Genomes and Genes
Summary: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
- Qinli Z, Meiqing L, Xia J, Li X, Weili G, Xiuliang J, et al. Necrostatin-1 inhibits the degeneration of neural cells induced by aluminum exposure. Restor Neurol Neurosci. 2013;31:543-55 pubmed publisher..Furthermore, Nec-1 may be useful for the prevention and treatment of neurodegenerative disorders. ..
- San Miguel J, Richardson P, Gunther A, Sezer O, Siegel D, Blade J, et al. Phase Ib study of panobinostat and bortezomib in relapsed or relapsed and refractory multiple myeloma. J Clin Oncol. 2013;31:3696-703 pubmed publisher..This phase Ib study sought to determine the maximum-tolerated dose (MTD) of panobinostat plus bortezomib in patients with relapsed or relapsed and refractory MM...
- Gritsch P, Stempel E, Gaich T. Enantioselective synthesis of cyclohepta[b]indoles: gram-scale synthesis of (S)-SIRT1-inhibitor IV. Org Lett. 2013;15:5472-5 pubmed publisher..This method was developed for application in natural product synthesis of a variety of indole alkaloids. ..
- Ahn K, Mahmoud M, Shim J, Kendall D. Distinct roles of ?-arrestin 1 and ?-arrestin 2 in ORG27569-induced biased signaling and internalization of the cannabinoid receptor 1 (CB1). J Biol Chem. 2013;288:9790-800 pubmed publisher..These results demonstrate for the first time the involvement of ?-arrestin in CB1-biased signaling by a CB1 allosteric modulator and also define the differential role of the two ?-arrestin isoforms in CB1 signaling and internalization. ..
- Richeldi L, du Bois R, Raghu G, Azuma A, Brown K, Costabel U, et al. Efficacy and safety of nintedanib in idiopathic pulmonary fibrosis. N Engl J Med. 2014;370:2071-82 pubmed publisher..A phase 2 trial suggested that treatment with 150 mg of nintedanib twice daily reduced lung-function decline and acute exacerbations in patients with idiopathic pulmonary fibrosis...
- Marcos I, Moro R, Costales I, Basabe P, Díez D. Sesquiterpenyl indoles. Nat Prod Rep. 2013;30:1509-26 pubmed publisherThe natural product sesquiterpenyl indoles are structural hybrids from farnesyl pyrophosphate and tryptophan or its precursors, often with unusual and complex structural features, many of them with interesting biological activities...
- Podoll J, Liu Y, Chang L, Walls S, Wang W, Wang X. Bio-inspired synthesis yields a tricyclic indoline that selectively resensitizes methicillin-resistant Staphylococcus aureus (MRSA) to ?-lactam antibiotics. Proc Natl Acad Sci U S A. 2013;110:15573-8 pubmed publisher..These data suggest that Of1 is a unique selective resistance-modifying agent for ?-lactam antibiotics, and it may be further developed to fight against resistant bacteria in the clinic. ..
- Busbee P, Nagarkatti M, Nagarkatti P. Natural indoles, indole-3-carbinol and 3,3'-diindolymethane, inhibit T cell activation by staphylococcal enterotoxin B through epigenetic regulation involving HDAC expression. Toxicol Appl Pharmacol. 2014;274:7-16 pubmed publisher..These studies not only suggest for the first time that plant-derived indoles are potent suppressors of SEB-induced T cell activation and cytokine storm but also that they may mediate these ..
- Reck M, Kaiser R, Mellemgaard A, Douillard J, Orlov S, Krzakowski M, et al. Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial. Lancet Oncol. 2014;15:143-55 pubmed publisher..The phase 3 LUME-Lung 1 study assessed the efficacy and safety of docetaxel plus nintedanib as second-line therapy for non-small-cell lung cancer (NSCLC)...
