Acs Medicinal Chemistry Letters Impact Factor
Acs Medicinal Chemistry Letters Impact Factor – Journal importance is determined by measuring the frequency with which an average article in a journal is cited in a given year.
Measures the weighted citations received by a journal. Citation weights are based on the categories and reputation of the citation journal.
Acs Medicinal Chemistry Letters Impact Factor
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Logd Contributions Of Substituents Commonly Used In Medicinal Chemistry
ACS Medicinal Chemistry Letters publishes brief communications on experimental or theoretical results of exceptional timeliness in all aspects of medicinal chemistry (pure and applied) and its extension to pharmacology. The journal publishes studies that range from compound design to optimization, biological evaluation, drug delivery and pharmacology. Specific areas include, but are not limited to: identification, synthesis and optimization of lead biologically active compounds and drugs; biological characterization of new chemical entities in the context of drug discovery; computational, chemistry and structural studies for identification or SAR analysis of bioactive molecules, ligands and their targets etc.; Novel and improved methods including radiation biochemistry with wide application in medicinal chemistry; Discovery techniques for biologically active compounds from synthetic and natural (plant and other) sources; Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response; Pharmacogenetic and pharmacogenomic studies are used to enhance drug design and translation of medicinal chemistry to the clinic, mechanistic drug metabolism and regulation of metabolic enzyme gene expression.
ACS Medicinal Chemistry Letters publishes brief communications on experimental or theoretical results of exceptional timeliness in all aspects of medicinal chemistry (pure and applied) and its extension to pharmacology. The journal publishes studies that range from combining … Read more
Sharad K. Verma1, Xinrong Tian1, Louis V. LaFrance1, Celine Duquenay1, Dominic Suarez1, Kenneth A. Neulander1, Stewart Paul Romerill1, Joel Loren Burgess1, Seth W. Grant1, Brackley James1, Allen P. Graves1, Daryl A. Art Shu1, Christine Thompson1, Heidi M. Ott1, Glenn S. Van Aller1, Carl A. Machuta1, Elsie Diaz1, Yong Jiang1, Johnson Neil W1, Steven D. Knight1, Ryan G. Kruger1, Michael T. McCabe1, Dashyant Dhanak1, Peter J. Tumino1, Caretha L. Chrissy1, William H. Miller1
Abstract: The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to cancer initiation and progression. As part of a drug discovery program targeting EZH2, we have identified a highly potent, selective, SAM-competitive and cell-active EZH2 inhibitor … The histone H3-lysine 27 (H3K27) methyltransferase plays an important role in regulating EZH2 gene expression. , and its aberrant activity has been linked to cancer initiation and progression. As part of a drug discovery program targeting EZH2, we have identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 (3) and GSK343 (6). These compounds are small molecule chemical tools that will be useful to further explore the biology of EZH2. Read more Read less
Efficacy Of Green Synthesized Silver Nanoparticles Via Ginger Rhizome Extract Against Leishmania Major In Vitro
Topics: Histone Methyltransferase (65%) 65% Paper Related , PRC2 (59%) 59% Paper Related , EZH2 (57%) 57% Paper Related , Histone (54%) 54% Paper Related , Methyltransferase (53%) 53% Related to the paper
Steven D. Knight1, Nicholas D. Adams1, Joel Lauren Burgess1, Amita M. Chowdhury1, Michael G. Darcy1, Carla A. Donatelli1, Juan I. Luengo1, Ken A. Neulander1, Cynthia A. Parrish1, Lance Ridgers1, Martha A. Sarpong1, Schmidt Stanley J1, Glenn S. Van Aller1, Jeffrey D. Carson1, Melody Diamond1, Patricia A. Elkins1, Christine M. Gardiner1, Eric Garver1, Seth A. Gilbert1, Richard R. Gontarek1, Jeffrey R. Jackson1, Kevin1 L. Kershner1, Lusong Luo1, Kaushik Raha1, Christian S. Sherk1, Chiu-Mei Sung1, David Sutton1, Peter J. Tummino1, Ronald Wegrzyn1, Kurt R. Auger1, Dashyant Dhanak1
Abstract: Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancer. The mammalian target of rapamycin (mTOR), class IV PI3K protein kinase, is also a central regulator of cell growth, and mTOR inhibitors are considered … Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation. , and its signaling pathway is the most commonly mutated pathway in human cancer. The mammalian target of rapamycin (mTOR), class IV PI3K protein kinase, is also a central regulator of cell growth, and mTOR inhibitors are thought to enhance the antiproliferative efficacy of PI3K/AKT pathway inhibition. 2, 4-Difluoro-N-benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models. Compound 1 is currently being evaluated in human clinical trials for the treatment of cancer. Read more Read less
Topics: RPTOR (62%)62% Paper Related , PI3K/AKT/mTOR Pathway (61%) 61% Paper Related, Cell Growth (52%)52% Paper Related, Protein Kinase A (50% 50% Paper Related
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Shifeng Pan1, Xu Wu1, Jiqing Jiang1, Wenqi Gao1, Yongqin Wan1, Dai Cheng1, Dong Han1, Jun Liu1, Nathan P. Englund1, Yan Wang1, Stefan Peukert2, Karen Miller-Moslin2, Jing Yuan2, Ribo Guoto2, Mel Anuto Vattay2, Yun Jiang2, Jeffrey Tsao2, Fangxian Sun1, AnneMarie Culazzo Pferdekamper1, Stephanie Kay Dodd2, Tove Tuntland1, Wieslawa Maniara2, Joseph Kelleher2, Yung-mae Yao2, Markus Warmuth2, Julion2, Market2, Market2.
