LIVIVO - Search results -

Search results

Result 1 - 10 of total 17

Search options

Article ; Online: SRI-32743, a novel allosteric modulator, attenuates HIV-1 Tat protein-induced inhibition of the dopamine transporter and alleviates the potentiation of cocaine reward in HIV-1 Tat transgenic mice.

2022 Volume 220, Page(s) 109239

Abstract: Cocaine abuse increases the incidence of HIV-1-associated neurocognitive disorders. We have demonstrated that HIV-1 transactivator of transcription (Tat) allosterically modulates dopamine (DA) reuptake through the human DA transporter (hDAT), potentially ...

Abstract	Cocaine abuse increases the incidence of HIV-1-associated neurocognitive disorders. We have demonstrated that HIV-1 transactivator of transcription (Tat) allosterically modulates dopamine (DA) reuptake through the human DA transporter (hDAT), potentially contributing to Tat-induced cognitive impairment and potentiation of cocaine conditioned place preference (CPP). This study determined the effects of a novel allosteric modulator of DAT, SRI-32743, on the interactions of HIV-1 Tat, DA, cocaine, and [
MeSH term(s)	Animals ; Cocaine/metabolism ; Cocaine/pharmacology ; Cocaine-Related Disorders/drug therapy ; Cricetinae ; Cricetulus ; Dopamine/metabolism ; Dopamine Plasma Membrane Transport Proteins/genetics ; Doxycycline ; HIV-1 ; Humans ; Mice ; Mice, Transgenic ; Reward ; Trans-Activators ; Transcription Factor DP1/metabolism ; tat Gene Products, Human Immunodeficiency Virus/genetics
Chemical Substances	Dopamine Plasma Membrane Transport Proteins ; Trans-Activators ; Transcription Factor DP1 ; tat Gene Products, Human Immunodeficiency Virus ; Cocaine (I5Y540LHVR) ; Doxycycline (N12000U13O) ; Dopamine (VTD58H1Z2X)
Language	English
Publishing date	2022-09-17
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	218272-5
ISSN	1873-7064 ; 0028-3908
ISSN (online)	1873-7064
ISSN	0028-3908
DOI	10.1016/j.neuropharm.2022.109239
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Ui I Zs.242: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Novel Compound Inhibitors of HIV-1

Robinson, Carolyn A / Lyddon, Terri D / Gil, Hwi Min / Evans, David T / Kuzmichev, Yury V / Richard, Jonathan / Finzi, Andrés / Welbourn, Sarah / Rasmussen, Lynn / Nebane, N Miranda / Gupta, Vandana V / Ananthan, Sam / Cai, Zhaohui / Wonderlich, Elizabeth R / Augelli-Szafran, Corinne E / Bostwick, Robert / Ptak, Roger G / Schader, Susan M / Johnson, Marc C

Viruses

2022 Volume 14, Issue 4

Abstract: HIV-1 Vpu targets the host cell proteins CD4 and BST-2/Tetherin for degradation, ultimately resulting in enhanced virus spread and host immune evasion. The discovery and characterization of small molecules that antagonize Vpu would further elucidate the ... ...