- Fricker M, Vilalta A, Tolkovsky A, Brown G. Caspase inhibitors protect neurons by enabling selective necroptosis of inflamed microglia. J Biol Chem. 2013;288:9145-52 pubmed publisher..We conclude that the activation of caspase-8 in inflamed microglia prevents their death by necroptosis, and thus, caspase-8 inhibitors may protect neurons in the inflamed brain by selectively killing activated microglia. ..
- Ranasinghe N, Jones G. Extending the versatility of the Hemetsberger-Knittel indole synthesis through microwave and flow chemistry. Bioorg Med Chem Lett. 2013;23:1740-2 pubmed publisherMicrowave, flow and combination methodologies have been applied to the synthesis of a number of substituted indoles. Based on the Hemetsberger-Knittel (HK) process, modifications allow formation of products rapidly and in high yield...
- Plummer R, Lorigan P, Steven N, Scott L, Middleton M, Wilson R, et al. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation. Cancer Chemother Pharmacol. 2013;71:1191-9 pubmed publisher..This study showed that temozolomide (150-200 mg/m(2)/day) can safely be given with a PARP inhibitory dose of rucaparib, increasing progression-free survival over historical controls in metastatic melanoma patients. ..
- Onajole O, Pieroni M, Tipparaju S, Lun S, Stec J, Chen G, et al. Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. J Med Chem. 2013;56:4093-103 pubmed publisher..These compounds were also devoid of apparent toxicity to Vero cells. Importantly, compound 12 was found to be active against the tested XDR-TB strains and orally active in the serum inhibition titration assay...
- Pénzváltó Z, Tegze B, Szász A, Sztupinszki Z, Liko I, Szendroi A, et al. Identifying resistance mechanisms against five tyrosine kinase inhibitors targeting the ERBB/RAS pathway in 45 cancer cell lines. PLoS ONE. 2013;8:e59503 pubmed publisher..In summary, we determined predictive biomarkers for five tyrosine kinase inhibitors, and validated sunitinib resistance biomarkers by immunohistochemistry in an independent patient cohort...
- Teguh S, Klonis N, Duffy S, Lucantoni L, Avery V, Hutton C, et al. Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. J Med Chem. 2013;56:6200-15 pubmed publisher..The quinoline-indoles show only weak activity as inhibitors of ?-hematin formation, and their activities are only weakly antagonized by ..
- Brooks M, Neelam S, Fudala R, Gryczynski I, Cammarata P. Lenticular mitoprotection. Part A: Monitoring mitochondrial depolarization with JC-1 and artifactual fluorescence by the glycogen synthase kinase-3? inhibitor, SB216763. Mol Vis. 2013;19:1406-12 pubmed..We conclude that inhibition of GSK-3? activity by the GSK-3? inhibitor SB216763 provides positive protection against mitochondrial depolarization. ..
- Nahata M, Muto S, Nakagawa K, Ohnishi S, Sadakane C, Saegusa Y, et al. Serotonin 2C receptor antagonism ameliorates novelty-induced hypophagia in aged mice. Psychoneuroendocrinology. 2013;38:2051-64 pubmed publisher..In conclusion, 5-HT2CR signaling enhancement and the subsequent activation of the CRF neuron were involved in novelty-induced hypophagia in aged mice, and the 5-HT2CR antagonists offer a promising therapeutic option for depression. ..
- Mahmoud M, Ali H, Ahn K, Damaraju A, Samala S, Pulipati V, et al. Structure-activity relationship study of indole-2-carboxamides identifies a potent allosteric modulator for the cannabinoid receptor 1 (CB1). J Med Chem. 2013;56:7965-75 pubmed publisher..It showed an equilibrium dissociation constant (KB) of 167.3 nM with a markedly high binding cooperativity factor (? = 16.55) and potent antagonism of agonist-induced GTP?S binding. ..
- Inaba Y, Kanai F, Aramaki T, Yamamoto T, Tanaka T, Yamakado K, et al. A randomised phase II study of TSU-68 in patients with hepatocellular carcinoma treated by transarterial chemoembolisation. Eur J Cancer. 2013;49:2832-40 pubmed publisher..The two deaths were related to the study treatment. These results suggest that further examination of the study design is necessary to determine whether TSU-68 has any clinical benefits when combined with TACE. ..
