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https://www.readbyqxmd.com/read/28548956/dalbinol-a-rotenoid-from-amorpha-fruticosa-l-exerts-anti-proliferative-activity-by-facilitating-%C3%AE-catenin-degradation-in-hepatocellular-carcinoma-cells
#1
Xiaohui Zhu, Xin Wu, Jing Cheng, Hongbo Liao, Xiaoqing Di, Lili Li, Rong Li, Yanfang Zhou, Xiangning Zhang
Hepatocellular carcinoma (HCC) is a highly malignant tumor, and the main cause of treatment failure is malignant proliferation. Aberrations in Wnt/β-catenin signaling are associated with HCC development. Despite the improvements in overall survival made over the past decade from the advent of molecularly targeted therapies, these treatments do not have efficacy in all patients with different pathogeneses. Therefore, there is a demand for novel chemotherapeutic agents for HCC. To this end, we built a natural compound library and screened out a rotenoid named dalbinol from the seeds of Amorpha fruticosa L...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28545370/a-systematic-analysis-of-physicochemical-and-adme-properties-of-all-small-molecule-kinase-inhibitors-approved-by-us-fda-from-january-2001-to-october-2015
#2
Zhihong O'Brien, Mehran F Moghaddam
BACKGROUND: During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. Accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monumental task as these are either scattered in the literature or have not been published. OBJECTIVE: Our goals were, 1) to compile the relevant data on all kinase inhibitors approved prior to 2016 for easy access by the biopharmaceutical community, 2) to provide a retrospective analysis to highlight trends and attributes which may have contributed to the "developability" of these drugs, and 3) to ignite focused debates on what constitutes "actionable", "nice-to-have", and unnecessary data...
May 23, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28545167/synthesis-of-s-2-s-3-4-chlorophenyl-n-4-chlorophenyl-sulfonyl-4-phenyl-4-5-dihydro-1h-pyrazole-1-carboximidamido-3-methyl-d3-butanamide-d5-octa-deuterated-jd5037
#3
Malliga R Iyer, Resat Cinar, Nathan J Coffey, Robert J Chorvat, George Kunos
JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB1 R) receptor. Peripheral CB1 receptor antagonists/inverse agonists have great potential in the treatment of metabolic disorders like type 2 diabetes, obesity and NASH. We report the synthesis of octa-deuterated [(2) H8 ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d8 starting material. The [(2) H8 ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard...
May 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28545015/motor-unit-number-index-munix-in-patients-with-anti-mag-neuropathy
#4
Farzad Fatehi, Emilien Delmont, Aude-Marie Grapperon, Emmanuelle Salort-Campana, Amandine Sévy, Annie Verschueren, José Boucraut, Shahram Attarian
OBJECTIVE: To investigate the relationship between Motor Unit Number Index (MUNIX) and functional scales in patients with anti-Myelin Associated Glycoprotein (MAG) neuropathy and to know if MUNIX is modify after rituximab (RTX) therapy. METHODS: 17 patients were enrolled, of whom 6 were prospectively evaluated during one year after RTX treatment. MUNIX technique was assessed in abductor digiti mini (ADM), abductor pollicis brevi (APB) and tibialis anterior (TA) muscles...
May 9, 2017: Clinical Neurophysiology: Official Journal of the International Federation of Clinical Neurophysiology
https://www.readbyqxmd.com/read/28544619/design-and-synthesis-of-some-acridine-piperazine-hybrids-for-the-improvement-of-cognitive-dysfunction
#5
Anuradha Sharma, Poonam Piplani
A novel series of hybrid molecules (5a-5m) was designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against cognitive dysfunction. Heterocyclic moieties acridine and piperazine were conjugated with suitable linkers in a single scaffold and the structures of the target compounds were confirmed by IR, (1) H NMR, (13) C NMR and LC-MS analysis. The pharmacological activity of synthesized compounds was evaluated using behavioral models of amnesia viz. step down passive avoidance and elevated plus maze at a dose 0...
May 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28544494/4-substituted-thieno-2-3-d-pyrimidines-as-potent-antibacterial-agents-rational-design-microwave-assisted-synthesis-biological-evaluation-and-molecular-docking-studies
#6
Rupinder K Gill, Harpreet Singh, Tilak Raj, Anuradha Sharma, Gagandeep Singh, Jitender Bariwal
In an attempt to discover a new class of antibacterial agents with improved efficacy and to overcome the drug resistant problems, some novel 4-substituted thieno[2,3-d]pyrimidines have been synthesized via microwave assisted methodology and evaluated for their in vitro antibacterial activity against various pathogenic bacterial strains. Compounds 12b and 13c showed the promising inhibitory potencies against S. aureus, B. subtilis, P. aeruginosa and E. coli with MICs ranging from 2 to 10 μg/ml. Compound 13c was also found to be highly potent against methicillin resistant S...
