BH3 mimetic
Antitumor effect of TW-37, a BH3 mimetic in human oral cancer
... Despite BH3 mimetics targeting members of Bcl-2 family have received much attention for the recent success of cancer treatments, particularly hematological malignan- cies, single drug BH3 mimetic ...
8
Small-molecule BH3 mimetic and pan-Bcl-2 inhibitor AT-101 enhances the antitumor efficacy of cisplatin through inhibition of APE1 repair and redox activity in non-small-cell lung cancer
... Figure 14 a scheme of possible mechanisms by which aT-101 enhances the anticancer activity of cDDP in nsclc. aT-101 is a Bh3 mimetic and pan inhibitor of Bcl-2 and cDDP acts as a Dna intercalator. cDDP can ...
24
Treatment of B RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimetic
... B-RAF is frequently mutated in solid tumors, resulting in activation of the MEK/ERK signaling pathway and ultimately tumor cell growth and survival. MEK inhibition in these cells results in cell cycle arrest and cytosta- ...
10
The BH3 mimetic drug ABT-737 induces apoptosis and acts synergistically with chemotherapeutic drugs in thyroid carcinoma cells
... termed BH3 mimetics [23, 35]. BH3 mimetic drugs, such as ABT-737, are due to counter apoptotic blocks by binding to anti-apoptotic proteins like BCL-2, BCL-xL and BCL-w [23, ...
12
γ Secretase inhibition promotes cell death, Noxa upregulation, and sensitization to BH3 mimetic ABT 737 in human breast cancer cells
... a BH3- mimetic inhibitor of additional antiapoptotic proteins, such as Bcl-2 and Bcl-xL, leads to both a synergistic apoptotic response in breast cancer cells and to an inhibitory effect on mammosphere ...
15
Cell death induction by the BH3 mimetic GX15-070 in thyroid carcinoma cells
... obvious: there was no BAX expression and a low BAK expression in FTC238 cells and C643 cells which were both sensitive to GX15-070 (IC50 values of 0.048 μM and 0.049 μM) and a high BAX expression in insensitive RO82W and ...
14
The deubiquitinating enzyme OTUD1 antagonizes BH3-mimetic inhibitor induced cell death through regulating the stability of the MCL1 protein
... In the present study, we screened a deubiquitinating enzyme expression library to identify the DUBs that regulate MCL1 stability. We found that OTU domain containing protein 1 (OTUD1) regulated the stabil- ity of MCL1 in ...
11
Targeting ERK1/2-bim signaling cascades by BH3-mimetic ABT-737 as an alternative therapeutic strategy for oral cancer
... how BH3 mimetics promote Bcl-2 family-mediated apoptosis in human oral cancer cells are still largely unknown, previous studies have established the role of the ERK1/2 signaling pathway in regulating cancer cell ...
17
The BH3-mimetic gossypol and noncytotoxic doses of valproic acid induce apoptosis by suppressing cyclin-A2/Akt/FOXO3a signaling
... To address these issues, we analyzed the combined effects of GOS with VPA, suberoylanilide hydroxamic acid SAHA, also known as Vorinostat or tubacin, and explored the potential action me[r] ...
15
Treatment with a BH3 mimetic overcomes the resistance of latency III EBV (+) cells to p53 mediated apoptosis
... P53 inactivation is often observed in Burkitt’s lymphoma (BL) cells due to mutations in the p53 gene or overexpression of its negative regulator, murine double minute-2 (MDM2). This event is now considered an essential ...
9
BH3 mimetic ABT-263 enhances the anticancer effects of apigenin in tumor cells with activating EGFR mutation
... a BH3-only member that has been proposed to play a key role in the control of apoptosis and initiation of apoptotic pathways ...the BH3 mimetics of ABT- 263 or ABT-737 sensitivity [53, ...
18
The trans-membrane domain of Bcl-2 a, but not its hydrophobic cleft, is a critical determinant for efficient IP
... putative BH3 motifs within the IP 3 R sequence (Figure ...a BH3-dependent mechanism, involving an interaction between the hydrophobic cleft of Bcl-Xl and two BH3 motifs in the C-term Dom of IP 3 R ...
17
Mechanistic rationale for MCL1 inhibition during androgen deprivation therapy
... The BH3-mimetic Obatoclax induces apoptosis and decreases MCL1 expression in androgen-sensitive PCa cells, while castration-resistant PCa cells are less sensitive and react with an upregulation of MCL1 ...
18
FACTORS INFLUENCING MALAYSIAN TAXI DRIVERS BEHAVIORAL INTENTION TO ADOPT MOBILE TAXI APPLICATION
... Licensed under Creative Common Page 149 The measurement items for this survey were adapted from previous research where their psychometric properties have been established. Multiple items for each construct organized in ...
18
Mimetic desire and scapegoat mechanism in sport
... He argued that human beings are mimetic beings, feel- ing an urge to create art that reflects and represents reality. In Poetics he said: “Man is distinguished from other life-forms by his capacity for imitation” ...
9
Type I Interferon Mimetics Bypass Vaccinia Virus Decoy Receptor Virulence Factor for Protection of Mice against Lethal Infection
... ␣ mimetic similarly possessed potent adjuvant effects against BSA, a weak ...mask mimetic adjuvancy, so the rationale behind the use of BSA as a test of adjuvancy was its weak immunoge- ...IFN-␣1 ...
7
Hypoxia mimetic agents for ischemic stroke
... Every year stroke claims more than 6 million lives worldwide. The majority of them are ischemic stroke. Small molecule-based therapeutics for ischemic stroke has attracted a lot of attention, but none has been shown to ...
13
Mimetic desire in autism spectrum disorder
... Mimetic desire (MD), the spontaneous propensity to pursue goals that others pursue, is a case of social influence that is believed to shape preferences. Autism spectrum disorder (ASD) is defined by both atypical ...
6
Structural Insight into BH3 Domain Binding of Vaccinia Virus Antiapoptotic F1L
... the BH3-only proteins (9). The BH3-only proteins include Puma, Noxa, Bid, Bmf, Bik, Bad, Hrk, and Bim; they func- tion by directly activating Bak and Bax or by sequestering and neutralizing the ...
11
Evidence for Involvement of BH3-Only Proapoptotic Members in Adenovirus-Induced Apoptosis
... for BH3- only proteins were obtained from various commercial sources: rabbit polyclonal BIM (Pharmingen), NOXA, BIK, BID, and BNIP3-L (Santa Cruz Biotechnol- ogy), UREB1/LASU1/MULE (MCL1 ubiquitin E3 ligase) ...
10