- Mantareva V, Kussovski V, Durmus M, Borisova E, Angelov I. Photodynamic inactivation of pathogenic species Pseudomonas aeruginosa and Candida albicans with lutetium (III) acetate phthalocyanines and specific light irradiation. Lasers Med Sci. 2016;31:1591-1598 pubmed..The PDI study on microbial biofilms showed incomplete photoinactivation (<3 logs) for the used gentle drug-light protocol. ..
- Lafayette E, de Almeida S, Cavalcanti Santos R, de Oliveira J, Amorim C, da Silva R, et al. Synthesis of novel indole derivatives as promising DNA-binding agents and evaluation of antitumor and antitopoisomerase I activities. Eur J Med Chem. 2017;136:511-522 pubmed publisher..Moreover, it was highlighted that basic side chains, such as thiazolidines and imidazolidines, and free amino group, are relevant for design of promising antitumor and DNA binding compounds. ..
- Uddin M, Werfel T, Crews B, Gupta M, Kavanaugh T, Kingsley P, et al. Fluorocoxib A loaded nanoparticles enable targeted visualization of cyclooxygenase-2 in inflammation and cancer. Biomaterials. 2016;92:71-80 pubmed publisher..v.-ready FA formulation, provide high signal-to-noise in inflamed, premalignant, and malignant tissues, and will uniquely enable clinical translation of the poorly water-soluble FA compound. ..
- Gieger T, Nettifee Osborne J, Hallman B, Johannes C, Clarke D, Nolan M, et al. The impact of carboplatin and toceranib phosphate on serum vascular endothelial growth factor (VEGF) and metalloproteinase-9 (MMP-9) levels and survival in canine osteosarcoma. Can J Vet Res. 2017;81:199-205 pubmed..Bien que ce traitement ait été bien toléré, les temps de survie n’ont pas excédé les résultats publiés antérieurement pour des chiens traités par amputation et chimiothérapie uniquement.(Traduit par Docteur Serge Messier). ..
- Robinson H. Respiratory Conditions Update: Restrictive Lung Disease. FP Essent. 2016;448:29-34 pubmed..Optimization of management may include weight loss, pulmonary rehabilitation, oxygen therapy, and respiratory support. ..
- Liang S, Yu H, Chen X, Shen T, Cui Z, Si G, et al. PDGF-BB/KLF4/VEGF Signaling Axis in Pulmonary Artery Endothelial Cell Angiogenesis. Cell Physiol Biochem. 2017;41:2333-2349 pubmed publisher..Overall, our study contributes to a better understanding of PAH pathogenesis. ..
- de Guglielmo G, Matzeu A, Kononoff J, Mattioni J, Martin Fardon R, George O. Cebranopadol Blocks the Escalation of Cocaine Intake and Conditioned Reinstatement of Cocaine Seeking in Rats. J Pharmacol Exp Ther. 2017;362:378-384 pubmed publisher..However, the conditioned place preference that was observed after cebranopadol administration suggests that this compound may have some intrinsic rewarding effects. ..
- Tuna D, Udvarhelyi A, Sobolewski A, Domcke W, Domratcheva T. Onset of the Electronic Absorption Spectra of Isolated and ?-Stacked Oligomers of 5,6-Dihydroxyindole: An Ab Initio Study of the Building Blocks of Eumelanin. J Phys Chem B. 2016;120:3493-502 pubmed publisher..This study contributes to advancing the understanding of the complex photophysics of the eumelanin biopolymer. ..
- Ruzzolini J, Peppicelli S, Andreucci E, Bianchini F, Margheri F, Laurenzana A, et al. Everolimus selectively targets vemurafenib resistant BRAFV600E melanoma cells adapted to low pH. Cancer Lett. 2017;408:43-54 pubmed publisher..Our results indicate that an acidic microenvironment may cooperate in inducing a BRAF inhibitor resistance in melanoma cells and a combined therapy with everolimus could be used to overcome that resistance. ..
