Role of Small-Molecule Modifiers in Replication Initiation

Author(s):  
Giacomo De Piccoli ◽  
Agnieszka Gambus
Author(s):  
Shohei Kumagai ◽  
Craig P. Yu ◽  
Shunsuke Nakano ◽  
Tatsuro Annaka ◽  
Masato Mitani ◽  
...  

Author(s):  
Guoqiang Sun ◽  
Dawei Rong ◽  
Zhouxiao Li ◽  
Guangshun Sun ◽  
Fan Wu ◽  
...  

Research on molecular targeted therapy of tumors is booming, and novel targeted therapy drugs are constantly emerging. Small molecule targeted compounds, novel targeted therapy drugs, can be administered orally as tablets among other methods, and do not draw upon genes, causing no immune response. It is easily structurally modified to make it more applicable to clinical needs, and convenient to promote due to low cost. It refers to a hotspot in the research of tumor molecular targeted therapy. In the present study, we review the current Food and Drug Administration (FDA)-approved use of small molecule targeted compounds in tumors, summarize the clinical drug resistance problems and mechanisms facing the use of small molecule targeted compounds, and predict the future directions of the evolving field.


2019 ◽  
Author(s):  
Christopher Southan

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.


F1000Research ◽  
2017 ◽  
Vol 6 ◽  
pp. 1015 ◽  
Author(s):  
Matthew S. Stratton ◽  
Saptarsi M. Haldar ◽  
Timothy A. McKinsey

Fibrosis is defined as excess deposition of extracellular matrix, resulting in tissue scarring and organ dysfunction. It is estimated that 45% of deaths in the developed world are due to fibrosis-induced organ failure. Despite the well-accepted role of fibrosis in the pathogenesis of numerous diseases, there are only two US Food and Drug Administration–approved anti-fibrotic therapies, both of which are currently restricted to the treatment of pulmonary fibrosis. Thus, organ fibrosis represents a massive unmet medical need. Here, we review recent findings suggesting that an epigenetic regulatory protein, BRD4, is a nodal effector of organ fibrosis, and we highlight the potential of small-molecule BRD4 inhibitors for the treatment of diverse fibrotic diseases.


2019 ◽  
Author(s):  
Christopher Southan

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.


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