Computer Modeling-Assisted Design And Synthesis Of Flavonols Derivatives As Proteasome Inhibitors

Planta Medica ◽  
2016 ◽  
Vol 82 (05) ◽  
Author(s):  
KY Orabi ◽  
MS Abaza ◽  
KA ElSayed ◽  
AY Elnagar ◽  
SI Faggal ◽  
...  
Keyword(s):  
Computer Modeling ◽  
Proteasome Inhibitors ◽  
Design And Synthesis

Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors

2007 ◽  
Vol 17 (4) ◽  
pp. 1102-1106 ◽  
Author(s):  
Yiqiu Fu ◽  
Bo Xu ◽  
Xiaomin Zou ◽  
Chao Ma ◽  
Xiaoming Yang ◽  
...  
Keyword(s):  
Proteasome Inhibitors ◽  
20S Proteasome ◽  
Design And Synthesis

Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors

2012 ◽  
Vol 22 (8) ◽  
pp. 2772-2774 ◽  
Author(s):  
Kai Xu ◽  
Zhiyan Xiao ◽  
Yan Bo Tang ◽  
Li Huang ◽  
Chin-Ho Chen ◽  
...  
Keyword(s):  
Proteasome Inhibitors ◽  
20S Proteasome ◽  
Antiproliferative Agents ◽  
Design And Synthesis

scholarly journals Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors

2020 ◽  
Vol 1 (5) ◽  
pp. 305-332
Author(s):  
Grace E. Hubbell ◽  
Jetze J. Tepe
Keyword(s):  
Neurodegenerative Disease ◽  
Natural Product ◽  
Parasitic Infection ◽  
Proteasome Inhibitors ◽  
20S Proteasome ◽  
Design And Synthesis

The 20S proteasome is a valuable target for the treatment of a number of diseases including cancer, neurodegenerative disease, and parasitic infection.

The design and synthesis of nonpeptide compounds as mimics of a conformation of methionine-enkephaline

1982 ◽  
Vol 60 (8) ◽  
pp. 1019-1029 ◽  
Author(s):  
Patrice C. Belanger ◽  
Claude Dufresne ◽  
John Scheigetz ◽  
Robert N. Young ◽  
James P. Springer ◽  
...  
Keyword(s):  
Double Bond ◽  
Computer Modeling ◽  
High Yield ◽  
Side Chain ◽  
Active Conformation ◽  
Methionine Enkephalin ◽  
Design And Synthesis ◽  
Structural Template ◽  
Subsequent Addition

A model for the active conformation of methionine-enkephalin containing a β-turn was derived from computer modeling. Using a trans-perhydronaphthalene as a structural template and a mimic of the β-turn, target compounds were designed and synthesized. Thus, a key intermediate, trans-3-oxo-5β-formamidomethyl-8a-phenylmethylperhydronaphthalene, was prepared by two different routes from cyclohexanone.The addition of a methionine-like side-chain to this key intermediate was best achieved by a reaction with the anion of methyl 2-trimethylsilyl-4-methylthiobutanoate. This led to the preparation of an exo-tetrasubstituted double bond in high yield. Subsequent addition of tyrosine through coupling with the 5β-aminomethyl group provided the desired perhydronaphthalene mimics of met-enkaphalin.

Prostatic Acid Phosphatase (PAP) Differentiated Ultracytochemically from Lysosomal Acid Phosphate in the Rat with a PAP/Specific Substrate, Phosphorylcholine

1975 ◽  
Vol 33 ◽  
pp. 450-451
Author(s):  
W. Allen Shannon ◽  
José A. Serrano ◽  
Hannah L. Wasserkrug ◽  
Anna A. Serrano ◽  
Arnold M. Seligman
Keyword(s):  
Acid Phosphatase ◽  
Phosphate Buffer ◽  
Prostatic Carcinoma ◽  
Prostatic Acid Phosphatase ◽  
Chemotherapeutic Agents ◽  
Specific Substrate ◽  
Acid Phosphate ◽  
Lysosomal Acid ◽  
Design And Synthesis ◽  
New Chemotherapeutic Agents

During the design and synthesis of new chemotherapeutic agents for prostatic carcinoma based on phosphorylated agents which might be enzyme-activated to cytotoxicity, phosphorylcholine, [(CH3)3+NCH2CH2OPO3Ca]Cl-, has been indicated to be a very specific substrate for prostatic acid phosphatase (PAP). This phenomenon has led to the development of specific histochemical and ultracytochemical methods for PAP using modifications of the Gomori lead method for acid phosphatase. Comparative histochemical results in prostate and kidney of the rat have been published earlier with phosphorylcholine (PC) and β-glycerophosphate (βGP). We now report the ultracytochemical results.Minced tissues were fixed in 3% glutaraldehyde-0.1 M phosphate buffered (pH 7.4) for 1.5 hr and rinsed overnight in several changes of 0.05 M phosphate buffer (pH 7.0) containing 7.5% sucrose. Tissues were incubated 30 min to 2 hr in Gomori acid phosphatase medium (2) containing 0.1 M substrate, either PC or βGP.

