Selective inhibitors of medium-size S1′ pocket matrix metalloproteinases: a stepping stone of future drug discovery
Among various matrix metalloproteinases (MMPs), MMPs having medium-size S1′ pockets
are established as promising biomolecular targets for executing crucial roles in cancer …
are established as promising biomolecular targets for executing crucial roles in cancer …
Anticancer Drug Discovery based on Natural products: from computational approaches to Clinical studies
Globally, malignancies cause one out of six mortalities, which is a serious health problem.
Cancer therapy has always been challenging, apart from major advances in …
Cancer therapy has always been challenging, apart from major advances in …
Bifunctional HDAC therapeutics: one drug to rule them all?
JP Smalley, SM Cowley, JT Hodgkinson - Molecules, 2020 - mdpi.com
Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and
are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer …
are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer …
Paradigm shift of “classical” HDAC inhibitors to “hybrid” HDAC inhibitors in therapeutic interventions
GN Vaidya, P Rana, A Venkatesh… - European journal of …, 2021 - Elsevier
Abstract 'Epigenetic'regulation of genes via post-translational modulation of proteins is the
current mainstay approach for the disease therapies, particularly explored in the Histone …
current mainstay approach for the disease therapies, particularly explored in the Histone …
Is dual inhibition of metalloenzymes HDAC-8 and MMP-2 a potential pharmacological target to combat hematological malignancies?
For the last three decades, metalloenzymes such as histone deacetylases (HDACs) and
matrix metalloproteinases (MMPs) have been identified in promoting solid as well as …
matrix metalloproteinases (MMPs) have been identified in promoting solid as well as …
Robust design of some selective matrix metalloproteinase-2 inhibitors over matrix metalloproteinase-9 through in silico/fragment-based lead identification and de novo …
Broad range of selectivity possesses serious limitation for the development of matrix
metalloproteinase-2 (MMP-2) inhibitors for clinical purposes. To develop potent and …
metalloproteinase-2 (MMP-2) inhibitors for clinical purposes. To develop potent and …
Design of dual MMP-2/HDAC-8 inhibitors by pharmacophore mapping, molecular docking, synthesis and biological activity
Recent analyses have highlighted the promotion of cancer migration and invasion, mediated
through HDAC via MMP-2 and MMP-9. Since both class 1 HDACs and MMP-2/9 are …
through HDAC via MMP-2 and MMP-9. Since both class 1 HDACs and MMP-2/9 are …
Insight into the structural requirements of gelatinases (MMP-2 and MMP-9) inhibitors by multiple validated molecular modelling approaches: Part II
Inhibition of the matrix metalloproteinases (MMPs) is effective against metastasis of
secondary tumours. Previous MMP inhibitors have failed in clinical trials due to their off …
secondary tumours. Previous MMP inhibitors have failed in clinical trials due to their off …
Ligand-based design of anticancer MMP2 inhibitors: a review
MMP2, a Zn2+-dependent metalloproteinase, is related to cancer and angiogenesis.
Inhibition of this enzyme might result in a potential antimetastatic drug to leverage the …
Inhibition of this enzyme might result in a potential antimetastatic drug to leverage the …
Insight into the structural requirement of aryl sulphonamide based gelatinases (MMP-2 and MMP-9) inhibitors–Part I: 2D-QSAR, 3D-QSAR topomer CoMFA and Naïve …
Gelatinases [gelatinase A–matrix metalloproteinase-2 (MMP-2), gelatinase B–matrix
metalloproteinase-9 (MMP-9)] play key roles in many disease conditions including cancer …
metalloproteinase-9 (MMP-9)] play key roles in many disease conditions including cancer …