Abstract	HIV-1 Vpu targets the host cell proteins CD4 and BST-2/Tetherin for degradation, ultimately resulting in enhanced virus spread and host immune evasion. The discovery and characterization of small molecules that antagonize Vpu would further elucidate the contribution of Vpu to pathogenesis and lay the foundation for the study of a new class of novel HIV-1 therapeutics. To identify novel compounds that block Vpu activity, we have developed a cell-based ‘gain of function’ assay that produces a positive signal in response to Vpu inhibition. To develop this assay, we took advantage of the viral glycoprotein, GaLV Env. In the presence of Vpu, GaLV Env is not incorporated into viral particles, resulting in non-infectious virions. Vpu inhibition restores infectious particle production. Using this assay, a high throughput screen of >650,000 compounds was performed to identify inhibitors that block the biological activity of Vpu. From this screen, we identified several positive hits but focused on two compounds from one structural family, SRI-41897 and SRI-42371. We developed independent counter-screens for off target interactions of the compounds and found no off target interactions. Additionally, these compounds block Vpu-mediated modulation of CD4, BST-2/Tetherin and antibody dependent cell-mediated toxicity (ADCC). Unfortunately, both SRI-41897 and SRI-42371 were shown to be specific to the N-terminal region of NL4-3 Vpu and did not function against other, more clinically relevant, strains of Vpu; however, this assay may be slightly modified to include more significant Vpu strains in the future.
MeSH term(s)	Anti-HIV Agents/chemistry ; Bone Marrow Stromal Antigen 2/metabolism ; GPI-Linked Proteins/metabolism ; HIV-1/metabolism ; Human Immunodeficiency Virus Proteins/antagonists & inhibitors ; Human Immunodeficiency Virus Proteins/metabolism ; Leukemia Virus, Gibbon Ape/metabolism ; Small Molecule Libraries ; Viral Regulatory and Accessory Proteins/antagonists & inhibitors ; Viral Regulatory and Accessory Proteins/metabolism ; Viroporin Proteins/antagonists & inhibitors
Chemical Substances	Anti-HIV Agents ; Bone Marrow Stromal Antigen 2 ; GPI-Linked Proteins ; Human Immunodeficiency Virus Proteins ; Small Molecule Libraries ; Viral Regulatory and Accessory Proteins ; Viroporin Proteins ; vpu protein, Human immunodeficiency virus 1
Language	English
Publishing date	2022-04-15
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2516098-9
ISSN	1999-4915 ; 1999-4915
ISSN (online)	1999-4915
ISSN	1999-4915
DOI	10.3390/v14040817
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: A role for GLUT3 in glioblastoma cell invasion that is not recapitulated by GLUT1.

Libby, Catherine J / Gc, Sajina / Benavides, Gloria A / Fisher, Jennifer L / Williford, Sarah E / Zhang, Sixue / Tran, Anh Nhat / Gordon, Emily R / Jones, Amber B / Tuy, Kaysaw / Flavahan, William / Gordillo, Juan / Long, Ashlee / Cooper, Sara J / Lasseigne, Brittany N / Augelli-Szafran, Corinne E / Darley-Usmar, Victor / Hjelmeland, Anita B

Cell adhesion & migration

2021 Volume 15, Issue 1, Page(s) 101–115

Abstract: ... in glycolytic metabolism that correlated with invasive phenotypes. We identified the GLUT3 C-terminus ... as mediating invasion: substituting the C-terminus of GLUT1 for that of GLUT3 reduced invasion. RNA-seq ...

Abstract	The multifaceted roles of metabolism in invasion have been investigated across many cancers. The brain tumor glioblastoma (GBM) is a highly invasive and metabolically plastic tumor with an inevitable recurrence. The neuronal glucose transporter 3 (GLUT3) was previously reported to correlate with poor glioma patient survival and be upregulated in GBM cells to promote therapeutic resistance and survival under restricted glucose conditions. It has been suggested that the increased glucose uptake mediated by GLUT3 elevation promotes survival of circulating tumor cells to facilitate metastasis. Here we suggest a more direct role for GLUT3 in promoting invasion that is not dependent upon changes in cell survival or metabolism. Analysis of glioma datasets demonstrated that GLUT3, but not GLUT1, expression was elevated in invasive disease. In human xenograft derived GBM cells, GLUT3, but not GLUT1, elevation significantly increased invasion in transwell assays, but not growth or migration. Further, there were no changes in glycolytic metabolism that correlated with invasive phenotypes. We identified the GLUT3 C-terminus as mediating invasion: substituting the C-terminus of GLUT1 for that of GLUT3 reduced invasion. RNA-seq analysis indicated changes in extracellular matrix organization in GLUT3 overexpressing cells, including upregulation of osteopontin. Together, our data suggest a role for GLUT3 in increasing tumor cell invasion that is not recapitulated by GLUT1, is separate from its role in metabolism and survival as a glucose transporter, and is likely broadly applicable since GLUT3 expression correlates with metastasis in many solid tumors.
MeSH term(s)	Brain Neoplasms/genetics ; Brain Neoplasms/metabolism ; Brain Neoplasms/pathology ; Gene Expression Regulation, Neoplastic ; Glioblastoma/genetics ; Glioblastoma/metabolism ; Glioblastoma/pathology ; Glucose Transporter Type 1/genetics ; Glucose Transporter Type 1/metabolism ; Glucose Transporter Type 3/genetics ; Glucose Transporter Type 3/metabolism ; Humans ; Nerve Tissue Proteins/metabolism ; Osteopontin/metabolism ; RNA-Seq
Chemical Substances	Glucose Transporter Type 1 ; Glucose Transporter Type 3 ; Nerve Tissue Proteins ; SLC2A1 protein, human ; SLC2A3 protein, human ; Osteopontin (106441-73-0)
Language	English
Publishing date	2021-04-10
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	2268518-2
ISSN	1933-6926 ; 1933-6918
ISSN (online)	1933-6926
ISSN	1933-6918
DOI	10.1080/19336918.2021.1903684
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: A limb-girdle muscular dystrophy 2I model of muscular dystrophy identifies corrective drug compounds for dystroglycanopathies.