Abstract: Blockade of aberrant Hedgehog (HH) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inhibitor of the Hh pathway through antagonism of the Smoothen receptor (Smo). Structure-activity relationship … Blockade of aberrant hedgehog (HH) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inhibitor of the Hh pathway through antagonism of the Smoothen receptor (Smo). Structure-activity relationship studies led to the discovery of a potent and specific smoothing antagonist N-(6-((2S, 6R)-2, 6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4′-(trifluoromethoxy) . )biphenyl-3-carboxamide (5m, NVP-LDE225), which is currently in clinical development. Read more Read less
Topics: Smoothen (67%)Related to 67% paper, Smoothen receptor (64%)Related to 64% paper, Hedgehog signaling pathway (57%)Related to 57% paper
Binh Thanh Vu1, Peter Michael Vovkulich1, Giacomo Pizzolato1, Allen John Lovey1, Qingjie Ding1, Nan Jiang1, Jin-Jun Liu1, Chunlin Zhao1, Kelli Glenn1, Yang Wen1, Christian Tovar1, Packman Kathryn E1, Lyubomir V Gravesd T, 1.
The Andrade Lab
Abstract: The p53 tumor suppressor is a potent transcription factor that plays a key role in regulating cellular responses to stress. It is regulated by its negative regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity MDM2 also targets p53 for degradation. The proteasome produces many tumors hi… The p53 tumor suppressor is a potent transcription factor that plays a key role in regulating cellular responses to stress and is regulated by its negative regulator MDM2, which directly binds to p53 and inhibits its transcriptional activity. is MDM2 also targets p53 for degradation by the proteasome Many tumors produce high levels of MDM2, thereby impairing p53 function Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment RG7112 (2g) The first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2 in cancer cells expressing wild-type p53, RG7112 s, destabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and human tumor xenografts. Leads to inhibition or regression Read more Read less
Topics: Mdm2 (55%)55% Paper Related, Transcription Factors (54%)54% Paper Related, Cancer Cell (54%)54% Paper Related, Proteasome (53%)53% Paper , Cell Cycle Checkpoint (50%) 50% paper related
Abstract: Two-dimensional representation of atoms is a popular communication medium in chemistry and related scientific fields. Computational methods for drawing small molecules with and without manual inspection are well established and widespread in the context of numerous software tools. Regarding planar representations… Two-dimensional representations of molecules are a popular communication medium in chemistry and related scientific fields. Computational methods for drawing small molecules with and without manual inspection are well established and widespread in the context of numerous software tools. Regarding the planar depiction of molecular complexes, there is little choice. We developed PoseView software, which automatically generates two-dimensional diagrams of macromolecular complexes, showing ligands, interactions, and interacting residues. All illustrated molecules are drawn as structure diagrams at the atomic level; Thus, the output plot is clearly structured and easily readable for the scientist. We tested the performance of PoseView in a large-scale application on almost all drug-like complexes in the PDB (about 200000 complexes); For more than 92% of the complexes considered for drawing, the layout can be calculated. In the following, we present the results of this application study. Read more Read less
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