A5102738329- Prostate Cancer Diagnosis and Treatment
- Prostate Cancer Treatment and Research
- Tryptophan and brain disorders
- Radiomics and Machine Learning in Medical Imaging
- Receptor Mechanisms and Signaling
- Particle physics theoretical and experimental studies
- Synthetic Organic Chemistry Methods
- Bladder and Urothelial Cancer Treatments
- Urologic and reproductive health conditions
- Chemical Synthesis and Analysis
- Renal cell carcinoma treatment
- Adenosine and Purinergic Signaling
- Asymmetric Synthesis and Catalysis
- Neutrino Physics Research
- Astrophysics and Cosmic Phenomena
- Pharmacological Receptor Mechanisms and Effects
- Urological Disorders and Treatments
- Amino Acid Enzymes and Metabolism
- Pharmacogenetics and Drug Metabolism
- Robotics and Automated Systems
- Synthesis and Catalytic Reactions
- Carbohydrate Chemistry and Synthesis
- Neuroendocrine Tumor Research Advances
- Click Chemistry and Applications
- Radical Photochemical Reactions
Peking University
2013-2024
Merck & Co., Inc., Rahway, NJ, USA (United States)
2014-2024
Peking University First Hospital
2013-2024
National Clinical Research Center for Digestive Diseases
2022
Beijing Chest Hospital
2018
Harvard University
2011
Shanghai Advanced Research Institute
2006
Lawrence Berkeley National Laboratory
1999-2005
Shanghai Institute of Organic Chemistry
2005
Lanzhou University
2004
The status of the research on muon colliders is discussed and plans are outlined for future theoretical experimental studies. Besides continued work parameters a 3-4 0.5 TeV center-of-mass (CoM) energy collider, many studies now concentrating machine near 0.1 that could be factory s-channel production Higgs particles. We discuss various components in such colliders, starting from proton accelerator needed to generate pions heavy-Z target proceeding through phase rotation decay ($\pi \to \mu...
We describe the status of our effort to realize a first neutrino factory and progress made in understanding problems associated with collection cooling muons towards that end. summarize physics can be done factories as well intense cold beams muons. The potential muon colliders is reviewed, both Higgs Factories compact high energy lepton colliders. timescale research development reviewed latest designs channels including promise ring coolers achieving longitudinal transverse simultaneously....
Recent success in legged robot locomotion is attributed to the integration of reinforcement learning and physical simulators. However, these policies often encounter challenges when deployed real-world environments due sim-to-real gaps, as simulators typically fail replicate visual realism complex geometry. Moreover, lack realistic rendering limits ability support high-level tasks requiring RGB-based perception like ego-centric navigation. This paper presents a Real-to-Sim-to-Real framework...
An efficient and highly convergent total synthesis of the potent antitumor agent phorboxazole B has been achieved. The synthetic strategy this features: 1) a substrate-controlled hydrogenation to construct functionalized cis-tetrahydropyrane unit; 2) iterative crotyl addition synthesize segment that contains alternating hydroxyl methyl substituents; 3) Hg(OAc)2/I2-induced cyclization establish moiety; 4) 1,3-asymmetric induction in Mukaiyama aldol reaction afford stereogenic centers at C9...
Here we describe a 5-step sequence to prepare the AB enone 1, key precursor fully synthetic tetracyclines, that begins with diastereoselective Michael–Claisen coupling of two simple starting materials, cyclohexenone (compound 2 or, in refinement, substituted variant, vide infra) and isoxazole ester 3. This advance defines an 8-step linear 6-deoxytetracycline antibiotics from three components similar complexity (cyclohexenone 2, 3, structurally diverse D-ring precursors) which sequential...
The application of bicyclo[1.1.1]pentanes (BCPs) as phenyl bioisosteres has garnered significant attention, these structural motifs can improve the physiochemical profiles drug candidates. Despite potential using 1-bicyclo[1.1.1]pentylpyrazoles (BCPPs) 1-phenylpyrazole bioisosteres, this area remains underexplored because relative lack reliable synthetic methods for preparation BCPPs. Herein we address gap and report development novel scalable routes to generate a host
Objective: To evaluate objective treatment efficacy and safety, subjective patient-reported outcomes in patients with complex ureteral strictures (US) undergoing minimally invasive lingual mucosal graft ureteroplasty (LMGU). Materials Methods: We prospectively enrolled underwent robotic or laparoscopic LMGU between May 2020 July 2022. Clinical success was defined as symptom-free no radiographic evidence of re-obstruction. Patient-reported outcomes, including health-related quality life...
Inhibition of leucine-rich repeat kinase 2 is a genetically supported mechanism for the treatment Parkinson's disease. We previously disclosed discovery an indazole series lead that demonstrated both safety and translational risks. The risks were hypothesized to be unknown origin, so structural diversity in subsequent chemical matter was prioritized. identified due low brain Kp
The action of arginase, a metalloenzyme responsible for the hydrolysis arginine to urea and ornithine, is hypothesized suppress immune-cell activity within tumor microenvironment, thus its inhibition may constitute means by which potentiate efficacy immunotherapeutics such as anti-PD-1 checkpoint inhibitors. Taking inspiration from reported enzyme–inhibitor cocrystal structures, we designed synthesized novel inhibitors human arginase possessing fused 5,5-bicyclic ring system. prototypical...