May 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28544150/a-randomized-clinical-trial-of-a-human-acellular-dermal-matrix-demonstrated-superior-healing-rates-for-chronic-diabetic-foot-ulcers-over-conventional-care-and-an-active-acellular-dermal-matrix-comparator
#7
Shawn Cazzell, Dean Vayser, Hau Pham, Jodi Walters, Alexander Reyzelman, Brian Samsell, Kimberly Dorsch, Mark Moore
This study compared the efficacy and safety of a human acellular dermal matrix (ADM), D-ADM, with a conventional care arm and an active comparator human ADM arm, GJ-ADM, for the treatment of chronic diabetic foot ulcers. The study design was a prospective, randomized controlled trial that enrolled 168 diabetic foot ulcer subjects in 13 centers across 9 states. Subjects in the ADM arms received one application but could receive one additional application of ADM if deemed necessary. Screen failures and early withdrawals left 53 subjects in the D-ADM arm, 56 in the conventional care arm, and 23 in the GJ-ADM arm (2:2:1 ratio)...
May 24, 2017: Wound Repair and Regeneration
https://www.readbyqxmd.com/read/28537398/discovery-of-clinical-candidate-2-2s-6s-2-phenyl-6-hydroxyadamantan-2-yl-1-3-hydroxyazetidin-1-yl-ethanone-bms-816336-an-orally-active-novel-selective-11%C3%AE-hydroxysteroid-dehydrogenase-type-1-inhibitor
#8
Xiang-Yang Ye, Stephanie Y Chen, Shung Wu, David S Yoon, Haixia Wang, Zhenqiu Hong, Stepen P O'Connor, Jun Li, James J Li, Lawrence L Kennedy, Steven J Walker, Akbar Nayeem, Steven Sheriff, Daniel M Camac, Vidyhashankar Ramamurthy, Paul E Morin, Rachel Zebo, Joseph R Taylor, Nathan N Morgan, Randolph P Ponticiello, Thomas Harrity, Atsu Apedo, Rajasree Golla, Ramakrishna Seethala, Mengmeng Wang, Timothy W Harper, Bogdan G Sleczka, Bin He, Mark Kirby, David K Leahy, Jianqing Li, Ronald L Hanson, Zhiwei Guo, Yi-Xin Li, John D DiMarco, Raymond Scaringe, Brad D Maxwell, Frederick Moulin, Joel C Barrish, David A Gordon, Jeffrey A Robl
BMS-816336 (6n-2), a hydroxyl-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000 fold selectivity over human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2). BMS-816336 exhibits a robust acute pharmacodynamic effects in cynomolgus monkeys (ED50 0.13 mpk) and in DIO mice. It is orally bioavailable (%F ranges from 20-72% in preclinical species) and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans...
May 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28534954/uncaria-alkaloids-reverse-abcb1-mediated-cancer-multidrug-resistance
#9
Bao-Yuan Huang, Yu Zeng, Ying-Jie Li, Xiao-Jun Huang, Nan Hu, Nan Yao, Min-Feng Chen, Zai-Gang Yang, Zhe-Sheng Chen, Dong-Mei Zhang, Chang-Qing Zeng
The overexpression of ATP-binding cassette (ABC) transporters is the main cause of cancer multidrug resistance (MDR), which leads to chemotherapy failure. Uncaria alkaloids are the major active components isolated from uncaria, which is a common Chinese herbal medicine. In this study, the MDR-reversal activities of uncaria alkaloids, including rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine (Icory), hirsutine and hirsuteine, were screened; they all exhibited potent reversal efficacy when combined with doxorubicin...
