Matches in SemOpenAlex for { <https://semopenalex.org/work/W4367394089> ?p ?o ?g. }
- W4367394089 endingPage "1062" @default.
- W4367394089 startingPage "1039" @default.
- W4367394089 abstract "Small molecule drugs that covalently bind irreversibly to their target proteins have several advantages over conventional reversible inhibitors. They include increased duration of action, less-frequent drug dosing, reduced pharmacokinetic sensitivity, and the potential to target intractable shallow binding sites. Despite these advantages, the key challenges of irreversible covalent drugs are their potential for off-target toxicities and immunogenicity risks. Incorporating reversibility into covalent drugs would lead to less off-target toxicity by forming reversible adducts with off-target proteins and thus reducing the risk of idiosyncratic toxicities caused by the permanent modification of proteins, which leads to higher levels of potential haptens. Herein, we systematically review electrophilic warheads employed during the development of reversible covalent drugs. We hope the structural insights of electrophilic warheads would provide helpful information to medicinal chemists and aid in designing covalent drugs with better on-target selectivity and improved safety." @default.
- W4367394089 created "2023-04-30" @default.
- W4367394089 creator A5025114145 @default.
- W4367394089 creator A5039590241 @default.
- W4367394089 creator A5047418048 @default.
- W4367394089 creator A5067699236 @default.
- W4367394089 date "2023-04-29" @default.
- W4367394089 modified "2023-10-16" @default.
- W4367394089 title "An update on the discovery and development of reversible covalent inhibitors" @default.
- W4367394089 cites W1526377515 @default.
- W4367394089 cites W1545065453 @default.
- W4367394089 cites W1948191447 @default.
- W4367394089 cites W1968310807 @default.
- W4367394089 cites W1975302732 @default.
- W4367394089 cites W1983759759 @default.
- W4367394089 cites W2002368219 @default.
- W4367394089 cites W2010654750 @default.
- W4367394089 cites W2010993054 @default.
- W4367394089 cites W2012437459 @default.
- W4367394089 cites W2019792957 @default.
- W4367394089 cites W2023033918 @default.
- W4367394089 cites W2046306695 @default.
- W4367394089 cites W2053997941 @default.
- W4367394089 cites W2061618283 @default.
- W4367394089 cites W2089553497 @default.
- W4367394089 cites W2129577287 @default.
- W4367394089 cites W2133776410 @default.
- W4367394089 cites W2133778100 @default.
- W4367394089 cites W2134917212 @default.
- W4367394089 cites W2136920201 @default.
- W4367394089 cites W2141361007 @default.
- W4367394089 cites W2145606109 @default.
- W4367394089 cites W2153977062 @default.
- W4367394089 cites W2154568785 @default.
- W4367394089 cites W2165398766 @default.
- W4367394089 cites W2261920671 @default.
- W4367394089 cites W2322836762 @default.
- W4367394089 cites W2338200863 @default.
- W4367394089 cites W2473899407 @default.
- W4367394089 cites W2474204065 @default.
- W4367394089 cites W2475019041 @default.
- W4367394089 cites W2495203971 @default.
- W4367394089 cites W2508430021 @default.
- W4367394089 cites W2517282085 @default.
- W4367394089 cites W2550486321 @default.
- W4367394089 cites W2553361146 @default.
- W4367394089 cites W2559265740 @default.
- W4367394089 cites W2606604357 @default.
- W4367394089 cites W2622009965 @default.
- W4367394089 cites W2676228912 @default.
- W4367394089 cites W2761579533 @default.
- W4367394089 cites W2785468597 @default.
- W4367394089 cites W2791369833 @default.
- W4367394089 cites W2794813379 @default.
- W4367394089 cites W2796108867 @default.
- W4367394089 cites W2882991765 @default.
- W4367394089 cites W2910570560 @default.
- W4367394089 cites W2949202626 @default.
- W4367394089 cites W2968913253 @default.
- W4367394089 cites W3004578208 @default.
- W4367394089 cites W3005775246 @default.
- W4367394089 cites W3011428441 @default.
- W4367394089 cites W3011701533 @default.
- W4367394089 cites W3014843513 @default.
- W4367394089 cites W3020300207 @default.
- W4367394089 cites W3033697130 @default.
- W4367394089 cites W3034228022 @default.
- W4367394089 cites W3036059651 @default.
- W4367394089 cites W3044277392 @default.
- W4367394089 cites W3080596815 @default.
- W4367394089 cites W3083643109 @default.
- W4367394089 cites W3087582521 @default.
- W4367394089 cites W3090894484 @default.
- W4367394089 cites W3096399688 @default.
- W4367394089 cites W3097591292 @default.
- W4367394089 cites W3109863631 @default.
- W4367394089 cites W3111372677 @default.
- W4367394089 cites W3124667367 @default.
- W4367394089 cites W3127932706 @default.
- W4367394089 cites W3130357905 @default.
- W4367394089 cites W3131767541 @default.
- W4367394089 cites W3134120587 @default.
- W4367394089 cites W3135105068 @default.
- W4367394089 cites W3145730265 @default.
- W4367394089 cites W3162589029 @default.
- W4367394089 cites W3165161076 @default.
- W4367394089 cites W3167205542 @default.
- W4367394089 cites W3168783480 @default.
- W4367394089 cites W3176883952 @default.
- W4367394089 cites W3190222902 @default.
- W4367394089 cites W3193440777 @default.
- W4367394089 cites W3204148409 @default.
- W4367394089 cites W3205127490 @default.
- W4367394089 cites W3210621584 @default.
- W4367394089 cites W4205202684 @default.
- W4367394089 cites W4220932642 @default.
- W4367394089 cites W4223439908 @default.
- W4367394089 cites W4224253542 @default.