Serafini, Peter R / Feyder, Michael J / Hightower, Rylie M / Garcia-Perez, Daniela / Vieira, Natássia M / Lek, Angela / Gibbs, Devin E / Moukha-Chafiq, Omar / Augelli-Szafran, Corinne E / Kawahara, Genri / Widrick, Jeffrey J / Kunkel, Louis M / Alexander, Matthew S

JCI insight

2018 Volume 3, Issue 18

Abstract: ... as limb-girdle muscular dystrophy 2I (LGMD2I), whereas patients with more C-terminal pathogenic mutations develop the severe ...

Abstract	Zebrafish are a powerful tool for studying muscle function owing to their high numbers of offspring, low maintenance costs, evolutionarily conserved muscle functions, and the ability to rapidly take up small molecular compounds during early larval stages. Fukutin-related protein (FKRP) is a putative protein glycosyltransferase that functions in the Golgi apparatus to modify sugar chain molecules of newly translated proteins. Patients with mutations in the FKRP gene can have a wide spectrum of clinical symptoms with varying muscle, eye, and brain pathologies depending on the location of the mutation in the FKRP protein. Patients with a common L276I FKRP mutation have mild adult-onset muscle degeneration known as limb-girdle muscular dystrophy 2I (LGMD2I), whereas patients with more C-terminal pathogenic mutations develop the severe Walker-Warburg syndrome (WWS)/muscle-eye-brain (MEB) disease. We generated fkrp-mutant zebrafish that phenocopy WWS/MEB pathologies including severe muscle breakdowns, head malformations, and early lethality. We have also generated a milder LGMD2I-model zebrafish via overexpression of a heat shock-inducible human FKRP (L276I) transgene that shows milder muscle pathology. Screening of an FDA-approved drug compound library in the LGMD2I zebrafish revealed a strong propensity towards steroids, antibacterials, and calcium regulators in ameliorating FKRP-dependent pathologies. Together, these studies demonstrate the utility of the zebrafish to both study human-specific FKRP mutations and perform compound library screenings for corrective drug compounds to treat muscular dystrophies.
MeSH term(s)	Animals ; Animals, Genetically Modified ; Disease Models, Animal ; Drug Evaluation, Preclinical ; Gene Knockout Techniques ; Glycosyltransferases/genetics ; Glycosyltransferases/metabolism ; Humans ; Locomotion ; Movement ; Muscle, Skeletal/physiopathology ; Muscular Dystrophies/drug therapy ; Muscular Dystrophies/genetics ; Muscular Dystrophies/physiopathology ; Muscular Dystrophies, Limb-Girdle/drug therapy ; Muscular Dystrophies, Limb-Girdle/genetics ; Muscular Dystrophies, Limb-Girdle/physiopathology ; Mutation ; Phenotype ; Proteins ; Transcriptome ; Walker-Warburg Syndrome ; Zebrafish ; Zebrafish Proteins/genetics ; Zebrafish Proteins/metabolism
Chemical Substances	FKRP protein, human ; Proteins ; Zebrafish Proteins ; FKRP protein, zebrafish (EC 2.4.-) ; Glycosyltransferases (EC 2.4.-)
Language	English
Publishing date	2018-09-20
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ISSN	2379-3708
ISSN (online)	2379-3708
DOI	10.1172/jci.insight.120493
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Inter-library loan at ZB MED

Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

Article ; Online: Identification of Quinolinones as Antivirals against Venezuelan Equine Encephalitis Virus.

