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 (87 a)は強力なp53活性化剤であり、sc150の値は0.05 mm未満である。
- GC73225ROS-generating agent 1CAS: 2369030-41-9Purity: >99.00%
ROS-generating agent 1 (compound 2c)はsec-498残基を共有修飾してrosを生成する。
- GC73272PARP-1-IN-3CAS: 2976342-33-1Purity: >99.00%
PARP-1-IN-3ベンズアミド誘導体は強力なPARP-1阻害剤であり、PARP-1とPARP-2のIC 50値はそれぞれ0.25 nMと2.34 nMである。
- GC73274EGFR T790M/L858R-IN-2CAS: 2955607-40-4Purity: >99.00%
EGFR T790M/L858R-IN-2は、egfrt790m / l858r、egfr wtに対するic50値3.5,1290 nmの強力かつ選択的なegfrt790m / l858r阻害剤である。
- GC73288CDK8-IN-13CAS: 918523-75-8Purity: >98.00%
CDK8-IN-13は有力で、選択的で、経口活性のCDK8阻害剤であり、IC 50 値は51.9nMである。
- GC73309Anti-melanoma agent 1CAS: 2418579-17-4Purity: >99.00%
Anti-melanoma agent 1 (compound 5m)は抗メラノーマ剤であり、細胞のアポトーシスを誘導する。
- GC73313PI3Kα-IN-9CAS: 2715287-67-3Purity: >99.00%
PI3Kα-IN-9(化合物27)は選択性、長期効果及び経口活性のPI 3 Kα阻害剤であり、PI 3 Kα、PI 3 Kγ、PI 3 Kδ及びPI 3 Kβに対するIC 50値はそれぞれ4.4、128、146及び153 nMである。
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73159 | KTX-582 | 2573298-13-0 | >98.00% | |
KTX-582は有効なIRAK 4分解剤であり、IRAK 4とイカロスのDC 50値はそれぞれ4 nMと5 nMである。 | ||||
| GC73166 | U7D-1 | - | >99.00% | |
U7D-1は、強力かつ選択的なusp7(ユビキチン特異的プロテアーゼ7)protac分解剤であり、rs4におけるdc50は33 nmである。 | ||||
| GC73168 | p53 Activator 3 | 2636839-90-0 | >95.00% | |
p53 Activator 3 (87 a)は強力なp53活性化剤であり、sc150の値は0.05 mm未満である。 | ||||
| GC73188 | SFI003 | 2361332-90-1 | >99.00% | |
SFI003は、srsf3 / dhcr24 / ros軸を介してcrc細胞のアポトーシスを促進するsrsf3阻害剤であり、in vitroおよびin vivoの両方で強力な抗腫瘍効果を示す。 | ||||
| GC73199 | M47 | 890808-56-7 | >99.00% | |
M47は、クリプトクロム1 (cry1)を選択的に不安定化させ、核内のcry1の分解を増加させる小分子である。 | ||||
| GC73210 | MTR-106 | 1639357-93-9 | >99.00% | |
MTR-106は強力な経口活性G-四鎖体安定剤とRNAポリメラーゼI阻害剤である。 | ||||
| GC73212 | TH-6 | 3031349-25-1 | >95.00% | |
TH-6は強力なHDAC阻害剤であり、HDAC 1、HDAC 2、HDAC 3、HDAC 6、HDAC 8のIC 50はそれぞれ0.115、0.135、0.242、0.138、2.120µMである。 | ||||
| GC73220 | LSD1-IN-24 | 4734-59-2 | >99.00% | |
LSD1-IN-24(複合3 s)は選択LSD1剤IC50 = 0.247μM。 | ||||
| GC73225 | ROS-generating agent 1 | 2369030-41-9 | >99.00% | |
ROS-generating agent 1 (compound 2c)はsec-498残基を共有修飾してrosを生成する。 | ||||
| GC73228 | MS78 | 3034773-00-4 | >99.00% | |
MS78はp 53腫瘍抑制タンパク質をアセチル化したアセチル化標的ブロック(AceTAC)である。 | ||||
| GC73232 | PRDX1-IN-1 | - | >98.00% | |
PRDX1-IN-1はPRDX 1の選択的阻害剤であり、IC 50値は0.164μMである。 | ||||
| GC73234 | MY-673 | 2944459-96-3 | >98.00% | |
MY-673は、微小管タンパク質の重合を抑制するコルヒチン結合部位抑制剤(CBSI)である。 | ||||
| GC73237 | BWA-522 | 3042820-12-9 | >99.00% | |
BWA-522は、AR-FLおよびAR-V 7に顕著な分解作用を有する低分子タンパク質標的キメラ(PROTACs)を経口投与する。 | ||||
| GC73243 | Nrf2-IN-3 | 6325-13-9 | >99.00% | |
Nrf2-IN-3(化合物r16)はnrf2阻害剤である。 | ||||
| GC73268 | PH14 | - | >99.00% | |
PH14はIC50の価値観でデュアルPI3K性もあり/ HDAC阻害薬と20.3 nMと24.5 nM PI3KαHDAC3、。 | ||||
| GC73269 | ABBV-467 | 2287186-66-5 | >99.00% | |
ABBV-467は選択的MCL-1阻害剤(Ki:<0.01 nM)である。 | ||||
| GC73272 | PARP-1-IN-3 | 2976342-33-1 | >99.00% | |
PARP-1-IN-3ベンズアミド誘導体は強力なPARP-1阻害剤であり、PARP-1とPARP-2のIC 50値はそれぞれ0.25 nMと2.34 nMである。 | ||||
| GC73274 | EGFR T790M/L858R-IN-2 | 2955607-40-4 | >99.00% | |
EGFR T790M/L858R-IN-2は、egfrt790m / l858r、egfr wtに対するic50値3.5,1290 nmの強力かつ選択的なegfrt790m / l858r阻害剤である。 | ||||
| GC73275 | PD-L1-IN-2 | 2894733-91-4 | >98.00% | |
PD-L1-IN-2はpd-l1を阻害する潜在的な腫瘍免疫剤である。 | ||||
| GC73288 | CDK8-IN-13 | 918523-75-8 | >98.00% | |
CDK8-IN-13は有力で、選択的で、経口活性のCDK8阻害剤であり、IC 50 値は51.9nMである。 | ||||
| GC73294 | F5446 | 2304465-89-0 | >99.00% | |
F5446(化合物1)は、SUV 39 H 1金属転移酵素の選択的小分子阻害剤である。 | ||||
| GC73309 | Anti-melanoma agent 1 | 2418579-17-4 | >99.00% | |
Anti-melanoma agent 1 (compound 5m)は抗メラノーマ剤であり、細胞のアポトーシスを誘導する。 | ||||
| GC73311 | STAT3-IN-13 | 2248552-86-3 | >99.00% | |
STAT3-IN-13(化合物6 f)は強力なSTAT 3阻害剤である。 | ||||
| GC73313 | PI3Kα-IN-9 | 2715287-67-3 | >99.00% | |
PI3Kα-IN-9(化合物27)は選択性、長期効果及び経口活性のPI 3 Kα阻害剤であり、PI 3 Kα、PI 3 Kγ、PI 3 Kδ及びPI 3 Kβに対するIC 50値はそれぞれ4.4、128、146及び153 nMである。 | ||||
