Abed Rahman Kawakibi
University of Michigan
Dopamine receptorCancerInternal medicineG protein-coupled receptorMutantOncologyAllosteric regulationReceptorChemistryCmaxGlioblastomaAntagonistAntagonismGliomaBile fluidNeurologic OncologyClinical efficacyNeuro oncologyDrd2 geneTherapeutic monitoringRats sprague dawleyDopamine receptor D2Cancer researchMedicinePharmacology
13Publications
2H-index
14Citations
Publications 13
Newest
#1Abed Rahman Kawakibi (UM: University of Michigan)H-Index: 2
#2Rohinton TaraporeH-Index: 17
Last. Carl Koschmann (UM: University of Michigan)H-Index: 14
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#1Varun Vijay PrabhuH-Index: 19
#2Sara MorrowH-Index: 1
Last. Joshua E. AllenH-Index: 25
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#1Varun Vijay PrabhuH-Index: 19
#2Caroline CuocoH-Index: 1
Last. Joshua E. AllenH-Index: 25
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#1Varun Vijay PrabhuH-Index: 19
#2Sara MorrowH-Index: 1
Last. Wafik S. El-Deiry (Brown University)H-Index: 122
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ONC201 was originally discovered as TNF-Related Apoptosis Inducing Ligand (TRAIL)-inducing compound TIC10. ONC201 appears to act as a selective antagonist of the G protein coupled receptor (GPCR) dopamine receptor D2 (DRD2), and as an allosteric agonist of mitochondrial protease caseinolytic protease P (ClpP). Downstream of target engagement, ONC201 activates the ATF4/CHOP-mediated integrated stress response leading to TRAIL/Death Receptor 5 (DR5) activation, inhibits oxidative phosphorylation v...
15 CitationsSource
#1Varun Vijay PrabhuH-Index: 19
#2Sara MorrowH-Index: 1
Last. Sharon DeMorrow (A&M: Texas A&M University)H-Index: 37
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ONC201 is the first clinical bitopic antagonist of dopamine receptor D2 (DRD2), that is well tolerated and induces durable tumor regressions in H3 K27M-mutant glioma patients. ONC206, a derivative of ONC201 that shares the imipridone core structure, is also a bitopic DRD2 antagonist that exhibits enhanced non-competitive effects, high specificity, nanomolar potency, and disruption of DRD2 homodimers. ONC206 exhibited a Ki of ~320nM for DRD2 with complete specificity across human GPCRs and comple...
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3617Background: Diffuse midline gliomas, H3 K27M-mutant are associated with a poor prognosis compared to H3 wild-type gliomas and have no effective therapy following first-line radiation. ONC201 is...
1 CitationsSource
#1Kyle Wierzbicki (UM: University of Michigan)H-Index: 3
#2Karthik Ravi (UM: University of Michigan)H-Index: 1
Last. Carl Koschmann (UM: University of Michigan)H-Index: 14
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The original version of this review article unfortunately contained a mistake in the author group section.
1 CitationsSource
#1Kyle Wierzbicki (UM: University of Michigan)H-Index: 3
#2Karthik Ravi (UM: University of Michigan)H-Index: 1
Last. Carl Koschmann (UM: University of Michigan)H-Index: 14
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Purpose of Review H3K27M is a frequent histone mutation within diffuse midline gliomas and is associated with a dismal prognosis, so much so that the 2016 CNS WHO classification system created a specific category of “Diffuse Midline Glioma, H3K27M-mutant”. Here we outline the latest pre-clinical data and ongoing current clinical trials that target H3K27M, as well as explore diagnosis and treatment monitoring by serial liquid biopsy.
5 CitationsSource
#2Sharon GardnerH-Index: 30
Last. Carl KoschmannH-Index: 14
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#1Varun Vijay PrabhuH-Index: 19
Last. Joshua E. AllenH-Index: 25
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1 CitationsSource