Haese, Nicole N / May, Nicholas A / Taft-Benz, Sharon / Moukha-Chafiq, Omar / Madadi, Nikhil / Zhang, Sixue / Karyakarte, Shuklendu D / Rodzinak, Kevin J / Nguyen, Theresa H / Denton, Michael / Streblow, Aaron D / Towers, Nichole A / Rasmussen, Lynn / Bostwick, Robert J / Maddry, Joseph A / Ananthan, Subramaniam / Augelli-Szafran, Corinne E / Suto, Mark J / Sanders, Wes /

Moorman, Nathaniel / DeFilippis, Victor / Heise, Mark T / Pathak, Ashish K / Streblow, Daniel N / Morrison, Thomas E

Antimicrobial agents and chemotherapy

2021 Volume 65, Issue 9, Page(s) e0024421

Abstract: ... Deep sequencing and reverse genetics studies identified two unique resistance mutations in the nsP2 gene (Y102S/C ...

Abstract	Venezuelan equine encephalitis virus (VEEV) is a reemerging alphavirus that can cause encephalitis resulting in severe human morbidity and mortality. Using a high-throughput cell-based screen, we identified a quinolinone compound that protected against VEEV-induced cytopathic effects. Analysis of viral replication in cells identified several quinolinone compounds with potent inhibitory activity against vaccine and virulent strains of VEEV. These quinolinones also displayed inhibitory activity against additional alphaviruses, such as Mayaro virus and Ross River virus, although the potency was greatly reduced. Time-of-addition studies indicated that these compounds inhibit the early-to-mid stage of viral replication. Deep sequencing and reverse genetics studies identified two unique resistance mutations in the nsP2 gene (Y102S/C; stalk domain) that conferred VEEV resistance on this chemical series. Moreover, introduction of a K102Y mutation into the nsP2 gene enhanced the sensitivity of chikungunya virus (CHIKV) to this chemical series. Computational modeling of CHIKV and VEEV nsP2 identified a highly probable docking alignment for the quinolinone compounds that require a tyrosine residue at position 102 within the helicase stalk domain. These studies identified a class of compounds with antiviral activity against VEEV and other alphaviruses and provide further evidence that therapeutics targeting nsP2 may be useful against alphavirus infection.
MeSH term(s)	Animals ; Antiviral Agents/pharmacology ; Chikungunya virus ; Encephalitis Virus, Venezuelan Equine/genetics ; Horses ; Humans ; Quinolones/pharmacology ; Virus Replication
Chemical Substances	Antiviral Agents ; Quinolones
Language	English
Publishing date	2021-08-17
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	217602-6
ISSN	1098-6596 ; 0066-4804
ISSN (online)	1098-6596
ISSN	0066-4804
DOI	10.1128/AAC.00244-21
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 809: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (1.OG) ab Jg. 2022: Lesesaal (EG)
Einzelsignatur: Show issues

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.

Ahmed, S Kaleem / Haese, Nicole N / Cowan, Jaden T / Pathak, Vibha / Moukha-Chafiq, Omar / Smith, Valerie J / Rodzinak, Kevin J / Ahmad, Fahim / Zhang, Sixue / Bonin, Kiley M / Streblow, Aaron D / Streblow, Cassilyn E / Kreklywich, Craig N / Morrison, Clayton / Sarkar, Sanjay / Moorman, Nathaniel / Sander, Wes / Allen, Robbie / DeFilippis, Victor /

Tekwani, Babu L / Wu, Mousheng / Hirsch, Alec J / Smith, Jessica L / Tower, Nichole A / Rasmussen, Lynn / Bostwick, Robert / Maddry, Joseph A / Ananthan, Subramaniam / Gerdes, John M / Augelli-Szafran, Corinne E / Suto, Mark J / Morrison, Thomas E / Heise, Mark T / Streblow, Daniel N / Pathak, Ashish K

Journal of medicinal chemistry

2021 Volume 64, Issue 8, Page(s) 4762–4786

Abstract: A benzo[6]annulene, 4-( ...

