ArticleMolecular pharmacology2019
CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax.
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Article in Molecular pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22citing papers in PubMed
1.5field-weighted citation impact, top 15% of its field
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Who cites it
22 citing papers in PubMed, 23 citations in OpenAlex.
- Cyclin-Dependent Kinase 5 Contributes to Bruton's Tyrosine Kinase Inhibitor Resistance via the IRE1α/XBP1 Axis in Mantle Cell Lymphoma.Research square · 2026Article
- Stabilization of cyclin D3 protein by CDKN1A (p21Cell communication and signaling : CCS · 2026Article
- Advantages of PROTACs in achieving selective degradation of homologous protein families.Beilstein journal of organic chemistry · 2026Review
- Emerging connectivity of programmed cell death pathways and pulmonary vascular remodelling during pulmonary hypertension.Journal of cellular and molecular medicine · 2024Review
- Increased MCL1 dependency leads to new applications of BH3-mimetics in drug-resistant neuroblastoma.British journal of cancer · 2023Article
- Current Advances and Future Strategies for BCL-2 Inhibitors: Potent Weapons against Cancers.Cancers · 2023Review
- Drugging Hijacked Kinase Pathways in Pediatric Oncology: Opportunities and Current Scenario.Pharmaceutics · 2023Review
- Synergistic activity of ABT-263 and ONC201/TIC10 against solid tumor cell lines is associated with suppression of anti-apoptotic Mcl-1, BAG3, pAkt, and upregulation of pro-apoptotic Noxa and Bax cleavage during apoptosis.American journal of cancer research · 2023Article
- Spirocyclic dimer SpiD7 activates the unfolded protein response to selectively inhibit growth and induce apoptosis of cancer cells.The Journal of biological chemistry · 2022Article
- Cdk5 drives formation of heterogeneous pancreatic neuroendocrine tumors.Oncogenesis · 2021Article
- Inhibitors, PROTACs and Molecular Glues as Diverse Therapeutic Modalities to Target Cyclin-Dependent Kinase.Cancers · 2021Review
- Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy.European journal of medicinal chemistry · 2021Article
- Combination Therapy of Navitoclax with Chemotherapeutic Agents in Solid Tumors and Blood Cancer: A Review of Current Evidence.Pharmaceutics · 2021Review
- Post-translational modifications of CDK5 and their biological roles in cancer.Molecular biomedicine · 2021Review
- Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.Bioorganic & medicinal chemistry letters · 2021Article
- Knockdown of Myeloid Cell Leukemia-1 by MicroRNA-101 Increases Sensitivity of A549 Lung Cancer Cells to Etoposide.Iranian journal of medical sciences · 2021Article
- Novel therapeutic strategies and perspectives for pancreatic cancer: Autophagy and apoptosis are key mechanisms to fight pancreatic cancer.Medical oncology (Northwood, London, England) · 2021Review
- Necroptosis, pyroptosis and apoptosis: an intricate game of cell death.Cellular & molecular immunology · 2021Review
- NCAPH is negatively associated with Mcl‑1 in non‑small cell lung cancer.Molecular medicine reports · 2020Article
- Bcl-2/Bcl-xL inhibitor navitoclax increases the antitumor effect of Chk1 inhibitor prexasertib by inducing apoptosis in pancreatic cancer cells via inhibition of Bcl-xL but not Bcl-2.Molecular and cellular biochemistry · 2020Article
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Authors and funding
13 authors at 1 institution in 1 country.
Smit KourEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Sandeep RanaEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Jacob I ContrerasEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Hannah M KingEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Caroline M RobbEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Yogesh A SonawaneEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Mourad BendjennatEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Ayrianne J CrawfordEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Carter J BargerEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Smitha KizhakeEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Xu LuoEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Michael A HollingsworthEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska.
Amarnath NatarajanEppley Institute for Research in Cancer and Allied Diseases (S.Ko., S.R., J.I.C., H.M.K., C.M.R., Y.A.S., M.B., A.J.C., C.J.B., S.Ki., X.L., M.A.H., A.N.), Departments of Pharmaceutical Sciences (A.N.) and Genetics Cell Biology and Anatomy (A.N.), and Fred & Pamela Buffett Cancer Center (X.L., M.A.H., A.N.), University of Nebraska Medical Center, Omaha, Nebraska anatarajan@unmc.edu.
University of Nebraska Medical Center · US
Funding
UNMC/EPPLEY CANCER CENTER SUPPORT GRANTP30CA036727 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI Joann B. Sweasy · 1985 to 2026
$55.0MTissue CoreP50CA127297 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI HOLLINGSWORTH, MICHAEL A. · 2008 to 2018
$17.1MCHEMICAL CARCINOGENESIS &CANCER BIOLOGYT32CA009476 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI Jennifer D. Black · 1988 to 2026
$6.2MCell Survival Determinants of Metastasis in IGF1R-Dependent CRCR01CA054807 · NCI · UNIVERSITY OF TOLEDO HEALTH SCI CAMPUS · PI BLACK, JENNIFER D. · 1991 to 2016
$3.7MDevelopment of Quinoxaline Based IKKbeta Inhibitors for Kras Driven CancersR01CA197999 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI Amarnath (Amar) Natarajan · 2016 to 2026
$3.3MMechanism of Bax/Bak Activation During ApoptosisR01GM118437 · NIGMS · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI LUO, XU · 2017 to 2020
$1.3MPhosphorylated Form of Activated IKKbeta and Pancreatic CancerR21CA182820 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI NATARAJAN, AMARNATH (AMAR) · 2014 to 2015
$440kBax/Bak activation without direct activator BH3-only proteins in cancer cellsR03CA205496 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI LUO, XU · 2017 to 2018
$151kNCI NIH HHS P30 CA036727NCI NIH HHS P50 CA127297NCI NIH HHS R01 CA054807NCI NIH HHS R01 CA197999NCI NIH HHS R03 CA205496NCI NIH HHS R21 CA182820NCI NIH HHS T32 CA009476NIGMS NIH HHS R01 GM118437
Abstract
Developing small molecules that indirectly regulate Mcl-1 function has attracted a lot of attention in recent years. Here, we report the discovery of an aminopyrazole, 2-([1,1'-biphenyl]-4-yl)-
Indexed as
Aniline CompoundsCell Line, TumorCell ProliferationCell SurvivalCyclin-Dependent Kinase 5Dose-Response Relationship, DrugDrug SynergismGene Expression Regulation, NeoplasticHeLa CellsHumansMyeloid Cell Leukemia Sequence 1 ProteinPancreatic NeoplasmsProtein Kinase InhibitorsPyrazolesSmall Molecule LibrariesSulfonamidesAniline CompoundsCyclin-Dependent Kinase 5MCL1 protein, humanMyeloid Cell Leukemia Sequence 1 ProteinnavitoclaxProtein Kinase InhibitorsPyrazolesSmall Molecule LibrariesSulfonamides
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