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(143)
- 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(87)
- MDM2(12)
- p53(153)
- PC-PLC(4)
- PKD(7)
- RasGAP (Ras- P21)(1)
- Survivin(13)
- Thymidylate Synthase(12)
- TNF-α(255)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(131)
- ASK1(4)
- PAR4(2)
- RIP kinase(57)
- FKBP(25)
- Cuproptosis(4)
Products Related to Apoptosis(3359)
- GC72931HTH-01-091 TFAPurity: >98.00%
HTH-01-091 TFA es un potente y selectivo inhibide la cinasa (MELK), con una IC50 de 10,5 nM.
- GC72985Z-LEVD-FMKCAS: 1135688-25-3Purity: >98.50%
Z-LEVD-FMK es un inhibide la caspasa-4 permeable a las células.
- GC72991(Rac)-LisaftoclaxCAS: 2651980-10-6Purity: >98.00%
(Rac)-Lisaftoclax Rac-APG-2575 es un inhibidor de Bcl-2 que puede ser uesd para la investigación de malignihematcn112898295a.
- GC73002Ganglioside GD3 diammoniumPurity: >98.00%
Ganglioside GD3 diammonium es un glicoesfingolípido ácido.
- GC73025Teprasiran sodiumCAS: 2169310-72-7Purity: >90.00%
Teprasiran sodium es un pequeño ARN interfiriendo que inhitemporalmente la muerte celular mediada por p53 que subyace a la lesión renal aguda (AKI).
- GC73093Custirsen sodiumPurity: >98.00%
Custirsen sodium inhila la producción de clusterina, una proteína antiapoptótica que se incrementa en respuesta a la quimioterapia y que confiere resistencia al tratamiento.
- GC73109Danvatirsen sodiumPurity: >97.00%
Danvatirsen sodium es un oligonucleótido antisentido dirigido a STAT3 con potencial actividad antitumoral.
- GC73112JPS014 TFAPurity: >98.00%
JPS014 TFA es un Von Hippel-Lindau (VHL) basado en benzamida proteólie3-ligasa dirigida a quimeras (PROTAC).
- GC73129SIAIS164018 hydrochloridePurity: >99.00%
SIAIS164018 hydrochloride es un degraalk y EGFR basado en protac, con un valor de IC50 de 2.5 nM y 6.6 nM para ALK y ALK G1202R, respectivamente.
- GC73133MisetionamideCAS: 856785-75-6Purity: >99.00%
Misetionamide es un compuesto similar a la oxatiazina oral.
- GC73138PBENZ-DBRMDCAS: 1454662-41-9Purity: >99.00%
PBENZ-DBRMD es un potente inhibidor de la iodotronina deiodinasa tipo 3 (DIO3).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC72915 | (R)-MRT199665 | - | >98.00% | |
(R)-MRT199665 es un isómero de MRT199665. | ||||
| GC72924 | PD173952 | 305820-75-1 | >99.00% | |
PD173952 es un inhibidor de tirosina cinasa con IC50s de 0.3, 1.7 y 6.6 nM contra Lyn, Abl y Csk, respectivamente. | ||||
| GC72928 | DB818 | 790241-43-9 | >98.00% | |
DB818 es un potente inhibidor de Homeobox A9 (HOXA9). | ||||
| GC72929 | DB818 dihydrochloride | - | - | |
DB818 dihydrochloride es la forma de sal de didroclorde DB818. | ||||
| GC72931 | HTH-01-091 TFA | - | >98.00% | |
HTH-01-091 TFA es un potente y selectivo inhibide la cinasa (MELK), con una IC50 de 10,5 nM. | ||||
| GC72933 | LQZ-7F | 354543-09-2 | >97.00% | |
LQZ-7F, un inhibidor de la dimeride de supervivencia, induce apoptosis espontánea y sinergia con Docetaxel en células cancerosas de próstata. | ||||
