Current Topics in Medicinal Chemistry - Volume 15, Issue 1, 2015

Drug repositioning is an important component of therapeutic stratification in the precision medicine paradigm. Molecular profiling and more sophisticated analysis of longitudinal clinical data are refining definitions of human diseases, creating needs and opportunities to re-target or reposition approved drugs for alternative indications. Drug repositioning studies have demonstrated success in complex diseases requiri Read More

The traditional knowledge of medicinal plants that are in use by the indigenous Jaintia tribes residing in few isolated pockets of North-East India is documented here. The present study was carried out through the personal discussion with the president of the Jaintia Indigenous Herbal Medicine Association, Dr.H.Carehome Pakyntein from Jowai, Meghalaya. The plants being used generation after generation by his family of herbali Read More

Ribonucleotide reductase subunit R2 regulates catalytic action of the enzyme to provide DNA synthesis material via reduction. It has been continuously investigated as anticancer drug target for design and discovery of its inhibitors. Present studies aim to design novel heterocyclic/aryl substituted and adamantyl added thiosemicarbazones out fitted with improved cell permeability and effective RNR inhibition. Design stra Read More

Human immunodeficiency virus type 1 (HIV-1) integrase (IN) is an essential enzyme in the viral replication cycle as it catalyzes the insertion of the reverse transcribed viral DNA into host chromosome. The structure of prototype foamy virus (PFV) IN has structural and functional homology with HIV-1 IN (no full-length structure available). In this study, we have used PFV IN-DNA complex as a surrogate model for HIV-1 IN-DNA com Read More

Salbutamol forms an important and widely administered β2 agonist prescribed in the symptomatic treatment of bronchial asthma. Unfortunately, a subset of patients show refractoriness to it owing to ADRB2 gene variant (rs 1800888). The variant substitutes Thr to Ile at the position 164 in the β2 adrenergic receptor leading to sub-optimal binding of agonists. The present study aims to associate the Salbutamol response with th Read More

Since the discovery of Hsp90, a decade ago, it has surfaced as a potential target in breast cancer therapy along with other cancers. In present study, we have selected seven established Hsp inhibitors viz., PU3, CCT-018159, CNF-2024, SNX-5422, NVP (AUY-922), EGCG and IPI-504 used in the treatment of cancer. Considering these seven inhibitors as a parent compound, ligand based search was carried out with 90% similarity i Read More

Currently available antiviral drugs target the pol-encoded retroviral enzymes or integrases, in addition, inhibitors that target HIV-1 envelope-receptor interactions have also been recently approved. Recent understanding of the interactions between HIV-1 and host restriction factors has provided fresh avenues for development of novel antiviral drugs. For example, viral infectivity factor (Vif) now surfaced as an important Read More

Tubulin has picked up great focus as a major target in drug discovery and consequently, tubulin inhibitors have pulling in a considerable attention as anticancer agents. Numerable naturally occurring agents have focused on tubulin system act as an imperative target of cancer chemotherapy. Substantial number of tubulin inhibitors has been discovered so far and these agents are classified as indicated by their interaction. The Read More