composée de 335 acides aminés, avec un poids moléculaire calculé approximativement 36,7kDa. Cathepsin B est localisé dans la compartiment endosomal/lysosomal, où Cathepsin B fonctionne à la fois comme une endoprotéase et une exoprotéase. Cathepsin B participe principalement au renouvellement régulier les protéines intracellulaires et extracellulaires, ainsi donc, maintient l'activité métabolique homéostatique en cellule. | ||||
| GF17531 | 8-Epixanthatin | 30890-35-8 | >98.00% | |
8-Epixanthatin est un inhibiteur de croissance induit par la lumière, qui régule la courbure phototropique des hypocotyles de tournesol. | ||||
| GN10005 | Schisandrin C | 61301-33-5 | >99.50% | |
| GN10017 | Wogonin | 632-85-9 | >98.00% | |
Wogonin est un inhibiteur compétitif puissant de CYP1A2, avec une constante Ki de 0.24μM. | ||||
| GN10019 | Ginsenoside Rg6 | 147419-93-0 | >99.50% | |
| GN10030 | Fisetin | 528-48-3 | >98.00% | |
Fisetin est un flavonoïde naturel trouvé dans les nombreux fruits et légumes qui possède les mutilples activités biologiques. | ||||
| GN10035 | 9-Methoxycamptothecin | 19685-10-0 | >99.00% | |
| GN10037 | Bisdemethoxycurcumin | 33171-05-0 | >98.00% | |
| GN10038 | Ginsenoside Rh3 | 105558-26-7 | >99.50% | |
| GN10040 | Dehydrocorydaline | 30045-16-0 | >98.00% | |
Dehydrocorydaline est l'un des alcaloïdes quarternaires de Corydalis Rhizoma. | ||||