- Nisha C, Kumar A, Vimal A, Bai B, Pal D, Kumar A. Docking and ADMET prediction of few GSK-3 inhibitors divulges 6-bromoindirubin-3-oxime as a potential inhibitor. J Mol Graph Model. 2016;65:100-7 pubmed publisher..Since, 6-BIO is a chemically modified form of the basic molecule Indirubin, we can hypothesize that certain other modified indirubins could be tested as GSK-3 targeted ligands. ..
- Vázquez Osorio I, Sánchez Aguilar M, García Rodiño S, Suárez Peñaranda J, Aliste C, Vázquez Veiga H. Vemurafenib-Induced Neutrophilic Panniculitis: A New Case and Review of the Literature. Am J Dermatopathol. 2016;38:e93-6 pubmed publisher..The presentation of this condition with a single lesion is particularly challenging. Recognition of this association is important given the increasing use of vemurafenib and the potential implications of treatment withdrawal. ..
- Liu F, Du J, Song D, Xu M, Sun G. A sensitive fluorescent sensor for the detection of endogenous hydroxyl radicals in living cells and bacteria and direct imaging with respect to its ecotoxicity in living zebra fish. Chem Commun (Camb). 2016;52:4636-9 pubmed publisher..In addition, it is an excellent sensor for in vivo imaging of Ë™OH generated following treatment with TiO2NPs in zebra fish. ..
- Bavcar S, De Vos J, Kessler M, de Fornel P, Buracco P, Murphy S, et al. Combination toceranib and lomustine shows frequent high grade toxicities when used for treatment of non-resectable or recurrent mast cell tumours in dogs: A European multicentre study. Vet J. 2017;224:1-6 pubmed publisher..A long term response (>1year) was observed in two dogs. Modifications of the protocol are required for future prospective studies. ..
- Keller K, Bradley J, Sun Y, Yang Y, Acott T. Tunneling Nanotubes are Novel Cellular Structures That Communicate Signals Between Trabecular Meshwork Cells. Invest Ophthalmol Vis Sci. 2017;58:5298-5307 pubmed publisher..Recently, specialized filopodia called tunneling nanotubes (TNTs) have been described, which communicate molecular signals and organelles directly between cells. Here, we investigate TNT formation by TM cells...
- Choueiri T, Halabi S, Sanford B, Hahn O, Michaelson M, Walsh M, et al. Cabozantinib Versus Sunitinib As Initial Targeted Therapy for Patients With Metastatic Renal Cell Carcinoma of Poor or Intermediate Risk: The Alliance A031203 CABOSUN Trial. J Clin Oncol. 2017;35:591-597 pubmed publisher..Conclusion Cabozantinib demonstrated a significant clinical benefit in PFS and ORR over standard-of-care sunitinib as first-line therapy in patients with intermediate- or poor-risk mRCC. ..
- Kaya T, Altun A, Turgut N, Ataseven H, Koyluoglu G. Effects of a Multikinase Inhibitor Motesanib (AMG 706) Alone and Combined with the Selective DuP-697 COX-2 Inhibitor on Colorectal Cancer Cells. Asian Pac J Cancer Prev. 2016;17:1103-10 pubmed..In addition, the increased effects of combination of motesanib with DuP-697 raise the possibility of using lower doses of these drugs and therefore avoid/minimize the dose-dependent side effects generally observed. ..
- Gao L, Zhang C, Gao D, Liu H, Yu X, Lai J, et al. Enhanced Anti-Tumor Efficacy through a Combination of Integrin ?v?6-Targeted Photodynamic Therapy and Immune Checkpoint Inhibition. Theranostics. 2016;6:627-37 pubmed publisher..Together, our results demonstrated the synergistic effect of tumor-targeted PDT and immune checkpoint inhibition for improving anti-tumor immunity and suppressing tumor growth/metastasis. ..
