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Literature DB >> 26985283

Epigenetic Medicinal Chemistry.

Abstract

The past decade has seen tremendous growth in our understanding of epigenetics and chromatin remodeling. Small, organic molecule modulators of a number of chromatin modifying proteins (CMPs) have been reported over this time frame and several of these have advanced to human clinical trials. In this Viewpoint, I summarize the current state of medicinal chemistry efforts focused on epigenetic targets and attempt to provide some insight into future directions on which the community may wish to focus.

Entities: Species

Year: 2015 PMID： 26985283 PMCID： PMC4753546 DOI： 10.1021/acsmedchemlett.5b00462

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

13 in total

Review 1. Epigenetic protein families: a new frontier for drug discovery.

Authors: Cheryl H Arrowsmith; Chas Bountra; Paul V Fish; Kevin Lee; Matthieu Schapira
Journal: Nat Rev Drug Discov Date: 2012-04-13 Impact factor: 84.694

2. Genetics of natural populations; recombination and variability in populations of Drosophila pseudoobscura.

Authors: T DOBZHANSKY
Journal: Genetics Date: 1946-05 Impact factor: 4.562

3. EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression.

Authors: Aline Renneville; Peter Van Galen; Matthew C Canver; Marie McConkey; John M Krill-Burger; David M Dorfman; Edward B Holson; Bradley E Bernstein; Stuart H Orkin; Daniel E Bauer; Benjamin L Ebert
Journal: Blood Date: 2015-08-28 Impact factor: 22.113

4. Inhibition of G9a methyltransferase stimulates fetal hemoglobin production by facilitating LCR/γ-globin looping.

Authors: Ivan Krivega; Colleen Byrnes; Jaira F de Vasconcellos; Y Terry Lee; Megha Kaushal; Ann Dean; Jeffery L Miller
Journal: Blood Date: 2015-05-15 Impact factor: 22.113

Review 5. Small molecule control of chromatin remodeling.

Authors: Aidan Finley; Robert A Copeland
Journal: Chem Biol Date: 2014-09-18

6. Combined DNA methyltransferase and histone deacetylase inhibition in the treatment of myeloid neoplasms.

Authors: Steven D Gore; Stephen Baylin; Elizabeth Sugar; Hetty Carraway; Carole B Miller; Michael Carducci; Michael Grever; Oliver Galm; Tianna Dauses; Judith E Karp; Michelle A Rudek; Ming Zhao; B Douglas Smith; Jasper Manning; Anchalee Jiemjit; George Dover; Abbie Mays; James Zwiebel; Anthony Murgo; Li-Jun Weng; James G Herman
Journal: Cancer Res Date: 2006-06-15 Impact factor: 12.701

7. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.

Authors: Sarah K Knutson; Natalie M Warholic; Tim J Wigle; Christine R Klaus; Christina J Allain; Alejandra Raimondi; Margaret Porter Scott; Richard Chesworth; Mikel P Moyer; Robert A Copeland; Victoria M Richon; Roy M Pollock; Kevin W Kuntz; Heike Keilhack
Journal: Proc Natl Acad Sci U S A Date: 2013-04-25 Impact factor: 11.205

8. DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.

Authors: Christine R Klaus; Dorothy Iwanowicz; Danielle Johnston; Carly A Campbell; Jesse J Smith; Mikel P Moyer; Robert A Copeland; Edward J Olhava; Margaret Porter Scott; Roy M Pollock; Scott R Daigle; Alejandra Raimondi
Journal: J Pharmacol Exp Ther Date: 2014-07-03 Impact factor: 4.030

Review 9. Epigenetics in human disease and prospects for epigenetic therapy.

Authors: Gerda Egger; Gangning Liang; Ana Aparicio; Peter A Jones
Journal: Nature Date: 2004-05-27 Impact factor: 49.962

10. Loss of BAP1 function leads to EZH2-dependent transformation.

Authors: Lindsay M LaFave; Wendy Béguelin; Richard Koche; Matt Teater; Barbara Spitzer; Alan Chramiec; Efthymia Papalexi; Matthew D Keller; Todd Hricik; Katerina Konstantinoff; Jean-Baptiste Micol; Benjamin Durham; Sarah K Knutson; John E Campbell; Gil Blum; Xinxu Shi; Emma H Doud; Andrei V Krivtsov; Young Rock Chung; Inna Khodos; Elisa de Stanchina; Ouathek Ouerfelli; Prasad S Adusumilli; Paul M Thomas; Neil L Kelleher; Minkui Luo; Heike Keilhack; Omar Abdel-Wahab; Ari Melnick; Scott A Armstrong; Ross L Levine
Journal: Nat Med Date: 2015-10-05 Impact factor: 53.440

1 in total

1. Rapid and Reliable Binding Affinity Prediction of Bromodomain Inhibitors: A Computational Study.

Authors: Shunzhou Wan; Agastya P Bhati; Stefan J Zasada; Ian Wall; Darren Green; Paul Bamborough; Peter V Coveney
Journal: J Chem Theory Comput Date: 2017-01-18 Impact factor: 6.006

1 in total