May 17, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28533752/protocatechuic-acid-a-phenolic-from-sansevieria-roxburghiana-leaves-suppresses-diabetic-cardiomyopathy-via-stimulating-glucose-metabolism-ameliorating-oxidative-stress-and-inhibiting-inflammation
#10
Niloy Bhattacharjee, Tarun K Dua, Ritu Khanra, Swarnalata Joardar, Ashis Nandy, Achintya Saha, Vincenzo De Feo, Saikat Dewanjee
Persistent hyperglycemia, impairment of redox status and establishment of inflammatory pathophysiology integrally play important role in the pathogenesis of diabetic cardiomyopathy (DC). Present study examined the therapeutic potential of protocatechuic acid isolated from the Sansevieria roxburghiana rhizomes against DC employing rodent model of type 2 diabetes (T2D). T2D was induced by high fat diet + a low-single dose of streptozotocin (35 mg/kg, i.p.). T2D rats exhibited significantly (p < 0.01) high fasting blood glucose level...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28529482/mode-of-action-analyses-of-neferine-a-bisbenzylisoquinoline-alkaloid-of-lotus-nelumbo-nucifera-against-multidrug-resistant-tumor-cells
#11
Onat Kadioglu, Betty Y K Law, Simon W F Mok, Su-Wei Xu, Thomas Efferth, Vincent K W Wong
Neferine, a bisbenzylisoquinoline alkaloid isolated from the green seed embryos of Lotus (Nelumbo nucifera Gaertn), has been previously shown to have various anti-cancer effects. In the present study, we evaluated the effect of neferine in terms of P-glycoprotein (P-gp) inhibition via in vitro cytotoxicity assays, R123 uptake assays in drug-resistant cancer cells, in silico molecular docking analysis on human P-gp and in silico absorption, distribution, metabolism, and excretion (ADME), quantitative structure activity relationships (QSAR) and toxicity analyses...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28526905/effectiveness-of-acellular-dermal-matrix-on-autologous-split-thickness-skin-graft-in-treatment-of-deep-tissue-defect-esthetic-subjective-and-objective-evaluation
#12
Yoo Jung Lee, Myong Chul Park, Dong Ha Park, Hyung Min Hahn, Sue Min Kim, Il Jae Lee
BACKGROUND: A split-thickness skin graft (STSG) is performed to cover a large full-thickness skin defect. Esthetic and functional deficits can result, and many studies have sought to overcome them. This study compared the effectiveness of the acellular dermal matrix (ADM) graft and STSG concerning esthetic and functional effectiveness of ADM on scar quality. METHODS: Of the patients who underwent anterolateral thigh free flap from 2011 to 2015, patients who received skin graft only (n = 10) or skin graft with ADM (n = 20) for coverage of the donor site were enrolled...
May 19, 2017: Aesthetic Plastic Surgery
https://www.readbyqxmd.com/read/28526475/identification-and-preliminary-structure-activity-relationships-of-1-indanone-derivatives-as-novel-indoleamine-2-3-dioxygenase-1-ido1-inhibitors
#13
Dingding Gao, Yingxia Li
Indoleamine 2,3-dioxygenase 1 (IDO1) plays a vital role in the catabolism of tryptophan along with the kynurenine pathway which is involved in many human diseases including cancer, Alzheimer's disease, etc. In this study, compound 1 bearing a 1-Indanone scaffold was identified as a novel IDO1 inhibitor by structure-based virtual screening, with moderate to good enzymatic and cellular inhibitory activities. Also, surface plasmon resonance analysis validated the direct interaction between compound 1 and IDO1 protein...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28523106/discovery-of-fluorine-containing-benzoxazinyl-oxazolidinones-for-the-treatment-of-multidrug-resistant-tuberculosis
#14
Hongyi Zhao, Yu Lu, Li Sheng, Zishuo Yuan, Bin Wang, Weiping Wang, Yan Li, Chen Ma, Xiaoliang Wang, Dongfeng Zhang, Haihong Huang
A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound 21 exhibited not only outstanding in vitro activity with a MIC value of 0.25-0.50 μg/mL against drug-susceptible H37Rv strain and two clinically isolated drug-resistant Mycobacterium tuberculosis strains, but also acceptable in vitro ADME/T properties. Moreover, this compound displayed excellent mouse pharmacokinetic profiles with an oral bioavailability of 102% and a longer elimination half-life of 4...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28523098/incb24360-epacadostat-a-highly-potent-and-selective-indoleamine-2-3-dioxygenase-1-ido1-inhibitor-for-immuno-oncology
#15
Eddy W Yue, Richard Sparks, Padmaja Polam, Dilip Modi, Brent Douty, Brian Wayland, Brian Glass, Amy Takvorian, Joseph Glenn, Wenyu Zhu, Michael Bower, Xiangdong Liu, Lynn Leffet, Qian Wang, Kevin J Bowman, Michael J Hansbury, Min Wei, Yanlong Li, Richard Wynn, Timothy C Burn, Holly K Koblish, Jordan S Fridman, Tom Emm, Peggy A Scherle, Brian Metcalf, Andrew P Combs
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure of INCB24360 contains several previously unknown or underutilized functional groups in drug substances, including a hydroxyamidine, furazan, bromide, and sulfamide. These moieties taken together in a single structure afford a compound that falls outside of "drug-like" space. Nevertheless, the in vitro ADME data is consistent with the good cell permeability and oral bioavailability observed in all species (rat, dog, monkey) tested...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28515964/radiologic-pathologic-correlation-acellular-dermal-matrix-alloderm-%C3%A2-used-in-breast-reconstructive-surgery
#16
Christine U Lee, Aleh Bobr, Jorge Torres-Mora
Acellular dermal matrix (ADM) such as Alloderm(®) is sometimes used in tissue reconstruction in primary and reconstructive breast surgeries. As ADM is incorporated into the native tissues, the evolving imaging findings that would correlate with varying degrees of host migration and neoangiogenesis into the matrix can be challenging to recognize. In the setting of a palpable or clinical area of concern after breast reconstructive surgery following breast cancer, confident diagnosis of a mass representing ADM rather than recurring or developing disease can be challenging...
