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(3387)
- GC73719BAY 1892005CAS: 2036352-13-1Purity: >99.00%
BAY 1892005 ist ein Regulator von p53 Protein und wirkt auf p53 Kondensate, ohne mutierte p53 Reaktivierung zu verursachen.
- GC73773PLK1/BRD4-IN-5Purity: >99.00%
PLK1/BRD4-IN-5 (Verbindung SC10) ist ein oral aktiver PLK1- und BRD4-Inhibitor mit IC50-Werten von 0,3 nM bzw. 60,8 nM.
- GC73823MMs02943764CAS: 708287-29-0Purity: >98.00%
MMs02943764 ist ein 1,2,4-Triazolderivat mit Antikrebsaktivität.
- GC73918BAY 249716CAS: 696628-24-7Purity: >99.00%
BAY 249716 stabilisiert alle drei p53 Proteinvarianten.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73719 | BAY 1892005 | 2036352-13-1 | >99.00% | |
BAY 1892005 ist ein Regulator von p53 Protein und wirkt auf p53 Kondensate, ohne mutierte p53 Reaktivierung zu verursachen. | ||||
| GC73725 | RIPK1-IN-17 | - | >98.00% | |
RIPK1-IN-17 (Verbindung 10) ist ein RIPK1- und RIPK3-Inhibitor. | ||||
| GC73740 | DCZ5418 | 2883709-99-5 | >99.00% | |
DCZ5418 ist ein Inhibitor von TRIP13. | ||||
| GC73744 | JAB-2485 | 2899209-55-1 | >98.00% | |
JAB-2485 ist ein potenter und selektiver Aurora Kinase A (AURKA)-Hemmer mit einem IC50 von 0,33 nM. | ||||
| GC73760 | Trilexium | 1983180-82-0 | >99.00% | |
Trilexium (TRX-E-009-1) ist eine dritte Generation von Benzopyran, die strukturell mit TRX-E-002-1 verwandt ist. | ||||
| GC73767 | PKM2-IN-6 | 771467-00-6 | >98.00% | |
PKM2-IN-6 (Verbindung 7d) ist ein potenter und oral aktiver PKM2-Inhibitor mit einem IC50-Wert von 23 nM. | ||||
| GC73773 | PLK1/BRD4-IN-5 | - | >99.00% | |
PLK1/BRD4-IN-5 (Verbindung SC10) ist ein oral aktiver PLK1- und BRD4-Inhibitor mit IC50-Werten von 0,3 nM bzw. 60,8 nM. | ||||
| GC73774 | YCH2823 | - | >99.00% | |
YCH2823 ist ein Inhibitor von USP7 (IC50.49.6 nM; Kd.0.117 μM). | ||||
| GC73795 | T-1-PMPA | 1323883-62-0 | >99.00% | |
T-1-PMPA ist ein potenter EGFR-Inhibitor mit apoptotischen Eigenschaften. | ||||
| GC73808 | Glutor | 2561471-22-3 | >99.00% | |
Glutor ist ein selektiver GLUT 1/2/3-Inhibitor, der die Glukoseaufnahme unterdrücken kann. | ||||
| GC73813 | IOX5 | - | >99.00% | |
IOX5 ist ein selektiver Prolyldroxylasen (PHD)-Hemmer. | ||||
| GC73822 | GNE-900 | 1200126-26-6 | >99.00% | |
GNE-900 ist ein ATP-kompetitiver, selektiver und oral aktiver ChK1-Inhibitor mit IC50s von 0,0011, 1,5 µM für ChKL bzw. ChK2. | ||||
| GC73823 | MMs02943764 | 708287-29-0 | >98.00% | |
MMs02943764 ist ein 1,2,4-Triazolderivat mit Antikrebsaktivität. | ||||
| GC73868 | WD6305 TFA | - | >98.00% | |
WD6305 TFA ist ein starker METTL3-gezielter PROTAC-Abbau. | ||||
| GC73881 | PRO-6E | 2353493-69-1 | >99.00% | |
PRO-6E ist ein orales aktives PROTAC auf Basis von Cereblon-Liganden und induziert den Abbau von MET mit maximalem Abbau von 81,9% bei 1 μM in MKN-45 Zellen. | ||||
| GC73893 | BLU-222 | 2888704-84-3 | >98.00% | |
BLU-222 ist ein oral aktiver und hochselektiver CDK2-Inhibitor. | ||||
| GC73900 | HA-9104 | 2412367-83-8 | >98.00% | |
HA-9104 ist ein potenter und selektiver Hemmer der Cullin-5-Neddylierung, der praktisch auf die V30-Tasche von UBE2F abzielt. | ||||
| GC73918 | BAY 249716 | 696628-24-7 | >99.00% | |
BAY 249716 stabilisiert alle drei p53 Proteinvarianten. | ||||
| GC73925 | YSR734 | 3032969-58-4 | >98.00% | |
YSR734 (Verbindung 21) ist ein kovalenter HDAC-Inhibitor mit IC50-Werten von 110 nM, 154 nM und 143 nM für HDAC1, HDAC2 und HDAC3. | ||||
| GC73928 | BDM19 | 500273-31-4 | >98.00% | |
BDM19 bindet und aktiviert zytosolische BAX Dimere und löst Zellapoptose entweder allein oder in Kombination mit BCL-2/BCL-XL Inhibitor Navitoclax aus. | ||||
| GC73932 | WK369 | - | >99.00% | |
WK369 ist ein neuartiger BCL6-Kleinmolekülhibitor, der eine hervorragende Anti-Eierstockkrebs-Bioaktivität aufweist, Zellzyklusarrest induziert und Apoptose verursacht. | ||||
| GC73935 | CBI1 formic | - | - | |
CBI1 formic ist ein kovalenter BAX-Hemmer. | ||||
| GC73939 | ATPase-IN-3 | 1134203-12-5 | >99.00% | |
ATPase-IN-3 (Verbindung 6) ist ein ATPase-Hemmer. | ||||
| GC73940 | BFC1108 | 692774-37-1 | >98.00% | |
BFC1108 ist ein kleiner Molekül Bcl-2 Funktionskonverter. | ||||
