scholarly journals Design and synthesis of active heparan sulfate-based probes

2015 ◽  
Vol 51 (55) ◽  
pp. 11019-11021 ◽  
Author(s):  
Wen Zhou ◽  
Po-Hung Hsieh ◽  
Yongmei Xu ◽  
Timothy R. O’Leary ◽  
Xuefei Huang ◽  
...  
Keyword(s):  
Heparan Sulfate ◽  
Molecular Probes ◽  
Design And Synthesis ◽  
Sulfated Carbohydrate ◽  
Specific Inhibitors

Synthesis of sulfated carbohydrate molecular probes and the utilities as specific inhibitors for carbohydrate sulfotransferases.

scholarly journals Design and synthesis of molecular probes for the determination of the target of the anthelmintic drug praziquantel

2014 ◽  
Vol 24 (11) ◽  
pp. 2469-2472 ◽  
Author(s):  
Lalit Kumar Sharma ◽  
Pauline M. Cupit ◽  
Tino Goronga ◽  
Thomas R. Webb ◽  
Charles Cunningham
Keyword(s):  
Molecular Probes ◽  
Anthelmintic Drug ◽  
Design And Synthesis

Design And Synthesis Of Dual-Affinity Molecular Probes Targeting The Opioid Receptors

Planta Medica ◽  
2016 ◽  
Vol 82 (05) ◽  
Author(s):  
AW Keasling ◽  
IA Khan ◽  
BL Roth ◽  
JK Zjawiony
Keyword(s):  
Opioid Receptors ◽  
Molecular Probes ◽  
Design And Synthesis

Tailored Design and Synthesis of Heparan Sulfate Oligosaccharide Analogues Using Sequential One-Pot Multienzyme Systems

2013 ◽  
Vol 125 (45) ◽  
pp. 12068-12072 ◽  
Author(s):  
Yi Chen ◽  
Yanhong Li ◽  
Hai Yu ◽  
Go Sugiarto ◽  
Vireak Thon ◽  
...  
Keyword(s):  
Heparan Sulfate ◽  
One Pot ◽  
Design And Synthesis ◽  
Tailored Design

Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents

2004 ◽  
Vol 14 (10) ◽  
pp. 2505-2509 ◽  
Author(s):  
Keisuke Ishida ◽  
Siro Simizu ◽  
Takayuki Teruya ◽  
Michal K. Wierzba ◽  
Hiroyuki Osada
Keyword(s):  
Heparan Sulfate ◽  
Rational Design ◽  
Design And Synthesis

Design and synthesis of structurally defined heparan sulfate (HS)-FK506 conjugates as an exogenous approach to investigate biological functions of nucleus HS

2018 ◽  
Vol 81 ◽  
pp. 203-210
Author(s):  
MaoLin Li ◽  
SiSi. Yuan ◽  
Jian Chen ◽  
Li Lv ◽  
ShiYin Guo ◽  
...  
Keyword(s):  
Heparan Sulfate ◽  
Biological Functions ◽  
Design And Synthesis

DESIGN AND SYNTHESIS OF SPECIFIC INHIBITORS OF THE 3′-PROCESSING STEP OF HIV-1 INTEGRASE

2005 ◽  
Vol 24 (5-7) ◽  
pp. 481-484 ◽  
Author(s):  
Guochen Chi ◽  
Byung I. Seo ◽  
Vasu Nair
Keyword(s):  
Design And Synthesis ◽  
Processing Step ◽  
Hiv 1 ◽  
Specific Inhibitors

scholarly journals Development of Isoform-specific Sensors of Polypeptide GalNAc-transferase Activity

2014 ◽  
Vol 289 (44) ◽  
pp. 30556-30566 ◽  
Author(s):  
Lina Song ◽  
Collin Bachert ◽  
Katrine T. Schjoldager ◽  
Henrik Clausen ◽  
Adam D. Linstedt
Keyword(s):  
High Throughput Screening ◽  
Secretory Pathway ◽  
Molecular Probes ◽  
Transferase Activity ◽  
Recognition Sequence ◽  
Fluorescence Sensors ◽  
Vast Array ◽  
Enzyme Recognition ◽  
Specific Inhibitors

