Application of a Sulfoxonium Ylide Electrophile to Generate Cathepsin X-Selective Activity-Based Probes

Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease. Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl) (4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity and antiviral activity against two important human enteroviruses (HEVs) members of the Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)]. Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a (CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense), double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant antiviral activity was determined. Conclusion: These results point towards a selective activity against CVB-5, an important human pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised patients.

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Novel open-ring analogues of N5,N10-methylenetetrahydrofolic acid with selective activity against brain tumor

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/0960-894x(95)00321-j ◽

1995 ◽

Vol 5 (17) ◽

pp. 1909-1912 ◽

Cited By ~ 2

Author(s):

Hui-po Wang ◽

Tung-shing Bai ◽

On Lee ◽

Kai-der Ker

Keyword(s):

Brain Tumor ◽

Open Ring ◽

Selective Activity

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Tool Selectivity in Left Occipitotemporal Cortex Develops without Vision

Journal of Cognitive Neuroscience ◽

10.1162/jocn_a_00411 ◽

2013 ◽

Vol 25 (8) ◽

pp. 1225-1234 ◽

Cited By ~ 48

Author(s):

Marius V. Peelen ◽

Stefania Bracci ◽

Xueming Lu ◽

Chenxi He ◽

Alfonso Caramazza ◽

...

Keyword(s):

Functional Organization ◽

Auditory Task ◽

Anatomical Location ◽

Resting State Functional Connectivity ◽

Frontoparietal Network ◽

Congenitally Blind ◽

Occipitotemporal Cortex ◽

Auditory Tasks ◽

Tool Motion ◽

Selective Activity

Previous studies have provided evidence for a tool-selective region in left lateral occipitotemporal cortex (LOTC). This region responds selectively to pictures of tools and to characteristic visual tool motion. The present human fMRI study tested whether visual experience is required for the development of tool-selective responses in left LOTC. Words referring to tools, animals, and nonmanipulable objects were presented auditorily to 14 congenitally blind and 16 sighted participants. Sighted participants additionally viewed pictures of these objects. In whole-brain group analyses, sighted participants showed tool-selective activity in left LOTC in both visual and auditory tasks. Importantly, virtually identical tool-selective LOTC activity was found in the congenitally blind group performing the auditory task. Furthermore, both groups showed equally strong tool-selective activity for auditory stimuli in a tool-selective LOTC region defined by the picture-viewing task in the sighted group. Detailed analyses in individual participants showed significant tool-selective LOTC activity in 13 of 14 blind participants and 14 of 16 sighted participants. The strength and anatomical location of this activity were indistinguishable across groups. Finally, both blind and sighted groups showed significant resting state functional connectivity between left LOTC and a bilateral frontoparietal network. Together, these results indicate that tool-selective activity in left LOTC develops without ever having seen a tool or its motion. This finding puts constraints on the possible role that this region could have in tool processing and, more generally, provides new insights into the principles shaping the functional organization of OTC.

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Important Amino Acid Residues that Confer CYP2C19 Selective Activity to CYP2C9

The Journal of Biochemistry ◽

10.1093/jb/mvn070 ◽

2008 ◽

Vol 144 (3) ◽

pp. 323-333 ◽

Cited By ~ 14

Author(s):

Y. Wada ◽

M. Mitsuda ◽

Y. Ishihara ◽

M. Watanabe ◽

M. Iwasaki ◽

...

Keyword(s):

Amino Acid ◽

Amino Acid Residues ◽

Important Amino Acid ◽

Selective Activity

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Durable and selective activity of Pd loaded on WO3/ZrO2 for NOCH4O2 in the presence of water vapor

Applied Catalysis B Environmental ◽

10.1016/s0926-3373(02)00206-0 ◽

2003 ◽

Vol 41 (1-2) ◽

pp. 137-142 ◽

Cited By ~ 16

Author(s):

Kazu Okumura ◽

Tetsuji Kusakabe ◽

Miki Niwa

Keyword(s):

Water Vapor ◽

Selective Activity

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Induction of Premalignant Host Responses by Cathepsin X/Z-Deficiency in Helicobacter Pylori-Infected Mice

PLoS ONE ◽

10.1371/journal.pone.0070242 ◽

2013 ◽

Vol 8 (7) ◽

pp. e70242 ◽

Cited By ~ 9

Author(s):

Sabine Krueger ◽

Anja Bernhardt ◽

Thomas Kalinski ◽

Martin Baldensperger ◽

Michael Zeh ◽

...

Keyword(s):

Helicobacter Pylori ◽

Host Responses ◽

Cathepsin X

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Desketoneoenactin-Siderophore Conjugates for Candida: Evidence of Iron Transport-Dependent Species Selectivity

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.49.1.241-248.2005 ◽

2005 ◽

Vol 49 (1) ◽

pp. 241-248 ◽

Cited By ~ 23

Author(s):

Geneviève Bernier ◽

Vinay Girijavallabhan ◽

Aaron Murray ◽

Noormohamed Niyaz ◽

Pingyu Ding ◽

...

Keyword(s):

Inhibitory Activity ◽

Parent Strain ◽

Iron Transport ◽

Growth Promotion ◽

Common Mechanism ◽

Iron Availability ◽

Species Selectivity ◽

Drug Conjugates ◽

Siderophore Transporter ◽

Selective Activity

ABSTRACT We investigated the inhibitory activity of synthetic isocyanurate-based as well as linear mono- and trihydroxamate siderophore-drug conjugates against Candida spp. The conjugated drug was 13C-desketoneoenactin (DE). The MICs of siderophore-drug conjugates were determined in the absence and presence of 2,2′-dipyridyl to restrict iron availability. The ability of various siderophore types to promote growth in an iron-restricted medium was also assayed. Addition of a siderophore portion to the drug strongly impaired the inhibitory activity of DE. However, the activity of the drug conjugates was increased by up to 16-fold in iron-depleted medium for species having their growth strongly promoted by most hydroxamate-type siderophores (C. albicans, C. stellatoidea, and C. pseudotropicalis). The uptake of 55Fe from ferrichrome and from two siderophore-drug conjugates was improved when C. albicans cells were grown in a low-iron medium. In the same assay, unlabeled ferrichrome was able to compete with the uptake of 55Fe from both conjugates, indicating a common mechanism of uptake. A C. albicans strain lacking the siderophore transporter CaSit1/CaArn1 was not able to use ferrichrome or the synthetic ornithine-based trihydroxamate siderophore for growth promotion and was much less susceptible to the siderophore-drug conjugates than its isogenic parent strain. In summary, the ability of some Candida spp. to use ferrichrome-like siderophores for growth promotion explains the selective activity of hydroxamate-drug conjugates, and this activity seems to be related to the presence, in C. albicans, of the siderophore transporter CaSit1/CaArn1. New conjugate designs are necessary to fully restore or improve the initial DE activity.

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