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(114)
- Pyroptosis(37)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(154)
- Bcl-xL(8)
- c-RET(8)
- IAP(31)
- KEAP1-Nrf2(81)
- MDM2(12)
- p53(145)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(12)
- Thymidylate Synthase(10)
- TNF-α(189)
- Other Apoptosis(877)
- Apoptosis Detection
- Caspase Substrate
- APC(6)
- PD-1/PD-L1 interaction(106)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(23)
- Cuproptosis(4)
Products Related to Apoptosis(3030)
- GN10727Forsythoside BCAS: 81525-13-5Purity: >98.00%
Forsythoside B는 전통 중국 의학 식물인 Forsythia suspensa의 잎에서 분리된 페닐에탄올 글리코사이드입니다. 이 물질은 여러 가지 생물학적 활성을 가지고 있고 염증성 질환을 치료하고 혈액 순환을 촉진하는 데 사용할 수 있다.
- GN10797TangeretinCAS: 481-53-8Purity: >98.00%
Tangeretin은 감귤 껍질에서 추출한 천연 다중 메톡시화된 플라보노이드 화합물로 노치-1 억제제로 작용한다.
- GP10028tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]Purity: >98%
P53 binding protein fragment
- GC12407Z-IETD-FMKCAS: 210344-98-2Purity: >98.00%
Z-IETD-FMK(Z-IE(OMe)TD(OMe)-FMK)은 선택성이 있고 세포를 통과할 수 있는 캄파스-8 억제제이다.
- GC13473Lenalidomide hemihydrateCAS: 847871-99-2Purity: >99.50%
탈리도마이드의 유도체인 레날리도마이드 반수화물(CC-5013 반수화물)은 분자 접착제 역할을 합니다. 레날리도마이드 반수화물은 경구 활성 면역 조절제입니다. 레날리도마이드 반수화물(CC-5013 hemihydrate)은 유비퀴틴 E3 리가제 세레블론(CRBN)의 리간드이며, CRBN-CRL4 유비퀴틴 리가제에 의해 두 개의 림프계 전사 인자 IKZF1 및 IKZF3의 선택적 유비퀴틴화 및 분해를 유발합니다. 레날리도마이드 반수화물(CC-5013 반수화물)은 다발성 골수종을 포함한 성숙한 B 세포 림프종의 성장을 특이적으로 억제하고 T 세포에서 IL-2 방출을 유도합니다.
- GC15036Raltegravir potassium saltCAS: 871038-72-1Purity: >98.00%
Raltegravir(MK 0518) 칼륨은 HIV 감염 치료에 사용되는 강력한 통합효소(IN) 억제제입니다.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GN10717 | Sanguinarine | 2447-54-3 | >98.00% | |
| GN10727 | Forsythoside B | 81525-13-5 | >98.00% | |
Forsythoside B는 전통 중국 의학 식물인 Forsythia suspensa의 잎에서 분리된 페닐에탄올 글리코사이드입니다. 이 물질은 여러 가지 생물학적 활성을 가지고 있고 염증성 질환을 치료하고 혈액 순환을 촉진하는 데 사용할 수 있다. | ||||
| GN10732 | Oroxin B | 114482-86-9 | >99.50% | |
| GN10733 | Carnosic acid | 3650-09-7 | >97.00% | |
| GN10734 | Polyphyllin B | 76296-72-5 | >98% | |
| GN10740 | Tetrahydropalmatine | 10097-84-4 | >99.00% | |
| GN10741 | Garcinone D | 107390-08-9 | >98.00% | |
| GN10751 | Dictamnine | 484-29-7 | >98.50% | |
| GN10776 | Obacunone | 751-03-1 | >98.00% | |
| GN10778 | Picroside II | 39012-20-9 | >95.00% | |
| GN10783 | (R) Ginsenoside Rh2 | 112246-15-8 | >98.00% | |
| GN10788 | Cucurbitacin IIb | 50298-90-3 | >98.00% | |
| GN10797 | Tangeretin | 481-53-8 | >98.00% | |
Tangeretin은 감귤 껍질에서 추출한 천연 다중 메톡시화된 플라보노이드 화합물로 노치-1 억제제로 작용한다. | ||||
| GN10800 | 20(S)-NotoginsenosideR2 | 80418-25-3 | >98.00% | |
| GN10802 | Brazilin | 474-07-7 | >98.00% | |
| GN10805 | Protopanaxdiol | 30636-90-9 | >98.00% | |
| GP10028 | tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus] | - | >98% | |
P53 binding protein fragment | ||||
| GP10036 | p53 tumor suppressor fragment | - | >98% | |
Regulates cell cycle | ||||
| GC12407 | Z-IETD-FMK | 210344-98-2 | >98.00% | |
Z-IETD-FMK(Z-IE(OMe)TD(OMe)-FMK)은 선택성이 있고 세포를 통과할 수 있는 캄파스-8 억제제이다. | ||||
| GC16990 | Z-LEHD-FMK | 210345-04-3 | >98.00% | |
Z-LEHD-FMK는 비가역적 시스테인-9 억제제이다. | ||||
| GC11908 | Cisplatin | 15663-27-1 | >98.00% | |
Cisplatin은 백금 함유 항암제로 다양한 고형 악성 종양의 치료에 가장 일반적으로 사용되는 세포 독성 약물 중 하나이다. | ||||
| GC13473 | Lenalidomide hemihydrate | 847871-99-2 | >99.50% | |
탈리도마이드의 유도체인 레날리도마이드 반수화물(CC-5013 반수화물)은 분자 접착제 역할을 합니다. 레날리도마이드 반수화물은 경구 활성 면역 조절제입니다. 레날리도마이드 반수화물(CC-5013 hemihydrate)은 유비퀴틴 E3 리가제 세레블론(CRBN)의 리간드이며, CRBN-CRL4 유비퀴틴 리가제에 의해 두 개의 림프계 전사 인자 IKZF1 및 IKZF3의 선택적 유비퀴틴화 및 분해를 유발합니다. 레날리도마이드 반수화물(CC-5013 반수화물)은 다발성 골수종을 포함한 성숙한 B 세포 림프종의 성장을 특이적으로 억제하고 T 세포에서 IL-2 방출을 유도합니다. | ||||
| GC15035 | PM00104 | 308359-57-1 | >98% | |
Potent antimyeloma agent | ||||
| GC15036 | Raltegravir potassium salt | 871038-72-1 | >98.00% | |
Raltegravir(MK 0518) 칼륨은 HIV 감염 치료에 사용되는 강력한 통합효소(IN) 억제제입니다. | ||||
