Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases

Pinard, Melissa A.; Boone, Christopher D.; Rife, Brittany D.; Supuran, Claudiu T.; McKenna, Robert

doi:10.1016/j.bmc.2013.08.033

Cited by 102 publications

(101 citation statements)

References 35 publications

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“…There was no statistically significant difference between two groups (p=0.924). The mean postoperative IOP (1 st day) of the first group was 15.27±2.90 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23) mmHg and that of the second group was 14.82±2.57 (SD) (11-23) mmHg. There was no statistically significant difference between two groups (p=0.505).…”

Section: Resultsmentioning

confidence: 98%

“…The most frequent ocular side effects of topical dorzolamide are burning and stinging. [13][14][15][16][17][18] The IOP lowering effect of dorzolamide is enhanced by combination of timolol maleate which is a beta-blocker. 14,19 In our study, we detected adverse effects of oral acetazolamide like headache, fatigue, polyuria, paraesthesia, nausea and vomiting.…”

Section: Discussionmentioning

confidence: 99%

“…R Re es su ul lt ts s: : The mean preoperative intraocular pressure (IOP) of the first group was 14.60±3.21 standard deviation (SD) (range 10-21) mmHg. and that of the second group was 14.67±2.77 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21) mmHg (p=0.924). The mean postoperative IOP(1 st day) of the first group was 15.27±2.90 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23) mmHg and that of the second group was 14.82±2.57 (SD) (11-23) mmHg (p=0.505).…”

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 94%

“…and that of the second group was 14.67±2.77 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21) mmHg (p=0.924). The mean postoperative IOP(1 st day) of the first group was 15.27±2.90 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23) mmHg and that of the second group was 14.82±2.57 (SD) (11-23) mmHg (p=0.505). The mean postoperative IOP (1 st week) of the first group was 13.72±2.44 (SD) (10-18) mmHg and that of the second group was 13.64±2.53 (SD) (10)(11)(12)(13)(14)(15)(16)(17)(18)(19) mmHg (p=0.895).…”

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 94%

“…The mean postoperative IOP(1 st day) of the first group was 15.27±2.90 (SD) (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23) mmHg and that of the second group was 14.82±2.57 (SD) (11-23) mmHg (p=0.505). The mean postoperative IOP (1 st week) of the first group was 13.72±2.44 (SD) (10-18) mmHg and that of the second group was 13.64±2.53 (SD) (10)(11)(12)(13)(14)(15)(16)(17)(18)(19) mmHg (p=0.895). C Co on nc cl lu us si io on n: : For prophylaxis of postoperative IOP rise after an uneventful cataract surgery, topical-dorzolamid timolol maleate combination and oral acetazolamide therapy have similar effects, however the adverse effects of systemic acetazolamide should be taken into account.…”

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 95%

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Comparison of Efficacy and Safety of Topical Dorzolamide-Timolol Maleate Combination with Oral Acetazolamide for Prevention of Intraocular Pressure Rise Following Phacoemulsification Surgery

