GLPBio

Apoptosis

Read More about this category

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

Products Related to Apoptosis(3381)

  • GC70114 structure
    GC70114Venetoclax-d8
    CAS: 1257051-06-1
    Purity: >99.50%

    Venetoclax-d8는 Venetoclax의 데우테르화 물질입니다. Venetoclax (ABT-199; GDC-0199)는 선택적이고 경구 효과가 있는 Bcl-2 억제제로, Ki 값은 0.01 nM보다 작습니다. Venetoclax는 자가포식을 유도할 수 있습니다.

  • GC70137 structure
    GC70137Vudalimab
    CAS: 2329669-72-7
    Purity: >99.00%

    Vudalimab는 효과적인 PD-1 및 CTLA-4 이중 억제제로, 완전 인간화된 이중 특이 단일 클론 항체입니다. Vudalimab는 면역 점검점 수용 체 PD-1 및 CTLA-4를 대상으로 하여 종양 선택적 T 세포 활성을 촉진합니다.

  • GC70145 structure
    GC70145WL12
    Purity: >98.00%

    WL12는 특이적으로 PD-L1 (프로그램된 세포사멸 리간드 1) 결합 펩타이드를 대상으로하는 타겟팅 프로그래밍 죽음 랜딩입니다. WL12는 다양한 방법으로 방사성 핵종을 마크하여 방사성 추적제를 생성하고 종양의 PD-L1 발현을 평가할 수 있습니다.

  • GC70242 structure
    GC70242Thymocartin TFA

    Thymocartin TFA는 티모카르틴의 TFA 소금 형태이다.

  • GC70257 structure
    GC70257Gallium maltolate
    CAS: 108560-70-9
    Purity: >98.00%

    Gallium maltolate (GAM) 는 항암 및 항염 활성을 가진 세포 사멸 유도제입니다.

  • GC70289 structure
    GC70289AC-VEID-CHO TFA
    Purity: >98.00%

    AC-VEID-CHO TFA은 펩타이드 유래 caspase 저해제이며 IC50 값이 각각 16.2 nM, 13.6 nM, 162.1 nM인 Caspase-6, Caspase-3, Caspase-7에 대한 억제 효능을 가지고 있다.

  • GC70298 structure
    GC70298Peginterferon beta-1a
    CAS: 1211327-92-2

    Peginterferon β-1a는 최초의 페질화된 인터페론 베타-1a 분자이다.

  • GC70332 structure
    GC70332(+)-Erinacin A
    CAS: 156101-08-5
    Purity: >99.00%

    (+)-Erinacin A 는 버섯 원숭이머리버섯에서 분리 될 수있는 항암 화합물입니다.

  • GC70388 structure
    GC70388Justicidin B
    CAS: 17951-19-8
    Purity: >99.00%

    Justicidin B 는 강력한 항암 나프타와 시체 촉진제이다.

  • GC70411 structure
    GC70411Nrf2-Activator-12G
    CAS: 1554271-18-9
    Purity: >99.00%

    Nrf2-Activator-12G (compd 12g) 는 Nrf2의 활성제입니다.

  • GC70418 structure
    GC70418Cipepofol
    CAS: 1637741-58-2
    Purity: >98.00%

    Cipepofol (Ciprool) 는 페놀 유도체를 대체하는 새로운 2,6-2 종으로, GABAA 수용체의 양변조 조절제이자 직접 흥분제이다.

  • GC70520 structure
    GC70520MIND4-17
    CAS: 345989-24-4
    Purity: >99.00%

    MIND4-17 Keap1의 C151 잔기를 공가로 수식하는 강력한 NRF2 활성제입니다.

  • GC70570 structure
    GC70570RH01386
    CAS: 301177-36-6
    Purity: >99.00%

    RH01386 는 내질망 스트레스 (ERS) 가 유도하는 베타세포 기능 장애와 사멸을 예방하고 사멸 촉진 유전자의 발현을 억제하는 소분자다.

  • GC70584 structure
    GC70584Actinomycin X2
    CAS: 18865-48-0
    Purity: >98.00%

    Actinomycin X2 (방선균소 V), 많은 스트렙토마이신에서 생성됩니다.

  • GC70658 structure
    GC70658C5 Lenalidomide
    CAS: 191732-70-4

    C5 Lenalidomide (레나도민 5'-아민) 는 일종의 샤를리도민 유사물로 TNF-α에서 나오는 강력한 억제제(LPS에서 자극하는 사람 PBMC에서 IC50=100μM)이다.

  • GC70659 structure
    GC706599-cis-Retinoic acid-d5
    Purity: >98.00%

    9-cis-Retinoic acid-d5 는 듀테륨 표기의 9-순식 비갑산이다.

  • GC70733 structure
    GC70733ABT-510 acetate
    CAS: 442526-87-6
    Purity: >99.00%

    ABT-510 acetate 는 상피성 난소암 원위동유전자 모델에서 세포의 사멸을 유도하고 난소종양의 성장을 억제하는 항혈관생성 TSP펩타이드(혈소판반응단백질-1 유사물)의 일종이다.

  • GC70742 structure
    GC70742Betamethasone-d5-1
    CAS: 2244574-92-1

    βmethasone-d5-1 듀테륨은 배타미송으로 표기되어 있다.

  • GC70753 structure
    GC70753PDK4-IN-1
    CAS: 2310262-10-1
    Purity: >98.00%

    PDK4-IN-1 는 안트라키논 유도체이자 강력한 경구 활성 아세톤산 탈수소 효소 효소 4 (PDK4) 억제제로서 IC50 값은 84nM입니다.

  • GC70756 structure
    GC70756Cytarabine-d2
    CAS: 40632-26-6
    Purity: >98.00%

    Cytarabine-d2 는 듀테륨 표기의 아당포닌이다.

  • GC70759 structure
    GC70759AQX-435
    CAS: 1619983-52-6
    Purity: >99.00%

    AQX-435 는 강력한 SHIP1 인산 효소 활성화제입니다.

  • GC70853 structure
    GC70853Broussochalcone A
    CAS: 99217-68-2
    Purity: >97.00%

    Broussochalcone A은 항 산화제와 Xanthine의 억제 Oxidase (IC50 = 2 μ M) 21, 무료로 급진적인 청소 활동이다.

  • GC70868 structure
    GC70868Nrf2 activator-3
    CAS: 2766570-23-2
    Purity: >98.00%

    Nrf2 activator-3은 강력한 Nrf2 활성제이다.

  • GC70875 structure
    GC70875RIPK1-IN-9
    CAS: 2682889-57-0

    RIPK1-IN-9 (실시례 45) 는 디하이드로나딘 화합물로서 강력하고 선택적인 RIPK1 억제제이다.