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)
- GC73168p53 Activator 3CAS: 2636839-90-0Purity: >95.00%
p53 Activator 3 (compuesto 87A) es un potente activador p53 con un valor SC150 de <0.05 mM.
- GC73220LSD1-IN-24CAS: 4734-59-2Purity: >99.00%
LSD1-IN-24(compuesto 3S) es un inhibidor selectivo de LSD1 con IC50 = 0.247 μM.
- GC73225ROS-generating agent 1CAS: 2369030-41-9Purity: >99.00%
ROS-generating agent 1 (compuesto 2c) modifica covalentemente el residuo Sec-498 de TrxR para generar ROS.
- GC73232PRDX1-IN-1Purity: >98.00%
PRDX1-IN-1 es un inhibidor selectivo de PRDX1 con un valor de IC50 de 0.164 μM.
- GC73272PARP-1-IN-3CAS: 2976342-33-1Purity: >99.00%
PARP-1-IN-3, un derivado de la benzamida, es un potente inhibidor de PARP-1 con valores de IC50 de 0,25 nM y 2,34 nM para PARP-1 y PARP-2, respectivamente.
- GC73274EGFR T790M/L858R-IN-2CAS: 2955607-40-4Purity: >99.00%
EGFR T790M/L858R-IN-2 es un potente y selectivo inhibidor de EGFRT790M/L858R con valores de IC50 de 3,5, 1290 nM para EGFRT790M/L858R, EGFR WT, respectivamente.
- GC73275PD-L1-IN-2CAS: 2894733-91-4Purity: >98.00%
PD-L1-IN-2 es un posible agente tumoral inmunológico al inhibir PD-L1.
- GC73288CDK8-IN-13CAS: 918523-75-8Purity: >98.00%
CDK8-IN-13 resulta un inhibidor potente, muy específico y apto para administración oral contra la CDK8, su valor IC 50 alcanza los 51.9nM.
- GC73309Anti-melanoma agent 1CAS: 2418579-17-4Purity: >99.00%
Anti-melanoma agent 1 (compuesto 5m) es un agente anti-melanoma e induce apoptosis celular.
- GC73311STAT3-IN-13CAS: 2248552-86-3Purity: >99.00%
STAT3-IN-13 (compuesto 6f) es un potente inhibidor de STAT3.
- GC73313PI3Kα-IN-9CAS: 2715287-67-3Purity: >99.00%
PI3Kα-IN-9 (compuesto 27) es un inhibidor selectivo, de acción prolongada y activo de PI3Kα con valores de IC50 de 4,4, 128, 146 y 153 nM para PI3Kα, PI3Kγ, PI3Kδ y PI3Kβ, respectivamente.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73159 | KTX-582 | 2573298-13-0 | >98.00% | |
KTX-582 es un degrader IRAK4 potente con valores DC50 de 4 nM y 5 nM para IRAK4 e Ikaros, respectivamente. | ||||
| GC73166 | U7D-1 | - | >99.00% | |
U7D-1 es el primer degrausp7 potente y selectivo en su clase (ubiquitin-specific protease 7), con un DC50 de 33 nM en RS4;11 células. | ||||
| GC73168 | p53 Activator 3 | 2636839-90-0 | >95.00% | |
p53 Activator 3 (compuesto 87A) es un potente activador p53 con un valor SC150 de <0.05 mM. | ||||
| GC73188 | SFI003 | 2361332-90-1 | >99.00% | |
SFI003 es un inhibidor de SRSF3 que conduce la apoptosis de las células del CRC a través del eje SRSF3/DHCR24/ROS y exhibe potentes efectos antitumorales tanto in vitro como in vivo. | ||||
| GC73199 | M47 | 890808-56-7 | >99.00% | |
M47 es una molécula pequeña que desestabiliselectivamente el criptocro1 (CRY1) y aumenta la degradación del CRY1 en el núcleo. | ||||
| GC73210 | MTR-106 | 1639357-93-9 | >99.00% | |
MTR-106 es un potente estabilig-quadruplex y un inhibide la ARN polimerasa I. | ||||
