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(133)
- Pyroptosis(40)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(175)
- Bcl-xL(8)
- c-RET(8)
- IAP(32)
- KEAP1-Nrf2(83)
- MDM2(12)
- p53(149)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(13)
- Thymidylate Synthase(10)
- TNF-α(231)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(123)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(24)
- Cuproptosis(4)
Products Related to Apoptosis(3219)
- GC78957(2S,3R,4S)-ASX-173CAS: 2748800-07-7Purity: >99.00%
(2S,3R,4S)-ASX-173 is the (2S,3R,4S)-enantiomer of ASX-173.
- GC78965ACT001 hydrochlorideCAS: 1403357-80-1Purity: >98.00%
ACT001 (Dimethylaminomicheliolide; DMAMCL) hydrochloride is an orally active, blood-brain barrier-permeable anti-inflammatory and anti-tumor agent.
- GC78968AritinerceptCAS: 3057276-00-0Purity: >99.50%
Aritinercept (AUR-200) is a recombinant fusion protein targeting TNFSF13B/BAFF/CD257.
- GC78972MI-773 TFACAS: 1303609-37-1Purity: >98.50%
MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a K i of 0.88 nM for MDM2.
- GC78973Peptide 234CM TFAPurity: >98.00%
Peptide 234CM TFA is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234.
- GC78974p53 (17-26) acetatePurity: >98.00%
p53 (17-26) acetate is a peptide derived from the P53 MDM2 binding domain, with a K d of 50 nM for MDM2.
- GC78980Rhodojaponin VICAS: 37720-87-9Purity: >99.50%
Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G.
- GC78982OlevaprubartCAS: 3062612-72-7Purity: >99.00%
Olevaprubart is a humanized IgG1-κ monoclonal antibody targeting TNFSF4, which can be used for the research of autoimmune diseases such as atopic dermatitis and alopecia areata [1] .
- GC78983Mouse Tnf ASOPurity: >96.00%
Mouse Tnf ASO is an antisense oligonucleotide ( ASO ) that targets the expression of mouse TNF-α. Mouse Tnf ASO reduces the tissue levels of various pro-inflammatory cytokines, Th1 cytokines and Th17 cytokines.
- GC78984Anti-Mouse CD120a Antibody (55R-170)Purity: >99.50%
Anti-Mouse CD120a Antibody (55R-170) reacts with the mouse CD120a.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC78954 | OH14 | 1018153-87-1 | >99.50% | |
OH14 is a cellular FLICE-like inhibitory protein ( cFLIP) inhibitor and TNF-related apoptosis-inducing ligand ( TRAIL ) sensitizer. | ||||
| GC78955 | AP21998 | 292606-90-7 | >99.00% | |
AP21998 is a non-immunosuppressive derivative of Rapamycin and an inducer of exocytosis. | ||||
| GC78957 | (2S,3R,4S)-ASX-173 | 2748800-07-7 | >99.00% | |
(2S,3R,4S)-ASX-173 is the (2S,3R,4S)-enantiomer of ASX-173. | ||||
| GC78958 | TMLB-C16 | 2923531-50-2 | >99.00% | |
TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a K D of 3.962 μM. | ||||
| GC78960 | DL78 | 132993-79-4 | >99.00% | |
DL78 is an effective anti-mitotic agent. | ||||
| GC78961 | GPS167 | 3034312-19-8 | >98.00% | |
GPS167 is a CLK kinase inhibitor that potently and selectively inhibits recombinant human CLK1, CLK2 and CLK4. | ||||
| GC78962 | MS1129 | - | >98.00% | |
MS1129 is a DNMT degrader that induces proteasomal degradation of DNMT1, DNMT3A and DNMT3B proteins. | ||||
| GC78963 | SM-122 | 874270-38-9 | >98.00% | |
SM-122 is a monovalent Smac mimetic targeting cellular inhibitor of apoptosis protein ( cIAP )-1/2. | ||||
| GC78964 | BV6 TFA | - | >99.50% | |
BV6 TFA is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis ( IAP ) family. | ||||
| GC78965 | ACT001 hydrochloride | 1403357-80-1 | >98.00% | |
ACT001 (Dimethylaminomicheliolide; DMAMCL) hydrochloride is an orally active, blood-brain barrier-permeable anti-inflammatory and anti-tumor agent. | ||||
| GC78966 | SK56 | - | >95.00% | |
SK56 is a GSDMD-NT pore inhibitor. | ||||
| GC78967 | ELTLGEFLKL | 303068-29-3 | >99.00% | |
ELTLGEFLKL is a survivin peptide. | ||||
| GC78968 | Aritinercept | 3057276-00-0 | >99.50% | |
Aritinercept (AUR-200) is a recombinant fusion protein targeting TNFSF13B/BAFF/CD257. | ||||
| GC78969 | WJH-C19 | - | >98.50% | |
WJH-C19 is an orally active RIPK1 inhibitor with an IC 50 of 5.7 nM. | ||||
| GC78970 | UCI-LC0019 | 1372406-51-3 | >98.50% | |
UCI-LC0019 is a mutant p53 reactivator. | ||||
| GC78971 | UCI-1014 | 304896-41-1 | >98.00% | |
UCI-1014 is a mutant p53 ( p53 R175H ) corrector/reactivator. | ||||
| GC78972 | MI-773 TFA | 1303609-37-1 | >98.50% | |
MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a K i of 0.88 nM for MDM2. | ||||
| GC78973 | Peptide 234CM TFA | - | >98.00% | |
Peptide 234CM TFA is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. | ||||
| GC78974 | p53 (17-26) acetate | - | >98.00% | |
p53 (17-26) acetate is a peptide derived from the P53 MDM2 binding domain, with a K d of 50 nM for MDM2. | ||||
| GC78980 | Rhodojaponin VI | 37720-87-9 | >99.50% | |
Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. | ||||
| GC78981 | HBS-101 | - | >99.50% | |
HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor ( K D = 38.4 nM). | ||||
| GC78982 | Olevaprubart | 3062612-72-7 | >99.00% | |
Olevaprubart is a humanized IgG1-κ monoclonal antibody targeting TNFSF4, which can be used for the research of autoimmune diseases such as atopic dermatitis and alopecia areata [1] . | ||||
| GC78983 | Mouse Tnf ASO | - | >96.00% | |
Mouse Tnf ASO is an antisense oligonucleotide ( ASO ) that targets the expression of mouse TNF-α. Mouse Tnf ASO reduces the tissue levels of various pro-inflammatory cytokines, Th1 cytokines and Th17 cytokines. | ||||
| GC78984 | Anti-Mouse CD120a Antibody (55R-170) | - | >99.50% | |
Anti-Mouse CD120a Antibody (55R-170) reacts with the mouse CD120a. | ||||