Abstract	A benzo[6]annulene, 4-(
MeSH term(s)	Animals ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacokinetics ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Benzene Derivatives/chemistry ; Benzene Derivatives/metabolism ; Benzene Derivatives/pharmacology ; Benzene Derivatives/therapeutic use ; Binding Sites ; Cell Line ; Cell Survival/drug effects ; Chikungunya Fever/drug therapy ; Chikungunya virus/physiology ; Dihydroorotate Dehydrogenase ; Disease Models, Animal ; Female ; Half-Life ; Humans ; Male ; Mice ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Oxidoreductases Acting on CH-CH Group Donors/antagonists & inhibitors ; Oxidoreductases Acting on CH-CH Group Donors/metabolism ; Structure-Activity Relationship ; Virus Replication/drug effects
Chemical Substances	Antiviral Agents ; Benzene Derivatives ; Dihydroorotate Dehydrogenase ; Oxidoreductases Acting on CH-CH Group Donors (EC 1.3.-)
Language	English
Publishing date	2021-04-09
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c02183
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Discovery of notch-sparing gamma-secretase inhibitors.

Augelli-Szafran, C E / Wei, H-X / Lu, D / Zhang, J / Gu, Y / Yang, T / Osenkowski, P / Ye, W / Wolfe, M S

Current Alzheimer research

2010 Volume 7, Issue 3, Page(s) 207–209

Abstract: ... gamma-secretase, which generates the C-terminus of Abeta; however, gamma-secretase inhibitors cause serious ...

Abstract	Overwhelming evidence supports a central role for the amyloid beta-peptide (Abeta) in the pathogenesis of Alzheimer's disease (AD), and the proteases that produce Abeta from its precursor protein APP are top targets for therapeutic intervention. Considerable effort has focused on targeting gamma-secretase, which generates the C-terminus of Abeta; however, gamma-secretase inhibitors cause serious toxicities due to interference with the Notch signaling pathway. We have been working toward compounds that directly alter gamma-secretase activity to reduce Abeta production without affecting the proteolysis of Notch. Using purified enzyme and substrate, we have shown that gamma-secretase can be selectively inhibited in this way by naphthyl-substituted gamma-aminoketones and gamma-aminoalcohols. These early hits, however, suffered from chemical instability and/or poor potency. Iterative design, synthesis and evaluation have led to the discovery of Notch-sparing gamma-secretase inhibitors with substantially increased potencies in biochemical and cellular assays. These compounds are of low molecular weight and are under evaluation for drug-like properties. The discovery and development of these compounds will be discussed.
MeSH term(s)	Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Alzheimer Disease/physiopathology ; Amyloid Precursor Protein Secretases/antagonists & inhibitors ; Amyloid Precursor Protein Secretases/metabolism ; Amyloid beta-Peptides/antagonists & inhibitors ; Amyloid beta-Peptides/biosynthesis ; Animals ; Disease Models, Animal ; Drug Design ; Drug Evaluation, Preclinical/methods ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Humans ; Molecular Structure ; Receptors, Notch/drug effects ; Receptors, Notch/metabolism ; Signal Transduction/drug effects ; Signal Transduction/physiology
Chemical Substances	Amyloid beta-Peptides ; Enzyme Inhibitors ; Receptors, Notch ; Amyloid Precursor Protein Secretases (EC 3.4.-)
Language	English
Publishing date	2010-01-19
Publishing country	United Arab Emirates
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2205170-3
ISSN	1875-5828 ; 1567-2050
ISSN (online)	1875-5828
ISSN	1567-2050
DOI	10.2174/156720510791050920
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 6235: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: The synthesis and structure-activity relationship of substituted N-phenyl anthranilic acid analogs as amyloid aggregation inhibitors.

Simons, Lloyd J / Caprathe, Bradley W / Callahan, Michael / Graham, James M / Kimura, Takenori / Lai, Yingjie / LeVine, Harry / Lipinski, William / Sakkab, Annette T / Tasaki, Yoshikazu / Walker, Lary C / Yasunaga, Tomoyuki / Ye, Yuyang / Zhuang, Nian / Augelli-Szafran, Corinne E

Bioorganic & medicinal chemistry letters

2009 Volume 19, Issue 3, Page(s) 654–657

Abstract: It is believed that beta-amyloid aggregation is an important event in the development of Alzheimer's disease. In the course of our studies to identify beta-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and ...

