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(144)
- Pyroptosis(42)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(188)
- Bcl-xL(8)
- c-RET(8)
- IAP(33)
- KEAP1-Nrf2(90)
- MDM2(12)
- p53(153)
- PC-PLC(4)
- PKD(7)
- RasGAP (Ras- P21)(1)
- Survivin(13)
- Thymidylate Synthase(12)
- TNF-α(262)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(132)
- ASK1(4)
- PAR4(2)
- RIP kinase(57)
- FKBP(25)
- Cuproptosis(4)
Products Related to Apoptosis(3381)
- GC68033TAS1553CAS: 2166023-31-8Purity: >98.00%
TAS1553 est un inhibiteur de l'interaction protéine-protéine de petite molécule qui supprime efficacement l'activité de la ribonucléotide réductase (RNR). En perturbant le processus de réplication de DNA et en réduisant le niveau intracellulaire de désoxyadénosine triphosphate (dATP), TAS1553 induit finalement l'apoptose.
- GC68470SPD304 dihydrochlorideCAS: 1049741-03-8Purity: >99.00%
SPD304 dihydrochloride est un inhibiteur sélectif du facteur de nécrose des tumeurs α (TNF-α), sa valeur d'IC50 est 22μM.
- GC685373-IN-PP1CAS: 2227110-54-3Purity: >98.00%
3-IN-PP1 est un inhibiteur de la protéine kinase D (PKD). Il présente une activité d'inhibition efficace et étendue sur PKD1, PKD2 et PKD3, avec des valeurs IC50 respectives de 108, 94 et 108 nM. 3-IN-PP1 est également un agent anticancéreux à large spectre qui a un effet inhibiteur sur la croissance de diverses cellules cancéreuses. Il peut être utilisé dans la recherche sur le cancer.
- GC685625-Aminolevulinic acid-13C-1 hydrochlorideCAS: 129720-94-1Purity: >98.00%
Le chlorhydrate d'acide 5-aminolévulinique-13C-1 (5-ALA-13C-1) est une forme marquée au carbone 13 de l'acide 5-aminolévulinique hydrochloride. L'acide 5-aminolévulinique hydrochloride (hydrochlorure de 5-ALA) est un intermédiaire de la biosynthèse de l'hème dans le corps, et il sert de précurseur à la porphyrine.
- GC68600Ac-DEVD-CMK TFAPurity: >98.00%
Ac-DEVD-CMK (Inhibiteur de la caspase-3 III) TFA est un inhibiteur sélectif et irréversible de la caspase-3. Ac-DEVD-CMK TFA inhibe significativement l'apoptose induite par le glucose élevé ou le dibenzoate 3,20 (IDB; 5). Ac-DEVD-CMK TFA peut être utilisé dans diverses méthodes expérimentales pour inhiber l'apoptose cellulaire.
- GC68621Ac-WEHD-AFC TFAPurity: >98.00%
Ac-WEHD-AFC TFA est un substrat de caspase-1 fluorescent. Ac-WEHD-AFC TFA peut détecter l'activité fluorescente de la caspase-1 et est utilisé dans la recherche sur les tumeurs et l'inflammation.
- GC68632AK-778-XXMUCAS: 1227045-76-2Purity: >99.50%
AK-778-XXMU est un inhibiteur efficace de l'antagoniste 2 de la liaison à l'ADN (ID2), avec une KD de 129 nM. AK-778-XXMU peut inhiber la migration et l'invasion des cellules tumorales du gliome, induire l'apoptose cellulaire et surtout ralentir la croissance tumorale.
