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)
- GC72931HTH-01-091 TFAPurity: >98.00%
HTH-01-091 TFA은 10.5 nM의 IC50으로 강력하고 선택적인 모체 배아성 루신 지퍼 키나아제 (MELK) 억제제이다.
- GC72991(Rac)-LisaftoclaxCAS: 2651980-10-6Purity: >98.00%
(Rac)-Lisaftoclax Rac-APG-2575는 혈액 악성 종양 연구 CN112898295A에 사용할 수있는 Bcl-2 억제제입니다.
- GC73025Teprasiran sodiumCAS: 2169310-72-7Purity: >90.00%
Teprasiran sodium 는 급성 신장 손상 (AKI) 의 기초인 p53이 매개하는 세포의 사멸을 일시적으로 억제하는 작은 간섭 RNA입니다.
- GC73093Custirsen sodiumPurity: >98.00%
Custirsen sodium 클러스터단백질의 생성을 억제한다. 클러스터단백질은 일종의 항시체단백질로서 화학료법후 상향조정하고 치료내약성을 부여한다.
- GC73109Danvatirsen sodiumPurity: >97.00%
Danvatirsen sodium은 잠재적인 항암 활성을 가진 STAT3를 타겟팅하는 안티센스 올리고뉴클레오타이드입니다.
- GC73112JPS014 TFAPurity: >98.00%
JPS014 TFA은 벤조메틸아미드 기반 Von Hippel-Lindau(VHL) E3 연결효소 단백질 가수분해 표적접합체(PROTAC)다.
- GC73129SIAIS164018 hydrochloridePurity: >99.00%
SIAIS164018 hydrochloride은 PROTAC-based ALK 및 EGFR 분해제로 ALK 및 ALK G1202R의 경우 각각 2.5 nM 및 6.6 nM의 IC50 값을 갖는다.
- GC73138PBENZ-DBRMDCAS: 1454662-41-9Purity: >99.00%
PBENZ-DBRMD 는 강력한 요오드 트리알칼리 탈요오드 효소 3형(DIO3) 억제제입니다.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC72915 | (R)-MRT199665 | - | >98.00% | |
(R)-MRT199665는 MRT199665의 이기체입니다. | ||||
| GC72924 | PD173952 | 305820-75-1 | >99.00% | |
PD173952는 Lyn, Abl 및 Csk에 대해 각각 0.3, 1.7 및 6.6 nM의 IC50s를 갖는 tyrosine kinases 억제제이다. | ||||
| GC72928 | DB818 | 790241-43-9 | >98.00% | |
DB818는 호메오박스 A9 (HOXA9)의 강력한 억제제이다. | ||||
| GC72929 | DB818 dihydrochloride | - | - | |
DB818 dihydrochloride 는 DB818의 디클로르 소금 형태입니다. | ||||
| GC72931 | HTH-01-091 TFA | - | >98.00% | |
HTH-01-091 TFA은 10.5 nM의 IC50으로 강력하고 선택적인 모체 배아성 루신 지퍼 키나아제 (MELK) 억제제이다. | ||||
| GC72933 | LQZ-7F | 354543-09-2 | >97.00% | |
survivin dimerization inhibitor인 LQZ-7F는 자발적 apoptosis를 유도하며 전립선암세포에서 Docetaxel과 시너지 효과를 낸다. | ||||
| GC72944 | MMRi64 | 430458-66-5 | >98.00% | |
MMRi64Mdm2-MdmX 상호작용을 파괴한다. | ||||
| GC72971 | INCB3619 | 791826-72-7 | >98.00% | |
INCB3619ADAM10과 ADAM17의 IC50은 각각 22nM과 14nM이다. | ||||
| GC72985 | Z-LEVD-FMK | 1135688-25-3 | >98.50% | |
Z-LEVD-FMK는 세포 투과성 카스파제4억제제이다. | ||||
| GC72991 | (Rac)-Lisaftoclax | 2651980-10-6 | >98.00% | |
(Rac)-Lisaftoclax Rac-APG-2575는 혈액 악성 종양 연구 CN112898295A에 사용할 수있는 Bcl-2 억제제입니다. | ||||
| GC72994 | RAPTA-C | 372948-28-2 | >99.00% | |
RAPTA-C (류 은이 (η 6-p-cymene) Cl2 (pta)) 항암과 anti-angiogenic 에이전트는 역할을 한다. | ||||
| GC73002 | Ganglioside GD3 diammonium | - | >98.00% | |
Ganglioside GD3 diammonium 는 산성 칼집 당지의 일종이다. | ||||
| GC73016 | AZD4877 | 758722-49-5 | >98.00% | |
AZD4877는 Ispinesib에 대한 또 다른 isostere 이며 2 nM의 IC50을 가진 kinesin spindle protein (Eg5) 억제제이기도 합니다. | ||||
| GC73025 | Teprasiran sodium | 2169310-72-7 | >90.00% | |
Teprasiran sodium 는 급성 신장 손상 (AKI) 의 기초인 p53이 매개하는 세포의 사멸을 일시적으로 억제하는 작은 간섭 RNA입니다. | ||||
| GC73077 | ARI-1 | - | >99.00% | |
ARI-1은 수용체 티로신 인산화 유사 고아 수용체 1 (ROR1) 억제제의 억제제이다. | ||||
| GC73093 | Custirsen sodium | - | >98.00% | |
Custirsen sodium 클러스터단백질의 생성을 억제한다. 클러스터단백질은 일종의 항시체단백질로서 화학료법후 상향조정하고 치료내약성을 부여한다. | ||||
| GC73109 | Danvatirsen sodium | - | >97.00% | |
Danvatirsen sodium은 잠재적인 항암 활성을 가진 STAT3를 타겟팅하는 안티센스 올리고뉴클레오타이드입니다. | ||||
| GC73112 | JPS014 TFA | - | >98.00% | |
JPS014 TFA은 벤조메틸아미드 기반 Von Hippel-Lindau(VHL) E3 연결효소 단백질 가수분해 표적접합체(PROTAC)다. | ||||
| GC73118 | EB1 | 42951-68-8 | >99.00% | |
EB1은 kinases의 억제와 MNK IC50s. 69의 μ M (MNK1)와 9. 4 μ M (MNK2) 입니다. | ||||
| GC73129 | SIAIS164018 hydrochloride | - | >99.00% | |
SIAIS164018 hydrochloride은 PROTAC-based ALK 및 EGFR 분해제로 ALK 및 ALK G1202R의 경우 각각 2.5 nM 및 6.6 nM의 IC50 값을 갖는다. | ||||
| GC73133 | Misetionamide | 856785-75-6 | >99.00% | |
Misetionamide은 구강 옥사티아진 유사 화합물이다. | ||||
| GC73136 | VPC-70063 | 13571-44-3 | >99.00% | |
VPC-70063 는 강력한 Myc-Max 억제제로서 Myc-Max 전사 활성을 억제하는 IC50 값은 8.9 μM입니다. | ||||
| GC73138 | PBENZ-DBRMD | 1454662-41-9 | >99.00% | |
PBENZ-DBRMD 는 강력한 요오드 트리알칼리 탈요오드 효소 3형(DIO3) 억제제입니다. | ||||
| GC73146 | Sonrotoclax | 2383086-06-2 | >99.00% | |
Sonrotoclax은 강력하고 구강 활성 Bcl2억제제입니다. | ||||