Abstract	It is believed that beta-amyloid aggregation is an important event in the development of Alzheimer's disease. In the course of our studies to identify beta-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for beta-amyloid inhibition activity. The synthesis, structure-activity relationship, and in vivo activity of these analogs are discussed.
MeSH term(s)	Alzheimer Disease ; Amyloid/chemistry ; Animals ; Chemistry, Pharmaceutical/methods ; Disease Models, Animal ; Drug Design ; Enzyme Inhibitors/pharmacology ; Fenamates/chemical synthesis ; Fenamates/chemistry ; Humans ; Mice ; Microscopy, Atomic Force ; Models, Chemical ; Molecular Structure ; Peptides/chemistry ; Structure-Activity Relationship
Chemical Substances	Amyloid ; Enzyme Inhibitors ; Fenamates ; Peptides
Language	English
Publishing date	2009-02-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2008.12.049
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 3203: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article: Identification and characterization of m4 selective muscarinic antagonists.

Augelli-Szafran, C E / Jaen, J C / Moreland, D W / Nelson, C B / Penvose-Yi, J R / Schwarz, R D

Bioorganic & medicinal chemistry letters

1998 Volume 8, Issue 15, Page(s) 1991–1996

Abstract: Our interest in the area of m4 muscarinic antagonists had led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7 nM at m4 receptors, and 72-fold (m1), ... ...

Abstract	Our interest in the area of m4 muscarinic antagonists had led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7 nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.
MeSH term(s)	Isoquinolines/chemistry ; Isoquinolines/metabolism ; Isoquinolines/pharmacology ; Muscarinic Antagonists/chemistry ; Muscarinic Antagonists/metabolism ; Muscarinic Antagonists/pharmacology ; Protein Binding ; Receptor, Muscarinic M4 ; Receptors, Muscarinic/drug effects ; Receptors, Muscarinic/metabolism
Chemical Substances	Isoquinolines ; Muscarinic Antagonists ; Receptor, Muscarinic M4 ; Receptors, Muscarinic
Language	English
Publishing date	1998-08-04
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/s0960-894x(98)00351-5
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 3203: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article: Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.

Hudack, Raymond A / Barta, Nancy S / Guo, Chuangxing / Deal, Judith / Dong, Liming / Fay, Lorraine K / Caprathe, Bradley / Chatterjee, Arindam / Vanderpool, Darin / Bigge, Christopher / Showalter, Richard / Bender, Steve / Augelli-Szafran, Corinne E / Lunney, Elizabeth / Hou, Xinjun

Journal of medicinal chemistry

2006 Volume 49, Issue 3, Page(s) 1202–1206

Abstract: Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to show ... ...

Abstract	Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to show neuroregenerative activity in a variety of cell and animal models including neurite outgrowth, age-related cognitive decline, Parkinson's disease, peripheral nerve injury, optic nerve degeneration, and diabetic neuropathy. We have designed and synthesized a unique series of tetracyclic aza-amides that have been shown to be potent FKBP12 rotamase inhibitors. The structure-activity relationships established in this study have demonstrated diverse structural modifications that result in potent rotamase inhibitory activity.
MeSH term(s)	Amides/chemical synthesis ; Amides/chemistry ; Aza Compounds/chemical synthesis ; Aza Compounds/chemistry ; Binding Sites ; Heterocyclic Compounds, 4 or More Rings/chemical synthesis ; Heterocyclic Compounds, 4 or More Rings/chemistry ; Hydrogen Bonding ; Isoquinolines/chemical synthesis ; Isoquinolines/chemistry ; Ligands ; Neuroprotective Agents/chemical synthesis ; Neuroprotective Agents/chemistry ; Structure-Activity Relationship ; Tacrolimus/chemistry ; Tacrolimus Binding Protein 1A/antagonists & inhibitors ; Tacrolimus Binding Protein 1A/chemistry
Chemical Substances	Amides ; Aza Compounds ; Heterocyclic Compounds, 4 or More Rings ; Isoquinolines ; Ligands ; Neuroprotective Agents ; Tacrolimus Binding Protein 1A (EC 5.2.1.-) ; Tacrolimus (WM0HAQ4WNM)
Language	English
Publishing date	2006-02-09
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/jm049161u
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

To top

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

Order via subito

Inter-library loan at ZB MED

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito