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(137)
- Pyroptosis(41)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(179)
- Bcl-xL(8)
- c-RET(8)
- IAP(32)
- KEAP1-Nrf2(86)
- MDM2(12)
- p53(151)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(13)
- Thymidylate Synthase(10)
- TNF-α(239)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(128)
- ASK1(4)
- PAR4(2)
- RIP kinase(57)
- FKBP(24)
- Cuproptosis(4)
Products Related to Apoptosis(3266)
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WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC 50 value of 1.33 μM.
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PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53 Y 220C -PLK1 ternary complex ( EC 50 = 1.4 μM).
- GC79009Tubulin polymerization-IN-84CAS: 2982893-14-9Purity: >99.50%
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with an IC 50 = 10.9 μM.
- GC79045LY3295668 erbumineCAS: 1919888-07-5Purity: >98.00%
LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a K i values for AurA and AurB of 0.8 nM and 1038 nM respectively.
- GC79046HDAC-IN-98CAS: 3124773-51-6Purity: >98.00%
HDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC 50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively.
- GC79047HDAC6-IN-75CAS: 400078-78-6Purity: >99.50%
HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC 50 of 0.17 nM against HDAC6.
- GC79048HDAC1/3-IN-1CAS: 244289-53-0Purity: >99.50%
HDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC 50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively.
- GC79058PARP1/NAMPT-IN-1CAS: 3084810-86-3Purity: >98.00%
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC 50 values of 1.2 nM and 6.7 nM, respectively.
- GC79067ADAR1i-124Purity: >98.50%
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110.
- GC79070WWQ-03-012CAS: 3076807-15-0Purity: >98.00%
WWQ-03-012 is a selective DESI2 inhibitor with an IC 50 of 47.3 nM.
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Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor.
- GC79104(Rac)-Chem-0199CAS: 122981-77-5Purity: >99.50%
(Rac)-Chem-0199 is the racemic mixture of Chem-0199.
- GC79109CZS-241 hydrochloridePurity: >98.50%
CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC 50 =2.6 nM).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC78998 | CTX-439 | 2377487-13-1 | >98.00% | |
CTX-439 is an orally active, ATP-competitive small-molecule inhibitor of CDK12 and CDK13, with an IC 50 of 3.1 nM and a K d of 0.38 nM against CDK12, and an IC 50 of 9.2 nM against CDK13. | ||||
| GC78999 | CID-078 | 3064485-16-8 | >99.00% | |
CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. | ||||
| GC79001 | SY-589 | 3077714-09-8 | >98.50% | |
SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor ( IC 50 =2.29 nM) and DNA damage inducer. | ||||
| GC79002 | C791-0064 | 902940-64-1 | >99.00% | |
C791-0064 is a RAD52 inhibitor. | ||||
| GC79003 | WCY-8-67 TFA | - | >99.00% | |
WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC 50 value of 1.33 μM. | ||||
| GC79004 | PMV6-PEG4-BI2536 | - | >98.00% | |
PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53 Y 220C -PLK1 ternary complex ( EC 50 = 1.4 μM). | ||||
| GC79009 | Tubulin polymerization-IN-84 | 2982893-14-9 | >99.50% | |
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with an IC 50 = 10.9 μM. | ||||
| GC79044 | ATC12 | 384860-40-6 | >98.00% | |
ATC12 is a Aurora-A kinase inhibitor. | ||||
| GC79045 | LY3295668 erbumine | 1919888-07-5 | >98.00% | |
LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a K i values for AurA and AurB of 0.8 nM and 1038 nM respectively. | ||||
| GC79046 | HDAC-IN-98 | 3124773-51-6 | >98.00% | |
HDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC 50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. | ||||
| GC79047 | HDAC6-IN-75 | 400078-78-6 | >99.50% | |
HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC 50 of 0.17 nM against HDAC6. | ||||
| GC79048 | HDAC1/3-IN-1 | 244289-53-0 | >99.50% | |
HDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC 50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively. | ||||
| GC79049 | CG-1521 | 674767-29-4 | >95.50% | |
CG-1521 is a histone deacetylase ( HDAC ) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. | ||||
| GC79050 | OUL312 | - | >99.00% | |
OUL312 is a potent PARP10 inhibitor ( IC 50 = 20 nM), showing more than 75-fold greater selectivity for PARP15 ( IC 50 = 1500 nM). | ||||
| GC79057 | BF-175 | 1333375-02-2 | >98.00% | |
BF-175 is a selective SIRT1 agonist. | ||||
| GC79058 | PARP1/NAMPT-IN-1 | 3084810-86-3 | >98.00% | |
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC 50 values of 1.2 nM and 6.7 nM, respectively. | ||||
| GC79067 | ADAR1i-124 | - | >98.50% | |
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110. | ||||
| GC79070 | WWQ-03-012 | 3076807-15-0 | >98.00% | |
WWQ-03-012 is a selective DESI2 inhibitor with an IC 50 of 47.3 nM. | ||||
| GC79072 | MS6076 | - | >98.00% | |
MS6076 is a mitochondrial protease ClpP agonist. | ||||
| GC79077 | DDO-6600 | 2640292-37-9 | >98.00% | |
DDO-6600 is a covalent Hsp90 inhibitor. | ||||
| GC79103 | Berzosertib hydrochloride | 1428935-04-9 | >98.50% | |
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. | ||||
| GC79104 | (Rac)-Chem-0199 | 122981-77-5 | >99.50% | |
(Rac)-Chem-0199 is the racemic mixture of Chem-0199. | ||||
| GC79109 | CZS-241 hydrochloride | - | >98.50% | |
CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC 50 =2.6 nM). | ||||
| GC79111 | CK2-TN03 | 313226-24-3 | >98.00% | |
CK2-TN03 is an ATP-competitive casein kinase 2 ( CK2 ) inhibitor, with an IC 50 of 165 nM and a K i of 20 nM. | ||||
