A5027235116- Click Chemistry and Applications
- Peptidase Inhibition and Analysis
- Bone Metabolism and Diseases
- Protein Degradation and Inhibitors
- Molecular Sensors and Ion Detection
- Advanced biosensing and bioanalysis techniques
- Lipid Membrane Structure and Behavior
- Bone health and treatments
- Bone fractures and treatments
- Molecular Biology Techniques and Applications
- Cholesterol and Lipid Metabolism
- Receptor Mechanisms and Signaling
- Hemostasis and retained surgical items
- Proteoglycans and glycosaminoglycans research
- Spacecraft Design and Technology
- Medical and Biological Sciences
- Bone and Joint Diseases
- TGF-β signaling in diseases
- Periodontal Regeneration and Treatments
- Rheumatoid Arthritis Research and Therapies
- Axon Guidance and Neuronal Signaling
- Platelet Disorders and Treatments
- Adenosine and Purinergic Signaling
- Protein purification and stability
- Knee injuries and reconstruction techniques
Jikei University School of Medicine
2017-2022
Mitsubishi Electric (Japan)
2022
Tokyo Medical and Dental University
2013-2022
Scripps Research Institute
2019-2021
Otsuka (Japan)
2019-2021
Ligand-induced protein degradation has emerged as a compelling approach to promote the targeted elimination of proteins from cells by directing these ubiquitin-proteasome machinery. So far, only limited number E3 ligases have been found support ligand-induced degradation, reflecting dearth E3-binding compounds for proteolysis-targeting chimera (PROTAC) design. Here, we describe functional screening strategy performed with focused library candidate electrophilic PROTACs discover bifunctional...
Abstract Bone remodeling maintains the robustness of bone tissue by balancing resorption osteoclasts and formation osteoblasts. Although these cells together play a crucial role in remodeling, only few reports are available on common factors involved differentiation two types cells. Here, we show family with sequence similarity 102 member A (Fam102a) as bone-remodeling factor that positively regulates both osteoclast osteoblast differentiation. Fam102a controlling recombination signal...
Significant advancement of chemoproteomics has contributed to uncovering the mechanism action (MoA) small-molecule drugs by characterizing drug–protein interactions in living systems. However, cell-membrane proteins such as G protein-coupled receptors (GPCRs) and ion channels, due their low abundance unique biophysical properties associated with multiple transmembrane domains, can present challenges for proteome-wide mapping drug–receptor interactions. Herein, we describe development novel...
Target engagement assays are crucial for establishing the mechanism-of-action of small molecules in living systems. Integral membrane transporters can present a challenging protein class assessing cellular by molecules. The chemical proteomic discovery alpha-chloroacetamide (αCA) compounds that covalently modify cysteine-54 (C54) MPC2 subunit mitochondrial pyruvate carrier (MPC) is presented. This finding used to create an alkyne-modified αCA, YY4-yne, serves as probe click chemistry-enabled...
Abstract Semaphorin 3A (Sema3A) coordinates bone resorption and formation under the control of estrogen signaling. However, contribution osteoblast lineage cell–derived Sema3A to vertebral homeostasis has remained unclear. Moreover, it is unknown whether androgen signaling involved in expression cells. In this study, we show that plays a key role independent Sema3a deletion with Sp7-Cre did not alter trabecular mass lumbar vertebrae, along there being no significant difference mRNA...
Good clinical results have been reported with anatomic anterior cruciate ligament (ACL) reconstructions in which rectangular bone-patellar tendon-bone (BTB) grafts were fixed into bone tunnels made at ACL insertion sites of the femur and tibia (anatomic tunnel BTB reconstruction). Notwithstanding these good results, some problems remained unsolved, including procedural complexity risk damage to femoral posterior wall, nerves blood vessels, cartilage. The purpose this report is present our...
Purpose: Low intensity pulsed ultrasound stimulation (LIPUS) has been clinically applied to promote bone fracture healing in the orthopedic field. Thus, it is likely that LIPUS also stimulates regeneration defects cranial-maxillofacial area. However, this not clearly proved. Furthermore, optimal time point and period of application after surgery reported. The purpose present study was evaluate effect on rat parietal especially focusing application. Materials Methods: Eighteen Wistar rats (14...
Electrophilic compounds originating from nature or chemical synthesis have profound effects on immune cells. These are thought to act by cysteine modification alter the functions of immune-relevant proteins; however, our understanding electrophile-sensitive cysteines in human proteome remains limited. Here, we present a global map primary T cells that susceptible covalent electrophilic small molecules. More than 3000 covalently liganded were found functionally and structurally diverse...
Abstract Target engagement assays are crucial for establishing the mechanism‐of‐action of small molecules in living systems. Integral membrane transporters can present a challenging protein class assessing cellular by molecules. The chemical proteomic discovery alpha‐chloroacetamide (αCA) compounds that covalently modify cysteine‐54 (C54) MPC2 subunit mitochondrial pyruvate carrier (MPC) is presented. This finding used to create an alkyne‐modified αCA, YY4‐yne, serves as probe click...