Tailoring microstructures of materials through biomimetics

1993 ◽  
Vol 51 ◽  
pp. 500-501
Author(s):  
Mehmet Sarikaya ◽  
Ilhan A. Aksay
Keyword(s):  
Chemical Properties ◽  
Design And Synthesis ◽  
Structure Sensitive ◽  
Macro Scale ◽  
Methods Of Synthesis ◽  
Successive Level ◽  
Engineering Materials ◽  
Physical And Chemical ◽  
And Chemical Properties ◽  
Synthesis Of Materials

Biomimetics involves investigation of structure, function, and methods of synthesis of biological composite materials. The goal is to apply this information to the design and synthesis of materials for engineering applications.Properties of engineering materials are structure sensitive through the whole spectrum of dimensions from nanometer to macro scale. The goal in designing and processing of technological materials, therefore, is to control microstructural evolution at each of these dimensions so as to achieve predictable physical and chemical properties. Control at each successive level of dimension, however, is a major challenge as is the retention of integrity between successive levels. Engineering materials are rarely fabricated to achieve more than a few of the desired properties and the synthesis techniques usually involve high temperature or low pressure conditions that are energy inefficient and environmentally damaging.In contrast to human-made materials, organisms synthesize composites whose intricate structures are more controlled at each scale and hierarchical order.

Proteasome inhibitors as therapeutics

2005 ◽  
Vol 41 ◽  
pp. 205-218
Author(s):  
Constantine S. Mitsiades ◽  
Nicholas Mitsiades ◽  
Teru Hideshima ◽  
Paul G. Richardson ◽  
Kenneth C. Anderson
Keyword(s):  
Multiple Myeloma ◽  
Drug Class ◽  
Proteasome Inhibitors ◽  
Cell Cycle Regulators ◽  
Current State ◽  
Intracellular Mechanism ◽  
Ubiquitin Proteasome ◽  
Proteasome Pathway ◽  
Hodgkin's Lymphomas ◽  
Clinical Research Data

The ubiquitin–proteasome pathway is a principle intracellular mechanism for controlled protein degradation and has recently emerged as an attractive target for anticancer therapies, because of the pleiotropic cell-cycle regulators and modulators of apoptosis that are controlled by proteasome function. In this chapter, we review the current state of the field of proteasome inhibitors and their prototypic member, bortezomib, which was recently approved by the U.S. Food and Drug Administration for the treatment of advanced multiple myeloma. Particular emphasis is placed on the pre-clinical research data that became the basis for eventual clinical applications of proteasome inhibitors, an overview of the clinical development of this exciting drug class in multiple myeloma, and a appraisal of possible uses in other haematological malignancies, such non-Hodgkin's lymphomas.

Design and synthesis of azaisoflavones

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
B Kang ◽  
YJ Jung ◽  
R Jeon
Keyword(s):  
Design And Synthesis

Computer modeling of the mitral valve for planning of complex repairs

2013 ◽  
Vol 61 (S 01) ◽  
Author(s):  
CJ Beller ◽  
I Baxter ◽  
K Kallenbach ◽  
T Mesana ◽  
M Labrosse
Keyword(s):  
Mitral Valve ◽  
Computer Modeling

The Role of Computer Modeling in Electrocardiography

1990 ◽  
Vol 29 (04) ◽  
pp. 282-288 ◽  
Author(s):  
A. van Oosterom
Keyword(s):  
Electrical Activity ◽  
Computer Modeling ◽  
Body Surface ◽  
Electrical Current ◽  
The Body ◽  
Volume Conductor ◽  
Current Generator ◽  
Cardiac Electrical Activity ◽  
Source Models

AbstractThis paper introduces some levels at which the computer has been incorporated in the research into the basis of electrocardiography. The emphasis lies on the modeling of the heart as an electrical current generator and of the properties of the body as a volume conductor, both playing a major role in the shaping of the electrocardiographic waveforms recorded at the body surface. It is claimed that the Forward-Problem of electrocardiography is no longer a problem. Several source models of cardiac electrical activity are considered, one of which can be directly interpreted in terms of the underlying electrophysiology (the depolarization sequence of the ventricles). The importance of using tailored rather than textbook geometry in inverse procedures is stressed.

Sign in / Sign up

Export Citation Format

Share Document