2017: Journal of Clinical Imaging Science
https://www.readbyqxmd.com/read/28514903/utility-of-the-central-motor-conduction-time-recorded-from-the-abductor-pollicis-brevis-and-the-abductor-digiti-minimi-muscles-in-patients-with-c6-7-myelopathy
#17
Yasuaki Imajo, Tsukasa Kanchiku, Hidenori Suzuki, Masahiro Funaba, Norihiro Nishida, Toshihiko Taguchi
OBJECTIVE: Central motor conduction time (CMCT) recorded from the abductor pollicis brevis (CMCT-APB) and abductor digiti minimi (CMCT-ADM) muscles may enable the evaluation of patients with C6-7 myelopathy. CMCT is more useful for the evaluation of the function of spinal cord than magnetic resonance imaging (MRI) findings. CMCT may be associated with age and height. However, there are few reports regarding CMCT-APB in normal subjects. This study aimed to investigate the relationships between age, height, and conduction parameters in normal subjects to assess the effectiveness of using CMCT-APB and CMCT-ADM for the evaluation of patients with C6-7 and C7-T1 myelopathy...
May 17, 2017: Journal of Spinal Cord Medicine
https://www.readbyqxmd.com/read/28514653/the-presence-of-interleukin-13-at-pancreatic-adm-panin-lesions-alters-macrophage-populations-and-mediates-pancreatic-tumorigenesis
#18
Geou-Yarh Liou, Ligia Bastea, Alicia Fleming, Heike Döppler, Brandy H Edenfield, David W Dawson, Lizhi Zhang, Nabeel Bardeesy, Peter Storz
The contributions of the innate immune system to the development of pancreatic cancer are still ill defined. Inflammatory macrophages can initiate metaplasia of pancreatic acinar cells to a duct-like phenotype (acinar-to-ductal metaplasia [ADM]), which then gives rise to pancreatic intraepithelial neoplasia (PanIN) when oncogenic KRas is present. However, it remains unclear when and how this inflammatory macrophage population is replaced by tumor-promoting macrophages. Here, we demonstrate the presence of interleukin-13 (IL-13), which can convert inflammatory into Ym1+ alternatively activated macrophages, at ADM/PanIN lesions...
May 16, 2017: Cell Reports
https://www.readbyqxmd.com/read/28512990/luminescence-circular-dichroism-and-in-silico-studies-of-binding-interaction-of-synthesized-naphthylchalcone-derivatives-with-bovine-serum-albumin
#19
Sharda Pasricha, Deepti Sharma, Himanshu Ojha, Pragya Gahlot, Mallika Pathak, Mitra Basu, Raman Chawla, Sugandha Singhal, Anju Singh, Rajeev Goel, Shrikant Kukreti, Shefali Shukla
Chalcones possess various biological properties, for example, antimicrobial, anti-inflammatory, analgesic, antimalarial, anticancer, antiprotozoal and antitubercular activity. In this study, naphthylchalcone derivatives were synthesized and characterized using (1) H NMR (13) C NMR, Fourier transform infrared and mass techniques. Yields for all derivatives were found to be >90%. Protein-drug interactions influence the absorption, distribution, metabolism and excretion (ADME) properties of a drug. Therefore, to establish whether the synthesized naphthylchalcone derivatives can be used as drugs, their binding interaction toward a serum protein (bovine serum albumin) was investigated using fluorescence, circular dichroism and molecular docking techniques under physiological conditions...
May 16, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28512025/synthesis-of-methanesulphonamido-benzimidazole-derivatives-as-gastro-sparing-antiinflammatory-agents-with-antioxidant-effect
#20
Ratika Sharma, Alka Bali, Bhim Bahadur Chaudhari
A series of 5-methanesulphonamido benzimidazole derivatives were designed by combining the structural features of clinically useful anti-inflammatory drugs (nimesulide and rofecoxib) and antiulcer drugs (lansoprazole, omeprazole, etc.) based on physicochemical and 3D similarity studies. The compounds were evaluated for their anti-inflammatory activity in carrageenan induced rat paw edema model taking rofecoxib and indomethacin as standard drugs. In vitro antioxidant activity of the compounds was assessed by potassium ferricyanide reducing power (PFRAP) assay...
May 6, 2017: Bioorganic & Medicinal Chemistry Letters
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