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)
- GC73355STAT3-SH2 domain inhibitor 1CAS: 2816059-41-1Purity: >98.50%
STAT3-SH2 domain inhibitor 1はSTAT 3(STAT 3-SH 2ドメイン)の強力なSrc相同性2(SH 2)ドメイン阻害剤であり、Kd値は1.57μMである。
- GC73371Enpp/Carbonic anhydrase-IN-2CAS: 2883495-39-2Purity: >99.00%
Enpp/Carbonic anhydrase-IN-2は強力なEnppと炭酸無水物酵素阻害剤であり、NPP 1、NPP 2、NPP 3、CA-IX、CA-XIIのIC 50はそれぞれ1.13、1.07、0.74、0.33、0.68である。
- GC73372(S)-SabutoclaxCAS: 1228178-73-1Purity: >98.00%
(S)-SabutoclaxS-BI-97 C 1は光学的に純粋な綿フェノール誘導体であり、アポトーシスB細胞リンパ腫/白血病-2 Bcl-2ファミリータンパク質に対する汎活性阻害剤である。
- GC73396PRMT6-IN-3CAS: 2890765-10-1Purity: >99.00%
PRMT6-IN-3(化合物25)は選択的PRMT 6阻害剤であり、IC 50値は192 nMである。
- GC73417CASP8-IN-1CAS: 1956368-39-0Purity: >98.00%
CASP8-IN-1(化合物63−R)はシステ天プロテアーゼ8(CASP 8)の選択的阻害剤であり、IC 50は0.7μMである。
- GC73424PRT062607 acetateCAS: 1370261-98-5Purity: >99.00%
PRT062607 acetateは経口で入手可能なsyk阻害剤(ic50: 1 nm)で、炎症とアポトーシスの誘導を阻害する。
- GC73428CWI1-2 hydrochlorideCAS: 2408590-37-2Purity: >98.00%
CWI1-2 hydrochlorideはIGF 2 BP 2を結合し、m 6 A修飾標的転写物との相互作用を抑制し、アポトーシスと分化を誘導するIGF 2 BP 2阻害剤である。
- GC73469Cereblon inhibitor 2CAS: 2639380-62-2Purity: >98.00%
Cereblon inhibitor 2 (compound 8)は、固形腫瘍、特に乳癌の研究に有用な脳の阻害剤である。
- GC73546PD-L1-IN-3CAS: 2953044-29-4Purity: >99.00%
PD-L1-IN-3(複合4 a)は対象とする複合免疫機能/ PD-L1 IC50値およびEC50値は4.97nM 2.70μM PD-L1や炎症を抑えるJurkat T細胞。
- GC73571Tubulin polymerization-IN-56CAS: 2966790-98-5Purity: >99.00%
Tubulin polymerization-IN-56インダゾール誘導体は強力な微小管タンパク質重合抑制剤であり、秋水仙サイトと相互作用することにより、細胞周期のブロックと細胞アポトーシスを引き起こす。
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73317 | ODN 1585 sodium | - | >93.00% | |
ODN 1585 sodiumはIFNとTNFαによる強力な誘導剤である。 | ||||
| GC73331 | BMS-37 | 1675202-20-6 | >98.00% | |
BMS-37はPD-1/PD-L 1免疫検査点阻害剤である。 | ||||
| GC73355 | STAT3-SH2 domain inhibitor 1 | 2816059-41-1 | >98.50% | |
STAT3-SH2 domain inhibitor 1はSTAT 3(STAT 3-SH 2ドメイン)の強力なSrc相同性2(SH 2)ドメイン阻害剤であり、Kd値は1.57μMである。 | ||||
| GC73371 | Enpp/Carbonic anhydrase-IN-2 | 2883495-39-2 | >99.00% | |
Enpp/Carbonic anhydrase-IN-2は強力なEnppと炭酸無水物酵素阻害剤であり、NPP 1、NPP 2、NPP 3、CA-IX、CA-XIIのIC 50はそれぞれ1.13、1.07、0.74、0.33、0.68である。 | ||||
| GC73372 | (S)-Sabutoclax | 1228178-73-1 | >98.00% | |
(S)-SabutoclaxS-BI-97 C 1は光学的に純粋な綿フェノール誘導体であり、アポトーシスB細胞リンパ腫/白血病-2 Bcl-2ファミリータンパク質に対する汎活性阻害剤である。 | ||||