Indoleamine-2,3-dioxygenase-1 (IDO1) has emerged as an attractive target for cancer immunotherapy. An automated ligand identification system screen afforded the tetrahydroquinoline class of novel IDO1 inhibitors. Potency and pharmacokinetic (PK) were key issues with this compounds. Structure-based drug design strategic incorporation polarity enabled rapid improvement on potency, solubility, oxidative metabolic stability. Metabolite studies revealed that amide hydrolysis in D-pocket was...
Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for treatment a number indications ranging from pulmonary and vascular disease to cancer. Thus, high demand exists selective small molecule ARG inhibitors with favorable druglike properties good oral bioavailability. In light significant challenges associated unique physicochemical previously disclosed inhibitors, we use structure-based drug design combined focused optimization strategy discover class boronic...
3,3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and cyclobutane functionalities. We report the discovery of a novel class oxetane indole-amine 2,3-dioxygenase (IDO1) inhibitors suitable Q3W (once every 3 weeks) oral parenteral dosing. A diamide IDO was discovered through an automated ligand identification system (ALIS). Installation fluorophenyl dramatically improved potency. Identification biaryl moiety unconventional amide isostere addressed metabolic...
Purpose To develop a cascaded deep learning model trained with apparent diffusion coefficient (ADC) and T2-weighted imaging (T2WI) for fully automated detection localization of clinically significant prostate cancer (csPCa). Methods This retrospective study included 347 consecutive patients (235 csPCa, 112 non-csPCa) high-quality MRI data, which were randomly selected training, validation, testing. The ground truth was obtained using manual csPCa lesion segmentation, according to...
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class triazole agonists was discovered through high throughput screen. The lead compound 4 suffered from poor metabolic stability and solubility. Lead optimization strategies to improve potency, efficacy, stability, solubility are described. This led 20e, which showed significant reduction glucose excursion in wild-type but not deficient mice an...
Comprehensive synthetic strategies afforded a diverse set of structurally unique bicyclic proline-containing arginase inhibitors with high degree three-dimensionality. The analogs that favored the Cγ-exo conformation proline improved potency over initial lead. novel reported here not only enable access to previously unknown stereochemically complex derivatives but also provide foundation for future synthesis analogs, which incorporate inherent three-dimensional character into building...
Cognitive fusion MRI-guided targeted biopsy (cTB) has been widely used in the diagnosis of prostate cancer (PCa). However, cTB relies heavily on operator's experience and confidence MRI readings. Our objective was to compare detection rates artificial intelligence-guided (AI-cTB) routine explore added value using AI for guidance cTB. This a prospective, single-institution randomized controlled trial (RCT) comparing clinically significant PCa (csPCa) between AI-cTB A total 380 eligible...
Herein the discovery of potent IDO1 inhibitors with low predicted human dose is discussed. Metabolite identification (MetID) and structural data were used to strategically incorporate cyclopropane rings into this tetrahydronaphthyridine series improve their metabolic stability potency. Enabling synthetic chemistry was developed construct these unique fused cyclopropyl compounds, leading improved pharmacokinetics whole blood potency a oral as 9 mg once daily (QD).
Prostatic stromal tumours of uncertain malignant potential (STUMPs) are rare prostate tumours. The purpose this study was to investigate the magnetic resonance imaging features STUMPs.A total 12 patients with STUMP confirmed pathology who underwent MRI from 2012 2020 were retrospectively reviewed. Pathological characteristics including histopathology and immunohistochemistry also recorded.Among STUMPs, detected in peripheral zone (41.7%[n = 5]) transitional (58.3% [n 7]) prostate. 8 cases...
A novel class of small-molecule, highly potent, and subtype-selective somatostatin SST3 agonists was discovered through modification a antagonist. As an example, (1R,2S)-9 demonstrated not only potent in vitro agonist activity but also vivo mouse oral glucose tolerance test (OGTT). These may be useful reagents for studying the physiological roles receptor potentially as therapeutic agents.
Abstract Purpose To explore a novel biopsy scheme for prostate cancer (PCa), and test the detection rate pathological agreement of standard systematic (SB) + targeted (TB) scheme. Methods Positive needles were collected from 194 patients who underwent SB TB (STB) followed by radical prostatectomy (RP). Our scheme, regional (TrSB) was defined as (4 SB-needles closest to TB-needles). The McNemar utilized compare performance clinical significant PCa (csPCa) insignificant (ciPCa). Moreover,...
You have accessJournal of UrologyReconstruction: Augmentation, Substitution, Diversion (PD21)1 May 2024PD21-09 HEALTH-RELATED QUALITY OF LIFE IN PATIENTS UNDERGOING ILEAL URETER REPLACEMENT FOR EXTENSIVE URETERAL STRICTURE: A MULTI-INSTITUTIONAL PROSPECTIVE STUDY Xiang Wang, Derun Li, Guanpeng Han, Kunlin Yang, Hua Guan, Zhihua Liqun Zhou, Kai Zhang, and Xuesong Li WangXiang Wang , LiDerun HanGuanpeng Han YangKunlin Yang GuanHua Guan LiZhihua ZhouLiqun Zhou ZhangKai Zhang LiXuesong View All...