Çetinkaya¹,

Akçam²,

Gürdağ³

et al. 2015

Turkiye Klinikleri J Ophthalmol

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A AB BS S T TR RA AC CT T O Ob bj je ec ct ti iv ve e: : To compare the efficacy and safety of topical dorzolamide-timolol maleate combination with oral acetazolamide for prevention of intraocular pressure rise following phacoemulsification surgery. M Ma at te er ri ia al l a an nd d M Me et th ho od ds s: : Sixty-seven eyes of 67 patients with cataracts (33 males, 34 females) who had undergone phacoemulsification and intraocular lens implantation surgery were evaluated retrospectively. Patients were divided into two groups. Group 1 comprised 33 (49%) patients who received oral acetazolamide 250 mg (Diazomid 250 mg tb) 1 hour before the surgery and 1hour after surgery and 125 mg 3 times a day for 3 days following surgery. Group 2 comprised 34 (51%) patients who received topical dorzolamidetimolol maleate combination 1 drop 1 hour before the surgery and twice a day for 3 days following surgery. R Re es su ul lt ts s: : The mean preoperative intraocular pressure (IOP) of the first group was 14.60±3.21 standard deviation (SD) (range 10-21) mmHg. and that of the second group was 14.67±2.77 (SD) (11-21) mmHg (p=0.924). The mean postoperative IOP(1 st day) of the first group was 15.27±2.90 (SD) (11-23) mmHg and that of the second group was 14.82±2.57 (SD) (11-23) mmHg (p=0.505). The mean postoperative IOP (1 st week) of the first group was 13.72±2.44 (SD) (10-18) mmHg and that of the second group was 13.64±2.53 (SD) (10-19) mmHg (p=0.895). C Co on nc cl lu us si io on n: : For prophylaxis of postoperative IOP rise after an uneventful cataract surgery, topical-dorzolamid timolol maleate combination and oral acetazolamide therapy have similar effects, however the adverse effects of systemic acetazolamide should be taken into account. Therefore it is better to prefer topical dorzolamide-timolol maleate combination therapy. K Ke ey y W Wo or rd ds s: : Phacoemulsification; intraocular pressure; acetazolamide; dorzolamide-timolol combination Ö ÖZ ZE ET T A Am ma aç ç: : Fakoemülsifikasyon cerrahisi sonrası artan göziçi basıncını azaltmak için kullanılan ağızdan verilen asetazolamid ile damla şeklinde uygulanan dorzolamid-timolol maleat kombinasyonunun etkinlik ve güvenilirliğinin kıyaslanmasıdır. G Ge er re eç ç v ve e Y Yö ön nt te em ml le er r: : Kataraktı olan ve fakoemülsifikasyon ve göziçi mercek (GİM) implantasyon cerrahisi geçiren 67 (33 erkek, 34 kadın) hastanın 67 gözü retrospektif olarak değerlendirildi. Hastalar iki gruba ayrıldılar. 1. grup 33 (%49) hastadan oluşmaktaydı, bu gruptaki hastalara ameliyattan 1 saat önce ve 1 saat sonra ağızdan 250 mg asetazolamid (toplam 500 mg) verildi ve ameliyattan sonraki 3 gün boyunca da 125 mg asetazolamid 3x1 önerildi. 2. grup 34 (%51) hastadan oluşmaktaydı, bu gruptaki hastalara ameliyattan 1 saat önce 1 damla dorzolamid-timolol maleat kombinasyonu uygulandı ve ameliyattan sonraki 3 gün boyunca da damla şeklinde dorzolamid-timolol maleat kombinasyonu 2x1 şek-linde önerildi. B Bu ul lg gu ul la ar r: : 1. grubun ortalama ameliyat öncesi göziçi basınç değeri 14,60±3,21 (SD)...

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Section: Resultsmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 94%

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 94%

Section: Comparison Of Efficacy and Safety Of Topical Dorzolamide-timmentioning

confidence: 95%

See 3 more Smart Citations

Comparison of Efficacy and Safety of Topical Dorzolamide-Timolol Maleate Combination with Oral Acetazolamide for Prevention of Intraocular Pressure Rise Following Phacoemulsification Surgery

Çetinkaya¹,

Akçam²,

Gürdağ³

et al. 2015

Turkiye Klinikleri J Ophthalmol

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Protein crystallization and structure determination at room temperature in the CrystalChip

Pachl,

Coudray,

Vincent

et al. 2024

FEBS Open Bio

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The production of high‐quality crystals is a key step in crystallography in general, but control of crystallization conditions is even more crucial in serial crystallography, which requires sets of crystals homogeneous in size and diffraction properties. This protocol describes the implementation of a simple and user‐friendly microfluidic device that allows both the production of crystals by the counter‐diffusion method and their in situ analysis by serial crystallography. As an illustration, the whole procedure is used to determine the crystal structure of three proteins from data collected at room temperature at a synchrotron radiation source.

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Structure–Activity Relationships of Benzenesulfonamide‐Based Inhibitors towards Carbonic Anhydrase Isoform Specificity

et al. 2016

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Carbonic anhydrases (CAs) are implicated in a wide range of diseases, including the upregulation of isoforms CA IX and XII in many aggressive cancers. However, effective inhibition of disease-implicated CAs should minimally affect the ubiquitously expressed isoforms, including CA I and II, to improve directed distribution of the inhibitors to the cancer-associated isoforms and reduce side effects. Four benzenesulfonamide-based inhibitors were synthesized by using the tail approach and displayed nanomolar affinities for several CA isoforms. The crystal structures of the inhibitors bound to a CA IX mimic and CA II are presented. Further in silico modeling was performed with the inhibitors docked into CA I and XII to identify residues that contributed to or hindered their binding interactions. These structural studies demonstrated that active-site residues lining the hydrophobic pocket, especially positions 92 and 131, dictate the positional binding and affinity of inhibitors, whereas the tail groups modulate CA isoform specificity. Geometry optimizations were performed on each ligand in the crystal structures and showed that the energetic penalties of the inhibitor conformations were negligible compared to the gains from active-site interactions. These studies further our understanding of obtaining isoform specificity when designing small molecule CA inhibitors.

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Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases

Cited by 102 publications

References 35 publications

Comparison of Efficacy and Safety of Topical Dorzolamide-Timolol Maleate Combination with Oral Acetazolamide for Prevention of Intraocular Pressure Rise Following Phacoemulsification Surgery

Comparison of Efficacy and Safety of Topical Dorzolamide-Timolol Maleate Combination with Oral Acetazolamide for Prevention of Intraocular Pressure Rise Following Phacoemulsification Surgery

Protein crystallization and structure determination at room temperature in the CrystalChip

Structure–Activity Relationships of Benzenesulfonamide‐Based Inhibitors towards Carbonic Anhydrase Isoform Specificity

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