| GC73374 | TD1092 | - | >99.00% | |
TD1092は、cIAP 1、cIAP 2、XIAPを分解することができる汎IAP分解剤である。 | ||||
| GC73396 | PRMT6-IN-3 | 2890765-10-1 | >99.00% | |
PRMT6-IN-3(化合物25)は選択的PRMT 6阻害剤であり、IC 50値は192 nMである。 | ||||
| GC73417 | CASP8-IN-1 | 1956368-39-0 | >98.00% | |
CASP8-IN-1(化合物63−R)はシステ天プロテアーゼ8(CASP 8)の選択的阻害剤であり、IC 50は0.7μMである。 | ||||
| GC73424 | PRT062607 acetate | 1370261-98-5 | >99.00% | |
PRT062607 acetateは経口で入手可能なsyk阻害剤(ic50: 1 nm)で、炎症とアポトーシスの誘導を阻害する。 | ||||
| GC73428 | CWI1-2 hydrochloride | 2408590-37-2 | >98.00% | |
CWI1-2 hydrochlorideはIGF 2 BP 2を結合し、m 6 A修飾標的転写物との相互作用を抑制し、アポトーシスと分化を誘導するIGF 2 BP 2阻害剤である。 | ||||
| GC73441 | EAPB 02303 | 1958290-51-1 | >99.00% | |
EAPB 02303は微小管破壊剤及び抑制剤である。 | ||||
| GC73469 | Cereblon inhibitor 2 | 2639380-62-2 | >98.00% | |
Cereblon inhibitor 2 (compound 8)は、固形腫瘍、特に乳癌の研究に有用な脳の阻害剤である。 | ||||
| GC73476 | MYC-RIBOTAC | - | >98.00% | |
MYC-RIBOTACはMYC内部のリボソーム進入部位(IRES)を標的とするリボヌクレアーゼキメラ(RIBOTAC)である。 | ||||
| GC73491 | RapaBlock | 2474076-02-1 | >98.00% | |
RapaBlockは、強力で非免疫抑制、および脳不透過性のFKBP 12リガンドである。 | ||||
| GC73501 | Wu-5 | 2630378-05-9 | >98.00% | |
Wu-5は、FLT 3とAMPK経路を抑制し、FLT 3-ITDの分解を誘導し、細胞アポトーシスを誘導するUSP 10阻害剤である。 | ||||
| GC73541 | PRMT5-IN-31 | - | >99.00% | |
PRMT5-IN-31(複合3 M)は選択PRMT5攻撃開始(IC50: 0.31μM)だった! | ||||
| GC73543 | FC-116 | 2417298-29-2 | >98.00% | |
FC-116はマウス腫瘍の成長を効果的に抑制する微小管タンパク質抑制剤である。 | ||||
| GC73546 | PD-L1-IN-3 | 2953044-29-4 | >99.00% | |
PD-L1-IN-3(複合4 a)は対象とする複合免疫機能/ PD-L1 IC50値およびEC50値は4.97nM 2.70μM PD-L1や炎症を抑えるJurkat T細胞。 | ||||
| GC73549 | LSD1-IN-27 | 2904571-94-2 | >98.00% | |
LSD1-IN-27(化合物5 ac)はLSD 1阻害剤(IC 50:13 nM)である。 | ||||
| GC73555 | PI3Kδ-IN-16 | 2766437-35-6 | >99.00% | |
PI3Kδ-IN-16はPI 3 Kδの強力な選択的阻害剤である。 | ||||
| GC73561 | YS-363 | 2470908-90-6 | >99.00% | |
YS-363は強力で選択的で経口活性のEGFR阻害剤であり、野生型とL 858 R変異型EGFRのIC 50はそれぞれ0.96 nMと0.67 nMである。 | ||||
| GC73567 | Os30 | 2998928-68-8 | >98.00% | |
Os30は強力な第4世代EGFR阻害剤であり、EGFRDel 19/T 790 M/C 797 S TKとEGFRL 858 R/T 790 M/C 797 S TKに対するIC 50値はそれぞれ18 nMと113 nMである。 | ||||
| GC73569 | MY-1076 | 3008262-76-5 | >99.00% | |
MY-1076はYAPの阻害剤である。 | ||||
| GC73571 | Tubulin polymerization-IN-56 | 2966790-98-5 | >99.00% | |
Tubulin polymerization-IN-56インダゾール誘導体は強力な微小管タンパク質重合抑制剤であり、秋水仙サイトと相互作用することにより、細胞周期のブロックと細胞アポトーシスを引き起こす。 | ||||
