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1.
Mol Divers ; 25(1): 603-624, 2021 Feb.
Article in English | MEDLINE | ID: mdl-32886304

ABSTRACT

Breast cancer is the most prominent, frequently diagnosed and leading cause of death among women. Estrogen is an agonist of estrogen receptor alpha (ER-α), expressed in mammary glands and is responsible for initiating many signalling pathways that lead to differentiation and development of breast tissue. Any mutations in these signalling pathways result in irregular growth of mammary tissue, leading to the development of tumour or cancer. All these observations attract the attention of researchers to antagonize ER-α receptor either by developing selective estrogen receptor modulators or by selective estrogen receptor degraders. Therefore, this article provides a brief overview of various factors that are responsible for provoking breast cancer in women and design strategies recently used by the various research groups across the world for antagonizing or demodulating ER-α.


Subject(s)
Breast Neoplasms/drug therapy , Estrogen Receptor alpha/metabolism , Molecular Targeted Therapy , Estrogen Receptor alpha/antagonists & inhibitors , Female , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/pharmacology , Heterocyclic Compounds/therapeutic use , Humans , Models, Molecular
2.
Chem Biol Drug Des ; 100(3): 443-468, 2022 09.
Article in English | MEDLINE | ID: mdl-35763448

ABSTRACT

Inhibition of xanthine oxidase (XO) is an effective and most prominent therapeutic approach for the management of gout. Discovery of its association in the pathophysiology of diabetes, cardiovascular disorders, etc., widened its therapeutic horizons. Limited drug candidates in clinical practice along with side effects forced researchers to develop more efficacious and safer XO inhibitors for the management of gout and other disorders associated with XO hyperactivity. In this regard, this review focus on (a) various drug candidates in clinical practice and under clinical trials, (b) Development of various heterocyclic motifs as XO inhibitors in last two decades and (c) various patented synthetic XO inhibitors.


Subject(s)
Gout , Xanthine Oxidase , Enzyme Inhibitors/pharmacology , Enzyme Inhibitors/therapeutic use , Gout/drug therapy , Humans
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