A5018061374- Protein Degradation and Inhibitors
- Ubiquitin and proteasome pathways
- Histone Deacetylase Inhibitors Research
- Genomics and Chromatin Dynamics
- Epigenetics and DNA Methylation
- Protein Kinase Regulation and GTPase Signaling
- Melanoma and MAPK Pathways
- Monoclonal and Polyclonal Antibodies Research
- Computational Drug Discovery Methods
- Cancer-related gene regulation
- Peptidase Inhibition and Analysis
- Estrogen and related hormone effects
- PI3K/AKT/mTOR signaling in cancer
- Chemical Synthesis and Analysis
- RNA Research and Splicing
- Multiple Myeloma Research and Treatments
- RNA regulation and disease
- Biochemical and Molecular Research
- Click Chemistry and Applications
- Glycosylation and Glycoproteins Research
- RNA modifications and cancer
- Circular RNAs in diseases
- Enzyme Structure and Function
- HER2/EGFR in Cancer Research
- DNA and Nucleic Acid Chemistry
Johns Hopkins University
2014-2025
Harvard University
1998-2025
Brigham and Women's Hospital
1993-2025
Boston VA Research Institute
2022-2024
Harvard University Press
2023
Johns Hopkins Medicine
2013-2022
University of Baltimore
2009-2020
Boston University
2020
Louisiana State University Health Sciences Center Shreveport
2013-2019
University of California, San Francisco
2016
A protein semisynthesis method—expressed ligation—is described that involves the chemoselective addition of a peptide to recombinant protein. This method was used ligate phosphotyrosine C terminus tyrosine kinase C-terminal Src (Csk). By intercepting thioester generated in with an N-terminal cysteine containing synthetic peptide, near quantitative chemical ligation achieved. The semisynthetic tail-phosphorylated Csk showed evidence intramolecular phosphotyrosine-Src homology 2 interaction...
Age at menopause and type of from hospital records breast cancer patients were compared with similar information reported by a national probability sample women. The series consisted 3,887 selected those to the Connecticut Cancer Registry between 1950 1959. comprised 3,581 women responding National Health Examination Survey 1960–1962. validity comparison effect relatively large number whose histories deficient evaluated; no substantial bias was identified. Overall, surgically induced...
Abstract We report here that butyrate, a naturally occurring fatty acid commonly used as nutritional supplement and differentiation agent, greatly enhances the efficiency of induced pluripotent stem (iPS) cell derivation from human adult or fetal fibroblasts. After transient butyrate treatment, iPS is enhanced by 15- to 51-fold using either retroviral piggyBac transposon vectors expressing 4 5 reprogramming genes. Butyrate stimulation more remarkable (>100- 200-fold) on in absence...
Metabolism Without Modification Obesity-associated metabolic disease has rapidly become a public health priority in the developed world and is being addressed through prevention strategies aimed at lifestyle changes pharmacological approaches. Barnett et al. (p. 1689 , published online 18 November) designed drug that inhibits action of ghrelin, circulating peptide hormone increases fat mass food intake. The drug, bisubstrate analog called GO-CoA-Tat, selective antagonist ghrelin...
Abstract Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 (tranylcypromine analog). Enzymologic analysis reveals that corin potently targets CoREST complex shows more sustained inhibition of activity compared with entinostat. Cell-based experiments demonstrate exhibits superior anti-proliferative profile against several melanoma lines cutaneous squamous cell carcinoma to its parent monofunctional inhibitors but is less toxic...
Widespread lysine β-hydroxybutyrylation plays diverse regulatory roles and is reversibly regulated by p300 HDAC1/2.
Abstract UM171 is a potent agonist of ex vivo human haematopoietic stem cell self-renewal 1 . By co-opting KBTBD4, substrate receptor the CUL3–RING E3 ubiquitin ligase (CRL3) complex, promotes degradation LSD1–CoREST corepressor thereby limiting attrition 2,3 However, direct target and mechanism action remain unclear. Here we show that acts as molecular glue to induce high-affinity interactions between KBTBD4 HDAC1/2 promote degradation. Through proteomics chemical inhibitor studies,...
The improper activation of the Abl tyrosine kinase results in chronic myeloid leukemia (CML). recognition an inactive conformation Abl, which a catalytically important Asp-Phe-Gly (DFG) motif is flipped by approximately 180° with respect to active conformation, underlies specificity cancer drug imatinib, used treat CML. DFG not crystal structures forms closely related Src kinases, and imatinib does inhibit c-Src. We present structure domain determined complex ATP–peptide conjugate, protein...