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| 1 | Malaria parasite carbonic anhydrase:inhibition of aromatic/heterocyclic sulfonamides and its therapeutic potential显示文摘Plasmodium falciparum(P.falciparum) is responsible for the majority of life-threatening cases of human malaria,causing 1.5-2.7 million annual deaths.The global emergence of drug-resistant malaria parasites necessitates identification and characterisation of novel drug targets and their potential inhibitors.We identified the carbonic anhydrase(CA) genes in P.falciparum.The pfGA gene encodes an α-carbonic anhydrase,a Zn^(2+)-metalloenzme,possessing catalytic properties distinct from that of the human host CA enzyme.The amino acid sequence of the pfCA enzyme is different from the analogous protozoan and human enzymes.A library of aromatic/heterocyclic sulfonamides possessing a large diversity of scaffolds were found to be very good inhibitors for the malarial enzyme at moderate-low micromolar and submicromolar inhibitions.The structure of the groups substituting the aromatic-ureido-or aromatic-azomethine fragment of the molecule and the length of the parent sulfonamide were critical parameters for the inhibitory properties of the sulfonamides.One derivative,that is,4-(3,4-dichlorophenylureido)thioureidobcnzcnesulfonamide(compound 10) was the most effective in vitro Plasmodium falciparum CA inhibitor,and was also the most effective antimalarial compound on the in vitro P.falciparum growth inhibition.The compound 10 was also effective in vivo antimalarial agent in mice infected with Plasmodium berghei,an animal model of drug testing for human malaria infection. It is therefore concluded that the sulphonamide inhibitors targeting the parasite CA may have potential for the development of novel therapies against human malaria. | Sudaratana R Krungkrai Jerapan Krungkrai | 2011 | Asian Pacific Journal of Tropical Biomedicine2011，1，3： | 10 |
| 2 | Artemisinin resistance or tolerance in human malaria patients显示文摘Malaria is a major cause of morbidity and mortality in the developing world.This situation is mainly due to emergence of resistance to most antimalarial drugs currently available. Artemisinin-based combination treatments are now first-line drugs for Plasmodium falciparum (P.falciparum) malaria.Artemisinin(qinghaosu) and its derivatives are the most rapid acting and efficacious antimalarial drugs.This review highlights most recent investigations into the emergence of artemisinin resistance in falciparum malaria patients on the Thai-Cambodian border,a historical epicenter for multidrug resistance spread spanning over 50 years.The study presents the first evidence that highlights the parasites reduced susceptibility to artemisinin treatment by prolonged parasite-clearance times,raising considerable concern on resistance development.Although the exact mechanism of action remains unresolved,development of resistance was proposed based from both in vitro experiments and human patients.Lines of evidence suggested that the parasites in the patients are in dormant forms,presumably tolerate to the drug pressure.The World Health Organization has launched for prevention and/or containment of the artemisinin-resistant malaria parasites.Taken together,the emergence of artemisinin resistance to the most potent antidote for falciparum malaria,poses a serious threat to global malaria control and prompts renewed efforts for urgent development of new antimalarial weapons. | Jerapan Krungkrai Waranya Imprasittichai Sumintra Otjungreed Sawirasagee Pongsabut Sudaratana R Krungkrai | 2010 | Asian Pacific Journal of Tropical Medicine2010，3，9： | 4 |
| 3 | Antimalarial qinghaosu/artemisinin: The therapy worthy of a Nobel Prize显示文摘Malaria is a major cause of human morbidity and mortality in the tropical endemic countries worldwide. This is largely due to the emergence and spread of resistance to most antimalarial drugs currently available. Based on the World Health Organization recommendation, artemisinin-based combination therapies are now used as first-line treatment for Plasmodium falciparum malaria. Artemisinin or qinghaosu(Chinese name) and its derivatives are highly potent, rapidly acting antimalarial drugs. Artemisinin was discovered in 1971 by a Chinese medical scientist Youyou Tu, who was awarded the Nobel Prize in 2015 on her discovering the antimalarial properties of qinghaosu from the traditional Chinese qinghao plant. Nevertheless, artemisinin resistance in falciparum malaria patients has first emerged on the Thai-Cambodian border in 2009, which is now prevalent across mainland Southeast Asia from Vietnam to Myanmar. Here, we reviewed malaria disease severity, history of artemisinin discovery, chemical structure, mechanism of drug action, artemisinin-based combination therapies, emergence and spread of drug resistance, including the recent findings on mechanism of resistance in the falciparum malaria parasite. This poses a serious threat to global malaria control and prompts renewed efforts for the urgent development of new antimalarial drugs. | Jerapan Krungkrai Sudaratana Rochanakij Krungkrai | 2016 | Asian Pacific Journal of Tropical Biomedicine2016，6，5： | 2 |
