8 research outputs found
Promising Microalgae Resources in Assam
56-57Assam is a biological hotspot with many rare and endemic plant and animal species. These rich and diverse bioresources of the region are yet to be explored for their potential biotechnological applications
Nonlinear distance measures under the framework of Pythagorean fuzzy sets with applications in problems of pattern recognition, medical diagnosis, and COVID-19 medicine selection
Abstract Background The concept of Pythagorean fuzzy sets (PFSs) is an utmost valuable mathematical framework, which handles the ambiguity generally arising in decision-making problems. Three parameters, namely membership degree, non-membership degree, and indeterminate (hesitancy) degree, characterize a PFS, where the sum of the square of each of the parameters equals one. PFSs have the unique ability to handle indeterminate or inconsistent information at ease, and which demonstrates its wider scope of applicability over intuitionistic fuzzy sets. Results In the present article, we opt to define two nonlinear distances, namely generalized chordal distance and non-Archimedean chordal distance for PFSs. Most of the established measures possess linearity, and we cannot incorporate them to approximate the nonlinear nature of information as it might lead to counter-intuitive results. Moreover, the concept of non-Archimedean normed space theory plays a significant role in numerous research domains. The proficiency of our proposed measures to overcome the impediments of the existing measures is demonstrated utilizing twelve different sets of fuzzy numbers, supported by a diligent comparative analysis. Numerical examples of pattern recognition and medical diagnosis have been considered where we depict the validity and applicability of our newly constructed distances. In addition, we also demonstrate a problem of suitable medicine selection for COVID-19 so that the transmission rate of the prevailing viral pandemic could be minimized and more lives could be saved. Conclusions Although the issues concerning the COVID-19 pandemic are very much challenging, yet it is the current need of the hour to save the human race. Furthermore, the justifiable structure of our proposed distances and also their feasible nature suggest that their applications are not only limited to some specific research domains, but decision-makers from other spheres as well shall hugely benefit from them and possibly come up with some further extensions of the ideas
Membrane Interaction and Protein Kinase C‑C1 Domain Binding Properties of 4‑Hydroxy-3-(hydroxymethyl) Phenyl Ester Analogues
Protein kinase C (PKC)-C1 domain
targeted regulator development
is considered as a potential therapeutic strategy for the treatment
of cancer and immunological and other diseases. Efforts are underway
to synthesize small molecules to achieve higher specificity for the
C1-domain than the natural activator, diacylglycerols (DAGs). In this
regard, we conveniently synthesized 4-hydroxy-3-(hydroxymethyl) phenyl
ester analogues and measured in vitro C1-domain binding properties.
We also investigated different physicochemical properties of the synthesized
molecules, including aggregation behavior in aqueous solution and
interaction with lipid bilayers, and others with an aim for better
understanding of their C1-domain binding properties. The results showed
that the membrane-active compounds aggregate in aqueous solution at
a reasonably lower concentration and strongly interact with the lipid
bilayer. The hydrophilic part of the compounds localize at the bilayer/water
interface and accessible for C1-domain binding. Biophysical studies
revealed that the hydroxyl, hydroxymethyl, and carbonyl groups and
acyl chain length are important for their interaction with the C1-domain.
The potent compound showed more than 10-fold stronger binding affinity
for the C1-domains than DAG under similar experimental conditions.
Therefore, our findings reveal that these ester analogues represent
an attractive group of C1-domain ligands that can be further structurally
modified to improve their binding and activity
Effects of Ortho Substituent Groups of Protocatechualdehyde Derivatives on Binding to the C1 Domain of Novel Protein Kinase C
Diacylglycerol (DAG) regulates a broad range of cellular
functions
including tumor promotion, apoptosis, differentiation, and growth.
Thus, the DAG-responsive C1 domain of protein kinase C (PKC) isoenzymes
is considered to be an attractive drug target for the treatment of
cancer and other diseases. To develop effective PKC regulators, we
conveniently synthesized (hydroxymethyl)Âphenyl ester analogues targeted
to the DAG binding site within the C1 domain. Biophysical studies
and molecular docking analysis showed that the hydroxymethyl group,
hydrophobic side chains, and acyl group at the ortho position are
essential for their interactions with the C1-domain backbone. Modifications
of these groups showed diminished binding to the C1 domain. The active
(hydroxymethyl)Âphenyl ester analogues showed more than 5-fold stronger
binding affinity for the C1 domain than DAG. Therefore, our findings
reveal that (hydroxymethyl)Âphenyl ester analogues represent an attractive
group of C1-domain ligands that can be further structurally modified
to improve their binding and activity
Effects of Ortho Substituent Groups of Protocatechualdehyde Derivatives on Binding to the C1 Domain of Novel Protein Kinase C
Diacylglycerol (DAG) regulates a broad range of cellular
functions
including tumor promotion, apoptosis, differentiation, and growth.
Thus, the DAG-responsive C1 domain of protein kinase C (PKC) isoenzymes
is considered to be an attractive drug target for the treatment of
cancer and other diseases. To develop effective PKC regulators, we
conveniently synthesized (hydroxymethyl)Âphenyl ester analogues targeted
to the DAG binding site within the C1 domain. Biophysical studies
and molecular docking analysis showed that the hydroxymethyl group,
hydrophobic side chains, and acyl group at the ortho position are
essential for their interactions with the C1-domain backbone. Modifications
of these groups showed diminished binding to the C1 domain. The active
(hydroxymethyl)Âphenyl ester analogues showed more than 5-fold stronger
binding affinity for the C1 domain than DAG. Therefore, our findings
reveal that (hydroxymethyl)Âphenyl ester analogues represent an attractive
group of C1-domain ligands that can be further structurally modified
to improve their binding and activity