Codelivery of BCL2 and MCL1 Inhibitors Enabled by Phenylboronic Acid‐Functionalized Polypeptide Nanovehicles for Synergetic and Potent Therapy of Acute Myeloid Leukemia
Sign Up to like & getrecommendations! Published in 2023 at "Advanced Science"
DOI: 10.1002/advs.202204866
Abstract: Acute myeloid leukemia (AML) is the most refractory hematologic malignancy characterized by acute onset, rapid progression, and high recurrence rate. Here, codelivery of BCL2 (ABT199) and MCL1 (TW37) inhibitors using phenylboronic acid‐functionalized polypeptide nanovehicles to… read more here.
Keywords: bcl2; mcl1; phenylboronic acid; acid functionalized ... See more keywords
The deubiquitinating enzyme USP20 regulates the stability of the MCL1 protein.
Sign Up to like & getrecommendations! Published in 2022 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2022.01.019
Abstract: Chemoresistance is a major obstacle faced by oesophageal cancer patients and is synonymous with a poor prognosis. MCL1 is a pivotal member of the anti-apoptotic Bcl-2 protein family, which has been found to play an… read more here.
Keywords: enzyme usp20; usp20 regulates; mcl1; deubiquitinating enzyme ... See more keywords
SUMOylation of MCL1 protein enhances its stability by regulating the ubiquitin-proteasome pathway.
Sign Up to like & getrecommendations! Published in 2020 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2020.109686
Abstract: In cancers, apoptosis evasion through dysregulation of pro-apoptotic and anti-apoptotic intracellular signals is a recurring event. Accordingly, selective inhibition of specific proteins represents an exciting therapeutic opportunity. Myeloid cell leukemia 1 (MCL1) is an anti-apoptotic… read more here.
Keywords: protein; sumoylation mcl1; proteasome pathway; mcl1 ... See more keywords
MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of Mitochondrial Oxidative Phosphorylation.
Sign Up to like & getrecommendations! Published in 2017 at "Cell metabolism"
DOI: 10.1016/j.cmet.2017.09.009
Abstract: Most patients with advanced triple-negative breast cancer (TNBC) develop drug resistance. MYC and MCL1 are frequently co-amplified in drug-resistant TNBC after neoadjuvant chemotherapy. Herein, we demonstrate that MYC and MCL1 cooperate in the maintenance of… read more here.
Keywords: chemotherapy; myc mcl1; mcl1; breast cancer ... See more keywords
Disruption of conserved polar interactions causes a sequential release of Bim mutants from the canonical binding groove of Mcl1.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.04.243
Abstract: Mcl1 is an important anti-apoptotic member of the Bcl2 family proteins that are upregulated in several cancer malignancies. The canonical binding groove (CBG) located at the surface of Mcl1 exhibits a critical role in binding… read more here.
Keywords: causes sequential; disruption conserved; mcl1; conserved polar ... See more keywords
From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00455
Abstract: Protein-protein interactions (PPIs) have emerged as significant targets for therapeutic development, owing to their critical nature in diverse biological processes. An ideal PPI-based target is the protein myeloid cell leukemia 1 (MCL1), a critical prosurvival… read more here.
Keywords: protein; cell leukemia; myeloid cell; mcl1 ... See more keywords
Expression Ratios of the Antiapoptotic BCL2 Family Members Dictate the Selective Addiction of Kaposi’s Sarcoma-Associated Herpesvirus-Transformed Primary Effusion Lymphoma Cell Lines to MCL1
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Virology"
DOI: 10.1128/jvi.01360-22
Abstract: Primary effusion lymphoma (PEL) is caused by Kaposi’s sarcoma-associated herpesvirus. We showed previously that PEL cell lines require the antiapoptotic protein MCL1 for survival but not the other BCL2 family proteins. ABSTRACT Kaposi’s sarcoma-associated herpesvirus… read more here.
Keywords: bcl2 family; mcl1; family; primary effusion ... See more keywords
Abstract 2978: The utilization of a human MCL1 knockin mouse suggests that reductions in B-cells and monocytes may serve as clinically relevant pharmacodynamic markers of MCL1 inhibition
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-2978
Abstract: The development of small-molecule inhibitors targeting pro-survival BCL-2 family members, such as MCL1 and BCL-2, is an attractive approach for the treatment of cancer. AMG 176 is a potent and selective first-in-class MCL1 inhibitor currently… read more here.
Keywords: mcl1 knockin; amg 176; human mcl1; mcl1 ... See more keywords
Abstract 3972: Combined inhibition of MCL1 and BCL-2 with AMG 176 and venetoclax induces anti-tumor effects in primary patient samples and models of acute myeloid leukemia
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-3972
Abstract: Acute myeloid leukemia (AML) is a heterogeneous hematological malignancy involving the clonal expansion of immature myeloid cells. Dysregulated expression of the BCL-2 family of proteins has been implicated in AML pathogenesis. Specifically, the anti-apoptotic family… read more here.
Keywords: combination; venetoclax; amg 176; inhibition ... See more keywords
Abstract 6218: Discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor
Sign Up to like & getrecommendations! Published in 2020 at "Cancer Research"
DOI: 10.1158/1538-7445.am2020-6218
Abstract: MCL1 inhibitors are an emerging class of therapeutics targeting key protein-protein interactions between MCL1 and BH3 domain containing pro-apoptotic BCL-2 family members. Several MCL1 inhibitors have entered clinical trials including AMG 176, currently in Phase… read more here.
Keywords: preclinical evaluation; amg 397; mcl1 inhibitor; discovery preclinical ... See more keywords
Abstract 6147: MCL1 inhibitor PRT1419 demonstrates anti-tumor activity in PBRM1-altered clear cell renal cancer and synergizes with standard of care agents
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-6147
Abstract: Induced myeloid leukemia cell differentiation protein (MCL1) is a member of the B-cell lymphoma-2 (BCL2) family of apoptosis regulators, which plays a critical role in maintaining cellular homeostasis and promoting cancer cell survival. Increased expression… read more here.
Keywords: cell; mcl1; pbrm1; prt1419 ... See more keywords