- Haas N, Manola J, Uzzo R, Flaherty K, Wood C, Kane C, et al. Adjuvant sunitinib or sorafenib for high-risk, non-metastatic renal-cell carcinoma (ECOG-ACRIN E2805): a double-blind, placebo-controlled, randomised, phase 3 trial. Lancet. 2016;387:2008-16 pubmed publisher..US National Cancer Institute and ECOG-ACRIN Cancer Research Group, Pfizer, and Bayer. ..
- Ikeda S, Sekine A, Baba T, Yamakawa H, Morita M, Kitamura H, et al. Administration of nintedanib after discontinuation for acute exacerbation of idiopathic pulmonary fibrosis: a case report. BMC Pulm Med. 2016;16:38 pubmed publisher..However, we recommend close monitoring and appropriate measures until the long-term safety profile is clarified. ..
- Néel N, Kröger J. Template Effect of the Graphene Moiré Lattice on Phthalocyanine Assembly. Molecules. 2017;22: pubmed publisher..They reflect the transition from a graphene template effect on the 2H-Pc arrangement to molecular superstructures that are mainly governed by the intermolecular coupling. ..
- Menderes G, Bonazzoli E, Bellone S, Black J, Altwerger G, Masserdotti A, et al. SYD985, a novel duocarmycin-based HER2-targeting antibody-drug conjugate, shows promising antitumor activity in epithelial ovarian carcinoma with HER2/Neu expression. Gynecol Oncol. 2017;146:179-186 pubmed publisher..e., 2+ and 1+) HER2/neu expression. SYD985 is more potent than T-DM1 in comparative experiments and unlike T-DM1, it is active against EOC demonstrating moderate/low or heterogeneous HER2/neu expression. ..
- Singh P, Kaur S, Sharma A, Kaur G, Bhatti R. TNF-? and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents. Eur J Med Chem. 2017;140:92-103 pubmed publisher..75% inhibition of acetic acid induced algesia in swiss albino mice was noticed in the presence of compound 4. Experimental data and molecular docking studies indicate that the compounds are targeting TNF-?, iNOS and IL-6. ..
- Swinford Jackson S, Anastasio N, Fox R, Stutz S, Cunningham K. Incubation of cocaine cue reactivity associates with neuroadaptations in the cortical serotonin (5-HT) 5-HT2C receptor (5-HT2CR) system. Neuroscience. 2016;324:50-61 pubmed publisher..Collectively, these outcomes are the first indication that neuroadaptations in the 5-HT2CR system may contribute to incubation of cocaine cue reactivity. ..
- Lahti S, Ludwig J, Xing M, Sun L, Zeng D, Kim H. In vitro biologic efficacy of sunitinib drug-eluting beads on human colorectal and hepatocellular carcinoma-A pilot study. PLoS ONE. 2017;12:e0174539 pubmed publisher..61 ?M (SE ±1.01). Sunitinib can be efficiently loaded to and released from LC beads, and the resulting sunitinib DEB demonstrate strong in vitro inhibition of human CRC and HCC cells. ..
- Sugiyama R, Aizawa N, Ito H, Fujimura T, Suzuki M, Nakagawa T, et al. Synergic Suppressive Effect of Silodosin and Imidafenacin on Non-Voiding Bladder Contractions in Male Rats with Subacute Bladder Outlet Obstruction. Low Urin Tract Symptoms. 2017;9:94-101 pubmed publisher..The present results indicate a suppressive effect of silodosin or imidafenacin alone and a synergic effect of the combination of these two drugs on NVCs in a subacute BOO model of male rats. ..
- Weeks H, Sanders A, Kynaston H, Jiang W. The Association Between WAVE1 and -3 and the ARP2/3 Complex in PC 3 Cells. Anticancer Res. 2016;36:1135-42 pubmed..These results implicate a contributory role of WAVE1 and -3 to the metastatic phenotype of PC-3 cells through their interaction with the ARP2/3 complex. ..