| GC72944 | MMRi64 | 430458-66-5 | >98.00% | |
MMRi64 altera las interacciones Mdm2-MdmX. | ||||
| GC72971 | INCB3619 | 791826-72-7 | >98.00% | |
INCB3619 es un inhibidor de ADAM selectivo y activo por vía oral con IC50 de 22 nM y 14 nM para ADAM10 y ADAM17, respectivamente. | ||||
| GC72985 | Z-LEVD-FMK | 1135688-25-3 | >98.50% | |
Z-LEVD-FMK es un inhibide la caspasa-4 permeable a las células. | ||||
| GC72991 | (Rac)-Lisaftoclax | 2651980-10-6 | >98.00% | |
(Rac)-Lisaftoclax Rac-APG-2575 es un inhibidor de Bcl-2 que puede ser uesd para la investigación de malignihematcn112898295a. | ||||
| GC72994 | RAPTA-C | 372948-28-2 | >99.00% | |
RAPTA-C (Ru(− 6-p-cymene)Cl2(PTA)) actúa como un agente anti-cáncer y anti-angiogénico. | ||||
| GC73002 | Ganglioside GD3 diammonium | - | >98.00% | |
Ganglioside GD3 diammonium es un glicoesfingolípido ácido. | ||||
| GC73016 | AZD4877 | 758722-49-5 | >98.00% | |
AZD4877 es otro isostere de Ispinesib y también un inhibide la proteína del huso de cinesina (Eg5) con IC50 de 2 nM. | ||||
| GC73025 | Teprasiran sodium | 2169310-72-7 | >90.00% | |
Teprasiran sodium es un pequeño ARN interfiriendo que inhitemporalmente la muerte celular mediada por p53 que subyace a la lesión renal aguda (AKI). | ||||
| GC73077 | ARI-1 | - | >99.00% | |
ARI-1 es un inhibidel receptor receptor de tirosina quinasa similar al receptor huérf1 (ROR1). | ||||
| GC73093 | Custirsen sodium | - | >98.00% | |
Custirsen sodium inhila la producción de clusterina, una proteína antiapoptótica que se incrementa en respuesta a la quimioterapia y que confiere resistencia al tratamiento. | ||||
| GC73109 | Danvatirsen sodium | - | >97.00% | |
Danvatirsen sodium es un oligonucleótido antisentido dirigido a STAT3 con potencial actividad antitumoral. | ||||
| GC73112 | JPS014 TFA | - | >98.00% | |
JPS014 TFA es un Von Hippel-Lindau (VHL) basado en benzamida proteólie3-ligasa dirigida a quimeras (PROTAC). | ||||
| GC73118 | EB1 | 42951-68-8 | >99.00% | |
EB1 es el inhibidor de las cinasas MNK con IC50s de 0,69 μM (MNK1) y 9,4 μM (MNK2). | ||||
| GC73129 | SIAIS164018 hydrochloride | - | >99.00% | |
SIAIS164018 hydrochloride es un degraalk y EGFR basado en protac, con un valor de IC50 de 2.5 nM y 6.6 nM para ALK y ALK G1202R, respectivamente. | ||||
| GC73133 | Misetionamide | 856785-75-6 | >99.00% | |
Misetionamide es un compuesto similar a la oxatiazina oral. | ||||
| GC73136 | VPC-70063 | 13571-44-3 | >99.00% | |
VPC-70063 es un potente inhibidor de Myc-Max con un valor de IC50 de 8.9 μM para inhibide la actividad transcripcional de Myc-Max. | ||||
| GC73138 | PBENZ-DBRMD | 1454662-41-9 | >99.00% | |
PBENZ-DBRMD es un potente inhibidor de la iodotronina deiodinasa tipo 3 (DIO3). | ||||
| GC73146 | Sonrotoclax | 2383086-06-2 | >99.00% | |
Sonrotoclax es un potente inhibidor de Bcl2. | ||||
