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[PDF] Top 20 Small molecule inhibitors of CRM1

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Small molecule inhibitors of CRM1

Small molecule inhibitors of CRM1

... first molecule of this family of small molecule compounds was found by a screening effort aimed to identify new anti-HIV Rev inhibitors (Daelemans et ...collection of ... See full document

9

Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design.

Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design.

... screen of 500 compounds using surface plasmon resonance (SPR), NMR and crystallography (data not shown) using the His-tagged IN-CCD protein from ...location of binding respectively. One of the hits ... See full document

11

Computational improvement of small-molecule inhibitors of Bacillus anthracis protective antigen activation through isostere-based substitutions

Computational improvement of small-molecule inhibitors of Bacillus anthracis protective antigen activation through isostere-based substitutions

... several of the good candidates identified in the docking stage are not promising leads for further ...presence of concentrated charges in the moiety which binds to the “open” lobe of the cavity (as ... See full document

16

A distinct translation initiation mechanism generates cryptic peptides for immune surveillance.

A distinct translation initiation mechanism generates cryptic peptides for immune surveillance.

... to small molecule inhibitors Although edeine distinguished the initiation complexes assembled at the AUG versus CUG codons, its various other side-effects preclude its use in living cells (data not ... See full document

12

Small-molecule inhibition of HIV pre-mRNA splicing as a novel antiretroviral therapy to overcome drug resistance.

Small-molecule inhibition of HIV pre-mRNA splicing as a novel antiretroviral therapy to overcome drug resistance.

... prevalence of drug-resistant human immu- nodeficiency virus type 1 (HIV-1) has highlighted the challenging issue of the optimal treatment of HIV-1-infected patients ...consisting of various ... See full document

10

A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

... silencing of TbHKs [3,4], with cell toxicity observed after 3– 5 days of RNAi ...known inhibitors of HKs have been demonstrated to inhibit ...one of two nearly identical TbHKs that the ... See full document

8

Design and synthesis of small molecule modulators of p53

Design and synthesis of small molecule modulators of p53

... one of the most studied. It is widely regarded as the “guardian of the genome”, playing a pivotal part in the preservation of genomic integrity by regulating cell cycle, apoptosis, DNA repair, ... See full document

263

Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.

Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.

... use of cholesterol-lowering drugs, cardiovascular disease remains one of the leading causes of death worldwide and there is a need for novel approaches to improve therapies ...levels of cir- ... See full document

26

In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.

In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.

... pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to ...number of available antifungals is ... See full document

17

Antiviral activity of a small molecule deubiquitinase inhibitor occurs via induction of the unfolded protein response.

Antiviral activity of a small molecule deubiquitinase inhibitor occurs via induction of the unfolded protein response.

... killing of Listeria monocytogenes in murine macrophages ...replication of Norwalk virus in the replicon ...target of WP1130 in murine macrophages. Inhibition of USP14 activity reduced MNV-1 ... See full document

15

Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling

Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling

... collection of chemical derivatives to perform structure activity relationship ...identification of the molecular target of a bioactive com- pound is of key importance ...mode of action ... See full document

17

Client Proteins and Small Molecule Inhibitors Display Distinct Binding Preferences for Constitutive and Stress-Induced HSP90 Isoforms and Their Conformationally Restricted Mutants.

Client Proteins and Small Molecule Inhibitors Display Distinct Binding Preferences for Constitutive and Stress-Induced HSP90 Isoforms and Their Conformationally Restricted Mutants.

... isoforms of the molecular chaperone HSP90, stress-inducible HSP90α and constitutively expressed HSP90β, fold, assemble and maintain the three- dimensional structure of numerous client ...HSP90 ... See full document

15

Potent host-directed small-molecule inhibitors of myxovirus RNA-dependent RNA-polymerases.

Potent host-directed small-molecule inhibitors of myxovirus RNA-dependent RNA-polymerases.

... inhibition of paramyxovirus family members was assessed, six compounds efficiently blocked the closely related canine distemper virus (CDV) and the more distantly related human parainfluenzavirus type 3 (HPIV3) in ... See full document

14

Small molecule inhibitors target the tissue transglutaminase and fibronectin interaction.

Small molecule inhibitors target the tissue transglutaminase and fibronectin interaction.

... mixture of 10 nM TG2 and 3 nM FN42 was used and SMIs were added at 1–30 mM ...SE of three ...presence of various concentrations of TG53 (from 0 mM to 16 ...concentration of inhibitor, ... See full document

10

The identification of a small molecule compound that reduces HIV-1 Nef-mediated viral infectivity enhancement.

The identification of a small molecule compound that reduces HIV-1 Nef-mediated viral infectivity enhancement.

... absence of 2c at the indicated ...concentration of p24 Gag protein in the supernatants using the RETROtek p24 Antigen ELISA kit ...expression of viral proteins in the cells by Western blotting. The ... See full document

12

Small molecule proprotein convertase inhibitors for inhibition of embryo implantation.

Small molecule proprotein convertase inhibitors for inhibition of embryo implantation.

... synthetic small molecule compounds derived from 2,5-dideoxystreptamine chemical scaf- fold previously reported by Jiao et ...Four of these compounds (1e, 1f, 1g, 1n) were previously shown to be ... See full document

8

Identification of small molecule inhibitors of PTPσ through an integrative virtual and biochemical approach.

Identification of small molecule inhibitors of PTPσ through an integrative virtual and biochemical approach.

... number of PTP experimental structures resolved by X-ray crystallography has stimulated structure-guided efforts to identify small molecule PTP ...descriptions of the biological roles, target ... See full document

8

The role of stress-activated protein kinase signaling in renal pathophysiology

The role of stress-activated protein kinase signaling in renal pathophysiology

... activation of both p38 and JNK pathways occurs in human renal disease, including glomerulonephritis, diabetic nephropathy and acute renal ...Administration of small molecule inhibitors ... See full document

9

J. Braz. Chem. Soc.  vol.25 número10

J. Braz. Chem. Soc. vol.25 número10

... properties of this protein in its full-length state is therefore key to improving our understanding of the flavivirus life cycle and informing the design of effective antiviral ...conservation ... See full document

11

The small molecule inhibitor QLT0267 Radiosensitizes squamous cell carcinoma cells of the head and neck.

The small molecule inhibitor QLT0267 Radiosensitizes squamous cell carcinoma cells of the head and neck.

... variety of human tumor cell models and in mouse fibroblasts ...targeting of ILK in patients receiving radiotherapy is highly questionable at the ...function of ILK, which suggested ILK as potent ... See full document

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