| 4 | Carbonic anhydrase inhibitors: Inhibition of Plasmodium faleiparumcarbonic anhydrase with aromatic/ heterocyclic sulfonamides in vitro and in vivo studies 显示文摘 | JERAPAN K SUDARATANA R K CLAUDIU T S | 2008 | Bioorganic Medicinal Chemistry Letters2008，18，： | 1 |
| 5 | Crystallization and preliminary X‐ray diffraction analysis of orotate phosphoribosyltransferase from the human malaria parasite Plasmodium falciparum显示文摘 | Yasuhide Takashima Eiichi Mizohata Keiji Tokuoka Sudaratana R. Krungkrai Yukiko Kusakari Saki Konishi Atsuko Satoh Hiroyoshi Matsumura Jerapan Krungkrai Toshihiro Horii Tsuyoshi Inoue | 2012 | Acta Cryst. F2012，，： | 1 |
| 6 | Kinetic benefits and thermal stability of orotate phosphoribosyltransferase and orotidine 5′-monophosphate decarboxylase enzyme complex in human malaria parasite Plasmodium falciparum显示文摘 | Panan Kanchanaphum Jerapan Krungkrai | 2009 | Biochemical and Biophysical Research Communications2009，，： | 1 |
| 7 | Carbonic anhydrase inhibitors: Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides—in vitro and in vivo studies显示文摘 | Jerapan Krungkrai Sudaratana R. Krungkrai Claudiu T. Supuran | 2008 | Bioorganic & Medicinal Chemistry Letters2008，，： | 1 |
| 8 | Characterisation of carbonic anhydrase in Plasmodium falciparum显示文摘 | Sudaratana R Krungkrai Nongluk Suraveratum Sunant Rochanakij Jerapan Krungkrai | 2001 | International Journal for Parasitology2001，，： | 1 |
| 9 | Kinetic benefits and thermal stability of orotate phosphoribosyltransferase and orotidine 5′-monophosphate decarboxylase enzyme complex in human malaria parasite Plasmodium falciparum显示文摘 | Panan Kanchanaphum Jerapan Krungkrai | 2009 | Biochemical and Biophysical Research Communications2009，，2： | 1 |
| 10 | Dihydroorotase of human malarial parasite Plasmodium falciparum differs from host enzyme显示文摘 | Sudaratana R. Krungkrai Nuchanat Wutipraditkul Jerapan Krungkrai | 2007 | Biochemical and Biophysical Research Communications2007，，3： | 1 |
| 11 | Purification, characterization and localization of mitochondrial dihydroorotate dehydrogenase in Plasmodium falciparum , human malaria parasite显示文摘 | Jerapan Krungkrai | 1995 | BBA - General Subjects1995，，： | 1 |
| 12 | Human malaria parasite orotate phosphoribosyltransferase: functional expression, characterization of kinetic reaction mechanism and inhibition profile显示文摘 | Sudaratana R Krungkrai Sayaka Aoki Nirianne Marie Q Palacpac Dan Sato Toshihide Mitamura Jerapan Krungkrai Toshihiro Horii | 2004 | Molecular & Biochemical Parasitology2004，，2： | 1 |
| 13 | Orotate phosphoribosyltransferase and orotidine 5 ′ -monophosphate decarboxylase exist as multienzyme complex in human malaria parasite Plasmodium falciparum显示文摘 | Sudaratana R Krungkrai Phisit Prapunwattana Toshihiro Horii Jerapan Krungkrai | 2004 | Biochemical and Biophysical Research Communications2004，，4： | 1 |
| 14 | Human malaria parasite orotate phosphoribosyltransferase: functional expression, characterization of kinetic reaction mechanism and inhibition profile显示文摘 | Sudaratana R Krungkrai Sayaka Aoki Nirianne Marie Q Palacpac Dan Sato Toshihide Mitamura Jerapan Krungkrai Toshihiro Horii | 2004 | Molecular & Biochemical Parasitology2004，，： | 1 |
| 15 | Orotate phosphoribosyltransferase and orotidine 5 ′ -monophosphate decarboxylase exist as multienzyme complex in human malaria parasite Plasmodium falciparum显示文摘 | Sudaratana R Krungkrai Phisit Prapunwattana Toshihiro Horii Jerapan Krungkrai | 2004 | Biochemical and Biophysical Research Communications2004，，： | 1 |
| 16 | Carbonic anhydrase inhibitors. Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic sulfonamides: towards antimalarials with a novel mechanism of action?显示文摘 | Jerapan Krungkrai Andrea Scozzafava Sutarnthip Reungprapavut Sudaratana R. Krungkrai Roonglawan Rattanajak Sumalee Kamchonwongpaisan Claudiu T. Supuran | 2004 | Bioorganic & Medicinal Chemistry2004，，： | 1 |
| 17 | Purification, characterization and localization of mitochondrial dihydroorotate dehydrogenase in Plasmodium falciparum , human malaria parasite显示文摘 | Jerapan Krungkrai | 1995 | BBA - General Subjects1995，，3： | 1 |
| 18 | Crystallization and preliminary crystallographic analysis of orotidine 5′‐monophosphate decarboxylase from the human malaria parasite Plasmodium falciparum显示文摘 | Sudaratana R. Krungkrai Keiji Tokuoka Yukiko Kusakari Tsuyoshi Inoue Hiroaki Adachi Hiroyoshi Matsumura Kazufumi Takano Satoshi Murakami Yusuke Mori Yasushi Kai Jerapan Krungkrai Toshihiro Horii | 2006 | Acta Cryst. F2006，，： | 1 |
| 19 | Carbonic anhydrase inhibitors: Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heteroeyclic sulfonamides in vitro and in vivo studies显示文摘 | JERAPAN K SUDARATANA R K CLAUDIU T S | 2008 | Bioorganic Medicinal Chemistry Letters2008，18，： | 1 |
| 20 | Dihydroorotase of human malarial parasite Plasmodium falciparum differs from host enzyme显示文摘 | Sudaratana R. Krungkrai Nuchanat Wutipraditkul Jerapan Krungkrai | 2007 | Biochemical and Biophysical Research Communications2007，，： | 1 |
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