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Author Details

Gerard M McGeehan
1989
61
24
PMIDPaper TitleJournal TitlePublished Year
38096371Mezigdomide is effective alone and in combination with menin inhibition in preclinical models of KMT2A-r and NPM1c AML.Blood2024
36977823Causal linkage of presence of mutant NPM1 to efficacy of novel therapeutic agents against AML cells with mutant NPM1.Leukemia2023
36635503Targeting Menin disrupts the KMT2A/B and polycomb balance to paradoxically activate bivalent genes.2023
37055414Targeting of epigenetic co-dependencies enhances anti-AML efficacy of Menin inhibitor in AML with MLL1-r or mutant NPM1.Blood Cancer J2023
36922593The menin inhibitor revumenib in KMT2A-rearranged or NPM1-mutant leukaemia.Nature2023
36922589MEN1 mutations mediate clinical resistance to menin inhibition.Nature2023
36727398Inhibition of menin, BCL-2, and FLT3 combined with a hypomethylating agent cures -ITD/-TKD mutant acute myeloid leukemia in a patient-derived xenograft model.2023
37520776The MLL-Menin Interaction is a Therapeutic Vulnerability in -rearranged AML.2023
34582559The menin-MLL1 interaction is a molecular dependency in NUP98-rearranged AML.Blood2022
35534777IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia.Nat Cancer2022
35017466Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c).Blood Cancer J2022
34232981Menin inhibition decreases Bcl-2 and synergizes with venetoclax in NPM1/FLT3-mutated AML.Blood2021
33542482Menin is necessary for long term maintenance of meningioma-1 driven leukemia.Leukemia2021
32589720Synergistic targeting of FLT3 mutations in AML via combined menin-MLL and FLT3 inhibition.Blood2020
32001657Therapeutic targeting of preleukemia cells in a mouse model of <i>NPM1</i> mutant acute myeloid leukemia.Science2020
32333633Evaluation of VTP-50469, a menin-MLL1 inhibitor, against Ewing sarcoma xenograft models by the pediatric preclinical testing consortium.Pediatr Blood Cancer2020
31355641Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of Screening and Optimization in CONTOUR.Journal of Chemical Information and Modeling2019
31821784A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia.Cancer Cell2019
29567358Effect of short-term liver X receptor activation on epidermal barrier features in mild to moderate atopic dermatitis: A randomized controlled trial.Ann Allergy Asthma Immunol2018
28528082Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.Bioorganic and Medicinal Chemistry2017
27599745Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.Bioorganic and Medicinal Chemistry Letters2016
27393460Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys.European Journal of Pharmacology2016
26990539Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.Journal of Medicinal Chemistry2016
26897089Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.Bioorganic and Medicinal Chemistry2016
25445047Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes.European Journal of Pharmacology2015
24470465Multiple ascending dose study with the new renin inhibitor VTP-27999: nephrocentric consequences of too much renin inhibition.Hypertension2014
22810003Regulation of sphingomyelin phosphodiesterase acid-like 3A gene (SMPDL3A) by liver X receptors.Molecular Pharmacology2012
21741239Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.Bioorganic and Medicinal Chemistry Letters2011
24900262Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.ACS Medicinal Chemistry Letters2011
21786805Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase type 1.Journal of Medicinal Chemistry2011
19959358Optimization of orally bioavailable alkyl amine renin inhibitors.Bioorganic and Medicinal Chemistry Letters2010
20864344Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1.Bioorganic and Medicinal Chemistry Letters2010
20064717Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.Bioorganic and Medicinal Chemistry Letters2010
19457666Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.Bioorganic and Medicinal Chemistry Letters2009
18582379Purification and characterization of recombinant human renin for X-ray crystallization studies.BMC Biochemistry2008
17942478Cloning, characterization and site-directed mutagenesis of canine renin.Journal of Biochemistry2007
16787263Development of inhibitors of the aspartyl protease renin for the treatment of hypertension.Current Protein and Peptide Science2006
15294281Purification and characterization of recombinant human cathepsin E expressed in human kidney cell line 293.Protein Expression and Purification2004
11969190Development of a homogeneous, fluorescence resonance energy transfer-based in vitro recruitment assay for peroxisome proliferator-activated receptor delta via selection of active LXXLL coactivator peptides.Analytical Biochemistry2002
10937713Solid-phase synthesis of an arylsulfone hydroxamate library.Bioorganic and Medicinal Chemistry Letters2000
11126297Polymer-supported tetrafluorophenol: a new activated resin for chemical library synthesis.2000
10475260Method to analyze collagenase and gelatinase activity by fibroblasts in culture.In Vitro Cellular and Developmental Biology - Animal1999
10052961Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.Journal of Medicinal Chemistry1999
29711099Nanomolar Inhibitors for Two Distinct Biological Target Families from a Single Synthetic Sequence: A Next Step in Combinatorial Library Design?Angewandte Chemie - International Edition1998
9034191Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha.Nature1997
9042103Structural features and biochemical properties of TNF-alpha converting enzyme (TACE).Journal of Neuroimmunology1997
8605725Effect of matrix metalloproteinase inhibitors on tumor growth and spontaneous metastasis.Clinical and Experimental Metastasis1996
8522351Monoclonal antibodies against human collagenase and stromelysin.1995
7674932Defined substrate mixtures for mapping of proteinase specificities.Methods in Enzymology1995
8278810Structure of the catalytic domain of fibroblast collagenase complexed with an inhibitor.Science1994
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