Humans express up to 20 isoforms of GalNAc-transferase (herein T1–T20) that localize to the Golgi apparatus and initiate O-glycosylation. Regulation of this enzyme family affects a vast array of proteins transiting the secretory pathway and diseases arise upon misregulation of specific isoforms. Surprisingly, molecular probes to monitor GalNAc-transferase activity are lacking and there exist no effective global or isoform-specific inhibitors. Here we describe the development of T2- and T3-isoform specific fluorescence sensors that traffic in the secretory pathway. Each sensor yielded little signal when glycosylated but was strongly activated in the absence of its glycosylation. Specificity of each sensor was assessed in HEK cells with either the T2 or T3 enzymes deleted. Although the sensors are based on specific substrates of the T2 and T3 enzymes, elements in or near the enzyme recognition sequence influenced their activity and required modification, which we carried out based on previous in vitro work. Significantly, the modified T2 and T3 sensors were activated only in cells lacking their corresponding isozymes. Thus, we have developed T2- and T3-specific sensors that will be valuable in both the study of GalNAc-transferase regulation and in high-throughput screening for potential therapeutic regulators of specific GalNAc-transferases.

Design and Synthesis of New Sulfonamides-Based Flt3 Inhibitors

2020 ◽  
Vol 16 (3) ◽  
pp. 403-412
Author(s):  
Reem F. Abutayeh ◽  
Jehad Almaliti ◽  
Mutasem O. Taha
Keyword(s):  
Acute Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Design And Synthesis ◽  
Flt3 Inhibitors ◽  
Crystallographic Structures ◽  
Specific Inhibitors ◽  
Acute Myeloid ◽  
Privileged Scaffolds

Background: Flt3 is an oncogenic kinase involved in different leukemias. It is most prominently associated with acute myeloid leukemia (AML). Flt3-specific inhibitors have shown promising results in interfering with AML. Methods: The crystallographic structures of two inhibitors complexed within Flt3, namely, quizartinib and F6M, were used to guide the synthesis of new sulfonamide-based Flt3 inhibitors. Results: One of the prepared compounds showed low micromolar anti-Flt3 bioactivity, and interestingly, low micromolar bioactivity against the related oncogenic kinase VEGFR2. Conclusion: Sulfonamides were successfully used as privileged scaffolds for the synthesis of novel Flt3 inhibitors of micromolar potencies.

scholarly journals Design and assembly of supramolecular dual-modality nanoprobes

Nanoscale ◽  
2015 ◽  
Vol 7 (21) ◽  
pp. 9462-9466 ◽  
Author(s):  
Shuang Liu ◽  
Pengcheng Zhang ◽  
Sangeeta Ray Banerjee ◽  
Jiadi Xu ◽  
Martin G. Pomper ◽  
...  
Keyword(s):  
Optical Imaging ◽  
Metal Ion ◽  
Molecular Probes ◽  
Dual Modality ◽  
Design And Synthesis ◽  
Self Assembling

We report the design and synthesis of self-assembling dual-modality molecular probes containing both a fluorophore for optical imaging and a metal ion chelator for imaging with MRI or radionuclide methods.

scholarly journals Strigolactone Analogs as Molecular Probes in Chasing the (SLs) Receptor/s: Design and Synthesis of Fluorescent Labeled Molecules

2013 ◽  
Vol 6 (1) ◽  
pp. 113-127 ◽  
Author(s):  
Cristina Prandi ◽  
Helèna Rosso ◽  
Beatrice Lace ◽  
Ernesto G. Occhiato ◽  
Alberto Oppedisano ◽  
...  
Keyword(s):  
Molecular Probes ◽  
Design And Synthesis
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