| GC73212 | TH-6 | 3031349-25-1 | >95.00% | |
TH-6 es un potente inhibidor de HDAC con IC50s de 0,115, 0,135, 0,242, 0,138, 2,120 µM para HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectivamente. | ||||
| GC73220 | LSD1-IN-24 | 4734-59-2 | >99.00% | |
LSD1-IN-24(compuesto 3S) es un inhibidor selectivo de LSD1 con IC50 = 0.247 μM. | ||||
| GC73225 | ROS-generating agent 1 | 2369030-41-9 | >99.00% | |
ROS-generating agent 1 (compuesto 2c) modifica covalentemente el residuo Sec-498 de TrxR para generar ROS. | ||||
| GC73228 | MS78 | 3034773-00-4 | >99.00% | |
MS78 es una acetilación dirigida a la quimera (AceTAC) que acetilla proteína suprestumoral p53. | ||||
| GC73232 | PRDX1-IN-1 | - | >98.00% | |
PRDX1-IN-1 es un inhibidor selectivo de PRDX1 con un valor de IC50 de 0.164 μM. | ||||
| GC73234 | MY-673 | 2944459-96-3 | >98.00% | |
MY-673 es un inhibidor del sitio de Unión a la colchicina (CBSI), que inhila la polimerización de la tubulina. | ||||
| GC73237 | BWA-522 | 3042820-12-9 | >99.00% | |
BWA-522 es una pequeña molécula disponible por vía oral con un efecto significativo de degradación en AR-FL y AR-V7. | ||||
| GC73243 | Nrf2-IN-3 | 6325-13-9 | >99.00% | |
Nrf2-IN-3 (compuesto R16) es un inhibidor de Nrf2. | ||||
| GC73268 | PH14 | - | >99.00% | |
PH14 es un inhibidor dual PI3K/HDAC con valores de IC50 de 20.3 nM y 24.5 nM para PI3Kα y HDAC3, respectivamente. | ||||
| GC73269 | ABBV-467 | 2287186-66-5 | >99.00% | |
ABBV-467 es un inhibidor selectivo de MCL-1 (Ki: <0.01 nM). | ||||
| GC73272 | PARP-1-IN-3 | 2976342-33-1 | >99.00% | |
PARP-1-IN-3, un derivado de la benzamida, es un potente inhibidor de PARP-1 con valores de IC50 de 0,25 nM y 2,34 nM para PARP-1 y PARP-2, respectivamente. | ||||
| GC73274 | EGFR T790M/L858R-IN-2 | 2955607-40-4 | >99.00% | |
EGFR T790M/L858R-IN-2 es un potente y selectivo inhibidor de EGFRT790M/L858R con valores de IC50 de 3,5, 1290 nM para EGFRT790M/L858R, EGFR WT, respectivamente. | ||||
| GC73275 | PD-L1-IN-2 | 2894733-91-4 | >98.00% | |
PD-L1-IN-2 es un posible agente tumoral inmunológico al inhibir PD-L1. | ||||
| GC73288 | CDK8-IN-13 | 918523-75-8 | >98.00% | |
CDK8-IN-13 resulta un inhibidor potente, muy específico y apto para administración oral contra la CDK8, su valor IC 50 alcanza los 51.9nM. | ||||
| GC73294 | F5446 | 2304465-89-0 | >99.00% | |
F5446 (compuesto 1) es un inhibiselectivo de pequeñas moléculas de SUV39H1 metltransferasa. | ||||
| GC73309 | Anti-melanoma agent 1 | 2418579-17-4 | >99.00% | |
Anti-melanoma agent 1 (compuesto 5m) es un agente anti-melanoma e induce apoptosis celular. | ||||
| GC73311 | STAT3-IN-13 | 2248552-86-3 | >99.00% | |
STAT3-IN-13 (compuesto 6f) es un potente inhibidor de STAT3. | ||||
| GC73313 | PI3Kα-IN-9 | 2715287-67-3 | >99.00% | |
PI3Kα-IN-9 (compuesto 27) es un inhibidor selectivo, de acción prolongada y activo de PI3Kα con valores de IC50 de 4,4, 128, 146 y 153 nM para PI3Kα, PI3Kγ, PI3Kδ y PI3Kβ, respectivamente. | ||||