- GC68729Bax activator-1CAS: 1638526-94-9Purity: >98.00%
Le Bax activateur-1 (composé 106) est un activateur de Bax qui induit l'apoptose des cellules tumorales dépendantes de Bax.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC68033 | TAS1553 | 2166023-31-8 | >98.00% | |
TAS1553 est un inhibiteur de l'interaction protéine-protéine de petite molécule qui supprime efficacement l'activité de la ribonucléotide réductase (RNR). En perturbant le processus de réplication de DNA et en réduisant le niveau intracellulaire de désoxyadénosine triphosphate (dATP), TAS1553 induit finalement l'apoptose. | ||||
| GC68043 | 2-tert-Butyl-1,4-benzoquinone | 3602-55-9 | >97.00% | |
| GC68051 | Citric acid-d4 | 147664-83-3 | >98.00% | |
| GC68213 | MitoBloCK-6 | 303215-67-0 | >98.00% | |
| GC68231 | 4-Methylsalicylic acid | 50-85-1 | >99.00% | |
| GC68288 | Brentuximab | 2088770-90-3 | >98.00% | |
| GC68305 | Dacetuzumab | 880486-59-9 | >98.00% | |
| GC68306 | Deoxynyboquinone | 96748-86-6 | >98.00% | |
| GC68308 | Bisdemethoxycurcumin-d8 | 2470233-08-8 | >98.00% | |
| GC68369 | Belantamab | 2061894-48-0 | >98.00% | |
| GC68371 | Mutant p53 modulator-1 | 2746371-35-5 | >98.00% | |
| GC68385 | TNF-α-IN-6 | 2699704-20-4 | >98.00% | |
| GC68388 | XIAP degrader-1 | 2803617-91-4 | >98.00% | |
| GC68404 | Human PD-L1 inhibitor IV | 2135542-83-3 | >98.00% | |
| GC68452 | 2,4,6-Triiodophenol | 609-23-4 | >98.00% | |
| GC68470 | SPD304 dihydrochloride | 1049741-03-8 | >99.00% | |
SPD304 dihydrochloride est un inhibiteur sélectif du facteur de nécrose des tumeurs α (TNF-α), sa valeur d'IC50 est 22μM. | ||||
| GC68537 | 3-IN-PP1 | 2227110-54-3 | >98.00% | |
3-IN-PP1 est un inhibiteur de la protéine kinase D (PKD). Il présente une activité d'inhibition efficace et étendue sur PKD1, PKD2 et PKD3, avec des valeurs IC50 respectives de 108, 94 et 108 nM. 3-IN-PP1 est également un agent anticancéreux à large spectre qui a un effet inhibiteur sur la croissance de diverses cellules cancéreuses. Il peut être utilisé dans la recherche sur le cancer. | ||||
| GC68562 | 5-Aminolevulinic acid-13C-1 hydrochloride | 129720-94-1 | >98.00% | |
Le chlorhydrate d'acide 5-aminolévulinique-13C-1 (5-ALA-13C-1) est une forme marquée au carbone 13 de l'acide 5-aminolévulinique hydrochloride. L'acide 5-aminolévulinique hydrochloride (hydrochlorure de 5-ALA) est un intermédiaire de la biosynthèse de l'hème dans le corps, et il sert de précurseur à la porphyrine. | ||||
| GC68600 | Ac-DEVD-CMK TFA | - | >98.00% | |
Ac-DEVD-CMK (Inhibiteur de la caspase-3 III) TFA est un inhibiteur sélectif et irréversible de la caspase-3. Ac-DEVD-CMK TFA inhibe significativement l'apoptose induite par le glucose élevé ou le dibenzoate 3,20 (IDB; 5). Ac-DEVD-CMK TFA peut être utilisé dans diverses méthodes expérimentales pour inhiber l'apoptose cellulaire. | ||||
| GC68621 | Ac-WEHD-AFC TFA | - | >98.00% | |
Ac-WEHD-AFC TFA est un substrat de caspase-1 fluorescent. Ac-WEHD-AFC TFA peut détecter l'activité fluorescente de la caspase-1 et est utilisé dans la recherche sur les tumeurs et l'inflammation. | ||||
| GC68632 | AK-778-XXMU | 1227045-76-2 | >99.50% | |
AK-778-XXMU est un inhibiteur efficace de l'antagoniste 2 de la liaison à l'ADN (ID2), avec une KD de 129 nM. AK-778-XXMU peut inhiber la migration et l'invasion des cellules tumorales du gliome, induire l'apoptose cellulaire et surtout ralentir la croissance tumorale. | ||||
| GC68700 | ASR-488 | 2690312-65-1 | >99.00% | |
ASR-488 peut activer la protéine de liaison à l'ARNm CPEB1, induisant l'apoptose cellulaire et inhibant la croissance du cancer de la vessie. | ||||
| GC68729 | Bax activator-1 | 1638526-94-9 | >98.00% | |
Le Bax activateur-1 (composé 106) est un activateur de Bax qui induit l'apoptose des cellules tumorales dépendantes de Bax. | ||||
| GC68744 | BC-?1258 | 1507370-40-2 | >98.00% | |
BC-1258 is an activator of F-box/LRR-repeat protein 2 (FBXL2) that stabilizes and upregulates FBXL2 levels. BC-1258 induces apoptosis in tumor cells and significantly inhibits tumor formation in mice. | ||||
